Michelle Arkin, PhD

Chair and Thomas William and Frederick John MacWilliam Distinguished Professor
Department of Pharmaceutical Chemistry
[email protected]
Phone: +1 415 514-4313
600 16th Street, Rm S512D
UCSF Box 2280
San Francisco, CA 94158
United States

Links

Arkin Lab UCSF Profiles

Affiliations

Education programs

PharmD Degree Program

UCSF centers, institutes, and research programs

Codirector, Small Molecule Discovery Center (SMDC)
Quantitative Biosciences Institute (QBI)
Adjunct Professor, Buck Institute for Research on Aging
UCSF Helen Diller Family Comprehensive Cancer Center

What I do

My research focuses on the development of drug-like molecules that alter important biological processes. These molecules will help us understand human biology and may lead to the design of new drugs. I also chair the Department of Pharmaceutical Chemistry. Details: Administration.

Departmental research area

chemical biology and medicinal chemistry
protein and cellular engineering

My research expertise

protein-protein interaction (PPI), allostery, enzymology, fragment-based lead discovery, neglected tropical diseases, neurodegeneration, Oncology, high-throughput screening (HTS)

Professional background

Degrees

PhD, Chemistry, California Institute of Technology (Caltech)
BA, Chemistry, Bryn Mawr College

Biography

Michelle’s lab develops innovative approaches to screen for chemical tools and drug leads, using biophysical approaches like fragment-based drug discovery and biological approaches including high-content imaging with primary cells and organisms. Our goal is to demonstrate ‘druggability’ of new target classes and to use our compounds to discover new targets for drug discovery. Areas of interest include protein-protein interactions, allosteric and scaffolding sites in enzymes, and orphan and neglected diseases. Michelle is co-Director of the Small Molecule Discovery Center, a collaborative research and core lab that includes a high-throughput screening facility and medicinal chemistry (smdc.ucsf.edu).

Research keywords

  • Interleukin-2
  • Protein Interaction Maps
  • Cysteine Endopeptidases
  • Small Molecule Libraries
  • proteins
  • Autophagy
  • High-Throughput Screening Assays
  • Caspase 6
  • Adenosine Triphosphatases
  • Estrogen Receptor alpha
  • 14-3-3 Proteins
  • Protein Binding
  • Preclinical Drug Evaluation
  • Cysteine
  • Drug Discovery
1. A new vision for the Small Molecule Discovery Center
2. School of Pharmacy shows out in Grad Slam storytelling competition
3. Update from the Dean: Putting plans in action
4. Celebrating women leaders in the School of Pharmacy
5. Manglik, Arkin, Bastian receive Mark Foundation ASPIRE Award for moonshot cancer research
6. UCSF School of Pharmacy leads in NIH funding for the 43rd straight year
7. Update from the Dean: Ongoing excellence and new frontiers
8. Pirating proteins for biomedicine
9. New clues in the hunt for Alzheimer’s therapies
10. UCSF QBI Coronavirus Research Group awarded $67.5 million to develop therapies for future pandemics
11. School community bids farewell to an impactful dean
12. Helium recycling project sets a new standard for sustainability at UCSF
13. Update from the Dean: Recovery and resilience after a pandemic year
14. Update from the Dean: Community during challenging times
15. Arkin named next chair of Department of Pharmaceutical Chemistry
16. Update from the Dean: Confronting racism and health inequities
17. School of Pharmacy leads in LivingGreen certifications
18. School reflects on legacy of achievement at Alumni Weekend 2019
19. Grants & Fellowships: Summer 2018
20. Arkin receives Ono Pharma Foundation Breakthrough Science Initiative Award
21. Showcasing School science and change at Alumni Weekend 2018
22. The epic journey to better medicines
23. Update from the Dean – March 2018
24. UCSF School of Pharmacy joins data-sharing partnership to speed cancer drugs
25. Update from the Dean - Spring/Summer 2014
26. Update from the Dean - Fall 2012
27. Teaching old drugs new tricks at the Small Molecule Discovery Center: arthritis drug could treat dysentery
28. Update from the Dean - Fall/Winter 2010
29. UCSF researchers join consortium to target cancer in new ways
1. Autobahn collaboration to accelerate UCSF innovation from bench to bedside
2. Explore molecular targets in daring new ways
3. Bay Area Scientists Say Computers Can Develop Cancer Drugs 6 Times Faster
4. How a Public-Private Consortium Is Revolutionizing Cancer Drug Discovery
1. Gordon Hammes Lecture Award, American Chemical Society, Biological Division, 2024
2. Cope Scholar Award, American Chemical Society, Organic Division, 2024
3. Breakthrough Chemical Biology Research Award, ONO Pharma Foundation, 2018-2021
4. Finalist, SLAS Innovation Award, SLAS, 2013
5. Daymon Runyon – Walter Winchell Cancer Research Foundation Postdoctoral Fellowship, Daymon Runyon – Walter Winchell Cancer Research Foundation, 1997-1999
6. National Institutes of Health Traineeship, National Institutes of Health, 1995-1997
7. Predoctoral Fellowship, National Science Foundation, 1992-1995
8. Blodgett Fellowship, General Electric Foundation, 1991-1992
9. European Traveling Fellowship, Bryn Mawr College, 1990-1991
10. Armed Forces Communications and Electronics Association Scholarship, Armed Force, 1989
11. Dorothy Nepper Marshall Fellowship, Bryn Mawr College, 1989
12. Shippen Science Scholarship, Bryn Mawr College, 1989

Publications

Chou J, Robinson TM, Egusa EA, Lodha R, Zhang M, Badura M, Mikayelyan M, Delavan H, Swinderman J, Wilson C, Zhu J, Das R, Nguyen M, Loehr A, Golsorkhi T, Simmons A, Abida W, Chinnaiyan AM, Arkin MR, Small EJ, Quigley DA, Yang L, Kim M, Ashworth A, Feng FY. Synthetic Lethal Targeting of Cyclin Dependent Kinase-12-Deficient Prostate Cancer with PARP Inhibitors. Clin Cancer Res. 2024 Sep 25.
Theofilas P, Wang C, Butler D, Morales DO, Petersen C, Ambrose A, Chin B, Yang T, Khan S, Ng R, Kayed R, Karch CM, Miller BL, Gestwicki JE, Gan L, Temple S, Arkin MR, Grinberg LT. iPSC-induced neurons with the V337M MAPT mutation are selectively vulnerable to caspase-mediated cleavage of tau and apoptotic cell death. Mol Cell Neurosci. 2024 Sep; 130:103954.
Somsen BA, Cossar PJ, Arkin MR, Brunsveld L, Ottmann C. 14-3-3 Protein-Protein Interactions: From Mechanistic Understanding to Their Small-Molecule Stabilization. Chembiochem. 2024 Jul 15; 25(14):e202400214.
Vickery HR, Virta JM, Konstantinidou M, Arkin MR. Development of a NanoBRET assay for evaluation of 14-3-3σ molecular glues. SLAS Discov. 2024 Jul; 29(5):100165.
Silva DB, Trinidad M, Ljungdahl A, Revalde JL, Berguig GY, Wallace W, Patrick CS, Bomba L, Arkin M, Dong S, Estrada K, Hutchinson K, LeBowitz JH, Schlessinger A, Johannesen KM, Møller RS, Giacomini KM, Froelich S, Sanders SJ, Wuster A. Haploinsufficiency underlies the neurodevelopmental consequences of SLC6A1 variants. Am J Hum Genet. 2024 06 06; 111(6):1222-1238.
Konstantinidou M, Arkin MR. Molecular glues for protein-protein interactions: Progressing toward a new dream. Cell Chem Biol. 2024 Jun 20; 31(6):1064-1088.
D'Ippolito RA, Rabara D, Blanco MA, Alberico E, Drew MR, Ramakrishnan N, Sontan D, Widmeyer SRT, Scheidemantle GM, Messing S, Turner D, Arkin M, Maciag AE, Stephen AG, Esposito D, McCormick F, Nissley DV, DeHart CJ. A Top-Down Proteomic Assay to Evaluate KRAS4B-Compound Engagement. Anal Chem. 2024 04 02; 96(13):5223-5231.
Lee JY, Reyes NS, Ravishankar S, Zhou M, Krasilnikov M, Ringler C, Pohan G, Wilson C, Ang KK, Wolters PJ, Tsukui T, Sheppard D, Arkin MR, Peng T. An in vivo screening platform identifies senolytic compounds that target p16INK4a+ fibroblasts in lung fibrosis. J Clin Invest. 2024 Mar 07; 134(9).
Jiang Z, Kuo YH, Arkin MR. Synthetic autophagy receptor. Autophagy. 2024 Mar; 20(3):701-703.
Ortiz G, Longbotham JE, Qin SL, Zhang MY, Lee GM, Neitz RJ, Kelly MJS, Arkin MR, Fujimori DG. Identifying ligands for the PHD1 finger of KDM5A through high-throughput screening. RSC Chem Biol. 2024 Mar 06; 5(3):209-215.
Braxton JR, Altobelli CR, Tucker MR, Tse E, Thwin AC, Arkin MR, Southworth DR. The p97/VCP adaptor UBXD1 drives AAA+ remodeling and ring opening through multi-domain tethered interactions. Nat Struct Mol Biol. 2023 Dec; 30(12):2009-2019.
Jiang Z, Kuo YH, Arkin MR. Autophagy Receptor-Inspired Antibody-Fusion Proteins for Targeted Intracellular Degradation. J Am Chem Soc. 2023 11 08; 145(44):23939-23947.
Konstantinidou M, Visser EJ, Vandenboorn E, Chen S, Jaishankar P, Overmans M, Dutta S, Neitz RJ, Renslo AR, Ottmann C, Brunsveld L, Arkin MR. Structure-Based Optimization of Covalent, Small-Molecule Stabilizers of the 14-3-3σ/ERα Protein-Protein Interaction from Nonselective Fragments. J Am Chem Soc. 2023 09 20; 145(37):20328-20343.
Visser EJ, Jaishankar P, Sijbesma E, Pennings MAM, Vandenboorn EMF, Guillory X, Neitz RJ, Morrow J, Dutta S, Renslo AR, Brunsveld L, Arkin MR, Ottmann C. From Tethered to Freestanding Stabilizers of 14-3-3 Protein-Protein Interactions through Fragment Linking. Angew Chem Int Ed Engl. 2023 09 11; 62(37):e202308004.
Emira J. Visser, Priyadarshini Jaishankar, Eline Sijbesma, Marloes A.M. Pennings, Edmee M.F. Vandenboorn, Xavier Guillory, R. Jeffrey Neitz, John Morrow, Shubhankar Dutta, Adam R. Renslo, Luc Brunsveld, Michelle R. Arkin, Christian Ottmann. From tethered to freestanding stabilizers of 14-3-3 protein-protein interactions via fragment linking. Angewandte Chemie. 2023 Aug 1.
Togo T, Tram L, Denton LG, ElHilali-Pollard X, Gu J, Jiang J, Liu C, Zhao Y, Zhao Y, Zheng Y, Zheng Y, Yang J, Fan P, Arkin MR, Härmä H, Sun D, Canan SS, Wheeler SE, Renslo AR. Systematic Study of Heteroarene Stacking Using a Congeneric Set of Molecular Glues for Procaspase-6. J Med Chem. 2023 07 27; 66(14):9784-9796.
Braxton JR, Altobelli CR, Tucker MR, Tse E, Thwin AC, Arkin MR, Southworth DR. The p97/VCP adapter UBXD1 drives AAA+ remodeling and ring opening through multi-domain tethered interactions. bioRxiv. 2023 May 15.
Robert A. D'Ippolito, Caroline J. DeHart, Dana Rabara, Maria Abreu Blanco, Emily Alberico, Nitya Ramakrishnan, Stephanie Widmeyer, Simon Messing, David Turner, Michelle Arkin, Anna Maciag, Andrew Stephen, Dominic Esposito, Frank McCormick, Dwight V. Nissley. Abstract A018: A top-down proteomic assay to evaluate KRAS4B-compound engagement. Molecular Cancer Research. 2023 May 1; 21(5_Supplement):a018-a018.
Andlovic B, Heilmann G, Ninck S, Andrei SA, Centorrino F, Higuchi Y, Kato N, Brunsveld L, Arkin M, Menninger S, Choidas A, Wolf A, Klebl B, Kaschani F, Kaiser M, Eickhoff J, Ottmann C. IFNα primes cancer cells for Fusicoccin-induced cell death via 14-3-3 PPI stabilization. Cell Chem Biol. 2023 06 15; 30(6):573-590.e6.
Pariury H, Fandel J, Bachl S, Ang KK, Markossian S, Wilson CG, Braun BS, Popescu B, Wohlfeil M, Beckman K, Xirenayi S, Roy RP, Olshen AB, Smith C, Arkin MR, Loh ML, Diaz-Flores E. Venetoclax and dinaciclib elicit synergistic preclinical efficacy against hypodiploid acute lymphoblastic leukemia. Haematologica. 2023 05 01; 108(5):1272-1283.
Van Horn KS, Wang D, Medina-Cleghorn D, Lee PS, Bryant C, Altobelli C, Jaishankar P, Leung KK, Ng RA, Ambrose AJ, Tang Y, Arkin MR, Renslo AR. Engaging a Non-catalytic Cysteine Residue Drives Potent and Selective Inhibition of Caspase-6. J Am Chem Soc. 2023 05 10; 145(18):10015-10021.
Kenanova DN, Visser EJ, Virta JM, Sijbesma E, Centorrino F, Vickery HR, Zhong M, Neitz RJ, Brunsveld L, Ottmann C, Arkin MR. A Systematic Approach to the Discovery of Protein-Protein Interaction Stabilizers. ACS Cent Sci. 2023 May 24; 9(5):937-946.
Somsen BA, Schellekens RJC, Verhoef CJA, Arkin MR, Ottmann C, Cossar PJ, Brunsveld L. Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERRγ Protein-Protein Interaction as a Molecular Glue Drug Discovery Approach. J Am Chem Soc. 2023 03 29; 145(12):6741-6752.
Koleske ML, McInnes G, Brown JEH, Thomas N, Hutchinson K, Chin MY, Koehl A, Arkin MR, Schlessinger A, Gallagher RC, Song YS, Altman RB, Giacomini KM. Functional genomics of OCTN2 variants informs protein-specific variant effect predictor for Carnitine Transporter Deficiency. Proc Natl Acad Sci U S A. 2022 Nov 16; 119(46):e2210247119.
Tang Y, Kay A, Jiang Z, Arkin MR. LC3B Binds to the Autophagy Protease ATG4b with High Affinity Using a Bipartite Interface. Biochemistry. 2022 11 01; 61(21):2295-2302.
Leanne C. Sayles, Henry Martell, Amanda Koehne, Kean-Hooi Ang, Chris Wilson, Michelle Arkin, E. Alejandro Sweet-Cordero. Abstract B004: ATR-CHK1-WEE1 pathway is a critical dependency in the context of DNA damage and replicative stress in osteosarcoma. Clinical Cancer Research. 2022 Sep 15; 28(18_Supplement):b004-b004.
Julian Braxton, Chad Altobelli, Michelle Arkin, Daniel Southworth. Cryo-EM structures reveal dramatic remodeling of the p97 hexamer by the multi-domain adapter UBXD1. Acta Crystallographica Section A: Foundations and advances. 2022 Jul 29; 78(a1):a202-a202.
Jiang Z, Kuo YH, Zhong M, Zhang J, Zhou XX, Xing L, Wells JA, Wang Y, Arkin MR. Adaptor-Specific Antibody Fragment Inhibitors for the Intracellular Modulation of p97 (VCP) Protein-Protein Interactions. J Am Chem Soc. 2022 07 27; 144(29):13218-13225.
Theofilas P, Piergies AMH, Oh I, Lee YB, Li SH, Pereira FL, Petersen C, Ehrenberg AJ, Eser RA, Ambrose AJ, Chin B, Yang T, Khan S, Ng R, Spina S, Seeley WW, Miller BL, Arkin MR, Grinberg LT. Caspase-6-cleaved tau is relevant in Alzheimer's disease and marginal in four-repeat tauopathies: Diagnostic and therapeutic implications. Neuropathol Appl Neurobiol. 2022 08; 48(5):e12819.
Chin MY, Ang KH, Davies J, Alquezar C, Garda VG, Rooney B, Leng K, Kampmann M, Arkin MR, Kao AW. Phenotypic Screening Using High-Content Imaging to Identify Lysosomal pH Modulators in a Neuronal Cell Model. ACS Chem Neurosci. 2022 05 18; 13(10):1505-1516.
Hulce KR, Jaishankar P, Lee GM, Bohn MF, Connelly EJ, Wucherer K, Ongpipattanakul C, Volk RF, Chuo SW, Arkin MR, Renslo AR, Craik CS. Inhibiting a dynamic viral protease by targeting a non-catalytic cysteine. Cell Chem Biol. 2022 05 19; 29(5):785-798.e19.
Kim GJ, Mo H, Liu H, Okorie M, Chen S, Zheng J, Li H, Arkin M, Huang B, Guo S. In Vivo Dopamine Neuron Imaging-Based Small Molecule Screen Identifies Novel Neuroprotective Compounds and Targets. Front Pharmacol. 2022; 13:837756.
Antonia M. H. Piergies, Panos Theofilas, Song Li, Cathrine Petersen, Alexander J. Ehrenberg, Rana April Eser, Brian Chin, Teddy Yang, Shireen Khan, Raymond Ng, Salvatore Spina, William W. Seeley, Bruce L. Miller, Michelle R. Arkin, Lea T. Grinberg. Caspase-6-cleaved tau is relevant in Alzheimer's disease but not in 4-repeat tauopathies: Diagnostic and therapeutic implications. Alzheimer's & Dementia. 2022 Feb 1; 17.
Panos Theofilas, Andrew J. Ambrose, David Butler, Chao Wang, Dulce O. Morales, Cathrine Petersen, Brian Chin, Teddy Yang, Shireen Khan, Raymond Ng, Rakez Kayed, Celeste M. Karch, Bruce L. Miller, Jason E. Gestwicki, Li Gan, Sally Temple, Michelle R. Arkin, Lea T. Grinberg. Caspase inhibition mitigates tau cleavage and neurotoxicity in iPSC-induced neurons with the V337M MAPT mutation. Alzheimer's & Dementia. 2021 Dec 1; 17(S3).
Kim GJ, Mo H, Liu H, Wu Z, Chen S, Zheng J, Zhao X, Nucum D, Shortland J, Peng L, Elepano M, Tang B, Olson S, Paras N, Li H, Renslo AR, Arkin MR, Huang B, Lu B, Sirota M, Guo S. A zebrafish screen reveals Renin-angiotensin system inhibitors as neuroprotective via mitochondrial restoration in dopamine neurons. Elife. 2021 09 22; 10.
Chin MY, Patwardhan AR, Ang KH, Wang AL, Alquezar C, Welch M, Nguyen PT, Grabe M, Molofsky AV, Arkin MR, Kao AW. Genetically Encoded, pH-Sensitive mTFP1 Biosensor for Probing Lysosomal pH. ACS Sens. 2021 06 25; 6(6):2168-2180.
Sijbesma E, Hallenbeck KK, Andrei SA, Rust RR, Adriaans JMC, Brunsveld L, Arkin MR, Ottmann C. Exploration of a 14-3-3 PPI Pocket by Covalent Fragments as Stabilizers. ACS Med Chem Lett. 2021 Jun 10; 12(6):976-982.
Espinosa JA, Pohan G, Arkin MR, Markossian S. Real-Time Assessment of Mitochondrial Toxicity in HepG2 Cells Using the Seahorse Extracellular Flux Analyzer. Curr Protoc. 2021 Mar; 1(3):e75.
Chin MY, Espinosa JA, Pohan G, Markossian S, Arkin MR. Reimagining dots and dashes: Visualizing structure and function of organelles for high-content imaging analysis. Cell Chem Biol. 2021 03 18; 28(3):320-337.
Tyagi R, Bulman CA, Cho-Ngwa F, Fischer C, Marcellino C, Arkin MR, McKerrow JH, McNamara CW, Mahoney M, Tricoche N, Jawahar S, Janetka JW, Lustigman S, Sakanari J, Mitreva M. An Integrated Approach to Identify New Anti-Filarial Leads to Treat River Blindness, a Neglected Tropical Disease. Pathogens. 2021 Jan 14; 10(1).
Chen S, Suzuki BM, Dohrmann J, Singh R, Arkin MR, Caffrey CR. A multi-dimensional, time-lapse, high content screening platform applied to schistosomiasis drug discovery. Commun Biol. 2020 12 21; 3(1):747.
Antonia MH Piergies, Panos Theofilas, Cathrine Petersen, Alexander J Ehrenberg, Song Li, Dulce Ovando Morales, Rana A Eser, Teddy Yang, Shireen Khan, Brian Chin, Raymond Ng, Michelle Arkin, Lea Tenenholz Grinberg. Caspase-6-mediated tau cleavage and pathology in Alzheimer’s disease and other tauopathies. Alzheimer's & Dementia. 2020 Dec 7; 16(S3).
Pohan G, Espinosa JA, Chen S, Ang KK, Arkin MR, Markossian S. Multiparametric High-Content Assays to Measure Cell Health and Oxidative Damage as a Model for Drug-Induced Liver Injury. Curr Protoc Chem Biol. 2020 12; 12(4):e90.
Sijbesma E, Somsen BA, Miley GP, Leijten-van de Gevel IA, Brunsveld L, Arkin MR, Ottmann C. Fluorescence Anisotropy-Based Tethering for Discovery of Protein-Protein Interaction Stabilizers. ACS Chem Biol. 2020 12 18; 15(12):3143-3148.
Abdel Aziz MH, Fan Y, Liu L, Moasser MM, Fu H, Jura N, Arkin MR. Expression and purification of active human kinases using Pichia pastoris as a general-purpose host. Protein Expr Purif. 2021 03; 179:105780.
Mendiola AS, Ryu JK, Bardehle S, Meyer-Franke A, Ang KK, Wilson C, Baeten KM, Hanspers K, Merlini M, Thomas S, Petersen MA, Williams A, Thomas R, Rafalski VA, Meza-Acevedo R, Tognatta R, Yan Z, Pfaff SJ, Machado MR, Bedard C, Coronado PER, Jiang X, Wang J, Pleiss MA, Green AJ, Zamvil SS, Pico AR, Bruneau BG, Arkin MR, Akassoglou K. Author Correction: Transcriptional profiling and therapeutic targeting of oxidative stress in neuroinflammation. Nat Immunol. 2020 Sep; 21(9):1135.
Blay V, Tolani B, Ho SP, Arkin MR. High-Throughput Screening: today's biochemical and cell-based approaches. Drug Discov Today. 2020 10; 25(10):1807-1821.
Leandro J, Khamrui S, Wang H, Suebsuwong C, Nemeria NS, Huynh K, Moustakim M, Secor C, Wang M, Dodatko T, Stauffer B, Wilson CG, Yu C, Arkin MR, Jordan F, Sanchez R, DeVita RJ, Lazarus MB, Houten SM. Inhibition and Crystal Structure of the Human DHTKD1-Thiamin Diphosphate Complex. ACS Chem Biol. 2020 08 21; 15(8):2041-2047.
Guillory X, Wolter M, Leysen S, Neves JF, Kuusk A, Genet S, Somsen B, Morrow JK, Rivers E, van Beek L, Patel J, Goodnow R, Schoenherr H, Fuller N, Cao Q, Doveston RG, Brunsveld L, Arkin MR, Castaldi P, Boyd H, Landrieu I, Chen H, Ottmann C. Fragment-based Differential Targeting of PPI Stabilizer Interfaces. J Med Chem. 2020 07 09; 63(13):6694-6707.
Mendiola AS, Ryu JK, Bardehle S, Meyer-Franke A, Ang KK, Wilson C, Baeten KM, Hanspers K, Merlini M, Thomas S, Petersen MA, Williams A, Thomas R, Rafalski VA, Meza-Acevedo R, Tognatta R, Yan Z, Pfaff SJ, Machado MR, Bedard C, Rios Coronado PE, Jiang X, Wang J, Pleiss MA, Green AJ, Zamvil SS, Pico AR, Bruneau BG, Arkin MR, Akassoglou K. Transcriptional profiling and therapeutic targeting of oxidative stress in neuroinflammation. Nat Immunol. 2020 05; 21(5):513-524.
Zhang P, Zhai Y, Cregg J, Ang KK, Arkin M, Kenyon C. Stress Resistance Screen in a Human Primary Cell Line Identifies Small Molecules That Affect Aging Pathways and Extend Caenorhabditis elegans' Lifespan. G3 (Bethesda). 2020 02 06; 10(2):849-862.
Chen X, Li Y, Wang C, Tang Y, Mok SA, Tsai RM, Rojas JC, Karydas A, Miller BL, Boxer AL, Gestwicki JE, Arkin M, Cuervo AM, Gan L. Promoting tau secretion and propagation by hyperactive p300/CBP via autophagy-lysosomal pathway in tauopathy. Mol Neurodegener. 2020 01 06; 15(1):2.
Chris G.M. Wilson, Michelle R. Arkin. Chapter 5 Screening and biophysics in small molecule discovery. . 2020 Jan 1; 127-161.
Sanchez MI, de Vries LE, Lehmann C, Lee JT, Ang KK, Wilson C, Chen S, Arkin MR, Bogyo M, Deu E. Identification of Plasmodium dipeptidyl aminopeptidase allosteric inhibitors by high throughput screening. PLoS One. 2019; 14(12):e0226270.
Walhart T, Isaacson-Wechsler E, Ang KH, Arkin M, Tugizov S, Palefsky JM. A Cell-Based Renilla Luminescence Reporter Plasmid Assay for High-Throughput Screening to Identify Novel FDA-Approved Drug Inhibitors of HPV-16 Infection. SLAS Discov. 2020 01; 25(1):79-86.
Ravalin M, Theofilas P, Basu K, Opoku-Nsiah KA, Assimon VA, Medina-Cleghorn D, Chen YF, Bohn MF, Arkin M, Grinberg LT, Craik CS, Gestwicki JE. Specificity for latent C termini links the E3 ubiquitin ligase CHIP to caspases. Nat Chem Biol. 2019 08; 15(8):786-794.
Panos Theofilas, Mifrah Hayath, Chao Wang, David Butler, Salome McAllen, Michelle Arkin, Jason Gestwicki, Ana Maria Cuervo, Rakez Kayed, Celeste M. Karch, Sally Temple, Li Gan, Lea T. Grinberg. TAU-MEDIATED CELL DEATH MECHANISMS IN MAPT V337M IPSC-DERIVED HUMAN NEURONS. Alzheimer's & Dementia. 2019 Jul 1; 15(7):p1006.
Zhong M, Lee GM, Sijbesma E, Ottmann C, Arkin MR. Modulating protein-protein interaction networks in protein homeostasis. Curr Opin Chem Biol. 2019 06; 50:55-65.
Sijbesma E, Hallenbeck KK, Leysen S, de Vink PJ, Skóra L, Jahnke W, Brunsveld L, Arkin MR, Ottmann C. Site-Directed Fragment-Based Screening for the Discovery of Protein-Protein Interaction Stabilizers. J Am Chem Soc. 2019 02 27; 141(8):3524-3531.
Klein HL, Ang KKH, Arkin MR, Beckwitt EC, Chang YH, Fan J, Kwon Y, Morten MJ, Mukherjee S, Pambos OJ, El Sayyed H, Thrall ES, Vieira-da-Rocha JP, Wang Q, Wang S, Yeh HY, Biteen JS, Chi P, Heyer WD, Kapanidis AN, Loparo JJ, Strick TR, Sung P, Van Houten B, Niu H, Rothenberg E. Guidelines for DNA recombination and repair studies: Mechanistic assays of DNA repair processes. Microb Cell. 2019 Jan 07; 6(1):65-101.
Laurie MT, White CV, Retallack H, Wu W, Moser MS, Sakanari JA, Ang K, Wilson C, Arkin MR, DeRisi JL. Functional Assessment of 2,177 U.S. and International Drugs Identifies the Quinoline Nitroxoline as a Potent Amoebicidal Agent against the Pathogen Balamuthia mandrillaris. mBio. 2018 10 30; 9(5).
Ryu JK, Rafalski VA, Meyer-Franke A, Adams RA, Poda SB, Rios Coronado PE, Pedersen LØ, Menon V, Baeten KM, Sikorski SL, Bedard C, Hanspers K, Bardehle S, Mendiola AS, Davalos D, Machado MR, Chan JP, Plastira I, Petersen MA, Pfaff SJ, Ang KK, Hallenbeck KK, Syme C, Hakozaki H, Ellisman MH, Swanson RA, Zamvil SS, Arkin MR, Zorn SH, Pico AR, Mucke L, Freedman SB, Stavenhagen JB, Nelson RB, Akassoglou K. Fibrin-targeting immunotherapy protects against neuroinflammation and neurodegeneration. Nat Immunol. 2018 11; 19(11):1212-1223.
LaPorte MG, Burnett JC, Colombo R, Bulfer SL, Alverez C, Chou TF, Neitz RJ, Green N, Moore WJ, Yue Z, Li S, Arkin MR, Wipf P, Huryn DM. Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97. ACS Med Chem Lett. 2018 Nov 08; 9(11):1075-1081.
Lee J, Pappalardo Z, Chopra DG, Hennings TG, Vaughn I, Lan C, Choe JJ, Ang K, Chen S, Arkin M, McManus MT, German MS, Ku GM. A Genetic Interaction Map of Insulin Production Identifies Mfi as an Inhibitor of Mitochondrial Fission. Endocrinology. 2018 09 01; 159(9):3321-3330.
El-Sakkary N, Chen S, Arkin MR, Caffrey CR, Ribeiro P. Octopamine signaling in the metazoan pathogen Schistosoma mansoni: localization, small-molecule screening and opportunities for drug development. Dis Model Mech. 2018 07 30; 11(7).
Coussens NP, Sittampalam GS, Guha R, Brimacombe K, Grossman A, Chung TDY, Weidner JR, Riss T, Trask OJ, Auld D, Dahlin JL, Devanaryan V, Foley TL, McGee J, Kahl SD, Kales SC, Arkin M, Baell J, Bejcek B, Gal-Edd N, Glicksman M, Haas JV, Iversen PW, Hoeppner M, Lathrop S, Sayers E, Liu H, Trawick B, McVey J, Lemmon VP, Li Z, McManus O, Minor L, Napper A, Wildey MJ, Pacifici R, Chin WW, Xia M, Xu X, Lal-Nag M, Hall MD, Michael S, Inglese J, Simeonov A, Austin CP. Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery. Clin Transl Sci. 2018 09; 11(5):461-470.
Ingrid Wertz, Lorna Kategaya, Paola Di Lello, Lionel Rouge, Richard Pastor, Kevin R. Clark, Jason Drummond, Tracy Kleinheinz, Eva Lin, John-Paul Upton, Sumit Prakash, Johanna Heideker, Mark McCleland, Maria Stella Ritorto, Dario R. Alessi, Matthias Trost, Travis W. Bainbridge, Michael C. Kwok, Taylur P. Ma, Zachary Stiffler, Bradley Brasher, Yinyan Tang, Priya Jaishanker, Brian Hearn, Adam R. Renslo, Michelle R. Arkin, Frederick Cohen, Kebing Yu, Frank Peale, Florian Gnad, Matthew T. Chang, Christiaan Klijn, Elizabeth Blackwood, Scott E. Martin, William F. Forrest, James A. Ernst, Chudi Ndubaku, Xiaojing Wang, Maureen H. Beresini, Vickie Tsui, Carsten Schwerdtfeger, Robert A. Blake, Jeremy Murray, Till Maurer. Abstract SY23-03: Development and mechanistic characterization of USP7 deubiquitinase inhibitors. Cancer Research. 2018 Jul 1; 78(13_Supplement):sy23-03-sy23-03.
Markossian S, Ang KK, Wilson CG, Arkin MR. Small-Molecule Screening for Genetic Diseases. Annu Rev Genomics Hum Genet. 2018 08 31; 19:263-288.
Christin Schmidt, Steven Chen, Shirin IIkhanizadeh, Hanna Sabelstrom, Edith Yuan, Andy Ding, William Weiss, Mitchel S Berger, Michelle Arkin, Anders Persson. EXTH-55. REPURPOSING THERAPEUTICS IN PATIENT-DERIVED GLIOMAS AND AN IDH1 MUTANT GLIOMA MODEL. Neuro-Oncology. 2017 Nov 6; 19(suppl_6):vi84-vi85.
Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, Stiffler Z, Brasher B, Tang Y, Jaishankar P, Hearn BR, Renslo AR, Arkin MR, Cohen F, Yu K, Peale F, Gnad F, Chang MT, Klijn C, Blackwood E, Martin SE, Forrest WF, Ernst JA, Ndubaku C, Wang X, Beresini MH, Tsui V, Schwerdtfeger C, Blake RA, Murray J, Maurer T, Wertz IE. USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. 2017 10 26; 550(7677):534-538.
Hallenbeck KK, Davies JL, Merron C, Ogden P, Sijbesma E, Ottmann C, Renslo AR, Wilson C, Arkin MR. A Liquid Chromatography/Mass Spectrometry Method for Screening Disulfide Tethering Fragments. SLAS Discov. 2018 02; 23(2):183-192.
Kostic M, Arkin M. Chemical Biology as a Driver of Innovation in Cancer Research and Drug Discovery. Cell Chem Biol. 2017 09 21; 24(9):1057.
Theofilas P, Ehrenberg AJ, Nguy A, Thackrey JM, Dunlop S, Mejia MB, Alho AT, Paraizo Leite RE, Rodriguez RD, Suemoto CK, Nascimento CF, Chin M, Medina-Cleghorn D, Cuervo AM, Arkin M, Seeley WW, Miller BL, Nitrini R, Pasqualucci CA, Filho WJ, Rueb U, Neuhaus J, Heinsen H, Grinberg LT. Probing the correlation of neuronal loss, neurofibrillary tangles, and cell death markers across the Alzheimer's disease Braak stages: a quantitative study in humans. Neurobiol Aging. 2018 01; 61:1-12.
Stacie L. Bulfer, Michelle R. Arkin. Applying Biophysical and Biochemical Methods to the Discovery of Allosteric Modulators of the AAA ATPase p97. Applied Biophysics for Drug Discovery. 2017 Aug 10; 217-240.
Plowright AT, Ottmann C, Arkin M, Auberson YP, Timmerman H, Waldmann H. Joining Forces: The Chemical Biology-Medicinal Chemistry Continuum. Cell Chem Biol. 2017 Sep 21; 24(9):1058-1065.
Carlson HK, Mullan MR, Mosqueda LA, Chen S, Arkin MR, Coates JD. High-Throughput Screening To Identify Potent and Specific Inhibitors of Microbial Sulfate Reduction. Environ Sci Technol. 2017 Jun 20; 51(12):7278-7285.
Burnett JC, Lim C, Peyser BD, Samankumara LP, Kovaliov M, Colombo R, Bulfer SL, LaPorte MG, Hermone AR, McGrath CF, Arkin MR, Gussio R, Huryn DM, Wipf P. A threonine turnstile defines a dynamic amphiphilic binding motif in the AAA ATPase p97 allosteric binding site. Org Biomol Chem. 2017 May 16; 15(19):4096-4114.
Pappalardo Z, Gambhir Chopra D, Hennings TG, Richards H, Choe J, Yang K, Baeyens L, Ang K, Chen S, Arkin M, German MS, McManus MT, Ku GM. A Whole-Genome RNA Interference Screen Reveals a Role for Spry2 in Insulin Transcription and the Unfolded Protein Response. Diabetes. 2017 06; 66(6):1703-1712.
Hallenbeck KK, Turner DM, Renslo AR, Arkin MR. Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery. Curr Top Med Chem. 2017; 17(1):4-15.
Visperas PR, Wilson CG, Winger JA, Yan Q, Lin K, Arkin MR, Weiss A, Kuriyan J. Identification of Inhibitors of the Association of ZAP-70 with the T Cell Receptor by High-Throughput Screen. SLAS Discov. 2017 03; 22(3):324-331.
Liu H, Chen S, Huang K, Kim J, Mo H, Iovine R, Gendre J, Pascal P, Li Q, Sun Y, Dong Z, Arkin M, Guo S, Huang B. A High-Content Larval Zebrafish Brain Imaging Method for Small Molecule Drug Discovery. PLoS One. 2016; 11(10):e0164645.
Gallagher CM, Garri C, Cain EL, Ang KK, Wilson CG, Chen S, Hearn BR, Jaishankar P, Aranda-Diaz A, Arkin MR, Renslo AR, Walter P. Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branch. Elife. 2016 07 20; 5.
Bulfer SL, Chou TF, Arkin MR. p97 Disease Mutations Modulate Nucleotide-Induced Conformation to Alter Protein-Protein Interactions. ACS Chem Biol. 2016 08 19; 11(8):2112-6.
Conor Caffrey, Steven Chen, Brian Suzuki, Rahul Singh, Michelle Arkin. Challenges and solutions to developing an automated high-throughput/high-content screening platform for the ‘neglected’ schistosome parasite. The FASEB Journal. 2016 Apr 1; 30(S1).
Banerjee S, Bartesaghi A, Merk A, Rao P, Bulfer SL, Yan Y, Green N, Mroczkowski B, Neitz RJ, Wipf P, Falconieri V, Deshaies RJ, Milne JL, Huryn D, Arkin M, Subramaniam S. 2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition. Science. 2016 Feb 19; 351(6275):871-5.
Stacie L. Bulfer, Frantz L. Jean-Francois, Michelle R. Arkin. Making FBDD Work in Academia. Fragment-based Drug Discovery Lessons and Outlook. 2016 Jan 11; 223-246.
Arkin M. Interview with Michelle Arkin, PhD. Assay Drug Dev Technol. 2016 Jan-Feb; 14(1):14-8.
Alverez C, Bulfer SL, Chakrasali R, Chimenti MS, Deshaies RJ, Green N, Kelly M, LaPorte MG, Lewis TS, Liang M, Moore WJ, Neitz RJ, Peshkov VA, Walters MA, Zhang F, Arkin MR, Wipf P, Huryn DM. Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway. ACS Med Chem Lett. 2016 Feb 11; 7(2):182-7.
Suzawa M, Miranda DA, Ramos KA, Ang KK, Faivre EJ, Wilson CG, Caboni L, Arkin MR, Kim YS, Fletterick RJ, Diaz A, Schneekloth JS, Ingraham HA. A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver. Elife. 2015 Dec 11; 4.
Visscher M, Arkin MR, Dansen TB. Covalent targeting of acquired cysteines in cancer. Curr Opin Chem Biol. 2016 Feb; 30:61-67.
Alverez C, Arkin MR, Bulfer SL, Colombo R, Kovaliov M, LaPorte MG, Lim C, Liang M, Moore WJ, Neitz RJ, Yan Y, Yue Z, Huryn DM, Wipf P. Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97. ACS Med Chem Lett. 2015 Dec 10; 6(12):1225-30.
Frye SV, Arkin MR, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS. Tackling reproducibility in academic preclinical drug discovery. Nat Rev Drug Discov. 2015 11; 14(11):733-4.
Khare S, Roach SL, Barnes SW, Hoepfner D, Walker JR, Chatterjee AK, Neitz RJ, Arkin MR, McNamara CW, Ballard J, Lai Y, Fu Y, Molteni V, Yeh V, McKerrow JH, Glynne RJ, Supek F. Utilizing Chemical Genomics to Identify Cytochrome b as a Novel Drug Target for Chagas Disease. PLoS Pathog. 2015 Jul; 11(7):e1005058.
Ekins S, de Siqueira-Neto JL, McCall LI, Sarker M, Yadav M, Ponder EL, Kallel EA, Kellar D, Chen S, Arkin M, Bunin BA, McKerrow JH, Talcott C. Machine Learning Models and Pathway Genome Data Base for Trypanosoma cruzi Drug Discovery. PLoS Negl Trop Dis. 2015; 9(6):e0003878.
Neitz RJ, Bryant C, Chen S, Gut J, Hugo Caselli E, Ponce S, Chowdhury S, Xu H, Arkin MR, Ellman JA, Renslo AR. Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease. Bioorg Med Chem Lett. 2015 Nov 01; 25(21):4834-4837.
Zhang X, Gui L, Zhang X, Bulfer SL, Sanghez V, Wong DE, Lee Y, Lehmann L, Lee JS, Shih PY, Lin HJ, Iacovino M, Weihl CC, Arkin MR, Wang Y, Chou TF. Altered cofactor regulation with disease-associated p97/VCP mutations. Proc Natl Acad Sci U S A. 2015 Apr 07; 112(14):E1705-14.
Tran K, Arkin MR, Beal PA. Tethering in RNA: an RNA-binding fragment discovery tool. Molecules. 2015 Mar 04; 20(3):4148-61.
Bulman CA, Bidlow CM, Lustigman S, Cho-Ngwa F, Williams D, Rascón AA, Tricoche N, Samje M, Bell A, Suzuki B, Lim KC, Supakorndej N, Supakorndej P, Wolfe AR, Knudsen GM, Chen S, Wilson C, Ang KH, Arkin M, Gut J, Franklin C, Marcellino C, McKerrow JH, Debnath A, Sakanari JA. Repurposing auranofin as a lead candidate for treatment of lymphatic filariasis and onchocerciasis. PLoS Negl Trop Dis. 2015 Feb; 9(2):e0003534.
Chimenti MS, Bulfer SL, Neitz RJ, Renslo AR, Jacobson MP, James TL, Arkin MR, Kelly MJ. A Fragment-Based Ligand Screen Against Part of a Large Protein Machine: The ND1 Domains of the AAA+ ATPase p97/VCP. J Biomol Screen. 2015 Jul; 20(6):788-800.
Pfaff SJ, Chimenti MS, Kelly MJ, Arkin MR. Biophysical methods for identifying fragment-based inhibitors of protein-protein interactions. Methods Mol Biol. 2015; 1278:587-613.
Visperas PR, Winger JA, Horton TM, Shah NH, Aum DJ, Tao A, Barros T, Yan Q, Wilson CG, Arkin MR, Weiss A, Kuriyan J. Modification by covalent reaction or oxidation of cysteine residues in the tandem-SH2 domains of ZAP-70 and Syk can block phosphopeptide binding. Biochem J. 2015 Jan 01; 465(1):149-61.
Rettenmaier TJ, Sadowsky JD, Thomsen ND, Chen SC, Doak AK, Arkin MR, Wells JA. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30; 111(52):18590-5.
Neitz RJ, Chen S, Supek F, Yeh V, Kellar D, Gut J, Bryant C, Gallardo-Godoy A, Molteni V, Roach SL, Khare S, Stinson M, Chatterjee AK, Robertson S, Renslo AR, Arkin M, Glynne R, McKerrow J, Siqueira-Neto JL. Lead identification to clinical candidate selection: drugs for Chagas disease. J Biomol Screen. 2015 Jan; 20(1):101-11.
Arkin MR, Tang Y, Wells JA. Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. Chem Biol. 2014 Sep 18; 21(9):1102-14.
Dar RD, Hosmane NN, Arkin MR, Siliciano RF, Weinberger LS. Screening for noise in gene expression identifies drug synergies. Science. 2014 Jun 20; 344(6190):1392-6.
Chou TF, Bulfer SL, Weihl CC, Li K, Lis LG, Walters MA, Schoenen FJ, Lin HJ, Deshaies RJ, Arkin MR. Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D1 and D2 ATPase domains. J Mol Biol. 2014 Jul 29; 426(15):2886-99.
Arkin MR, Ang KK, Chen S, Davies J, Merron C, Tang Y, Wilson CG, Renslo AR. UCSF Small Molecule Discovery Center: innovation, collaboration and chemical biology in the Bay Area. Comb Chem High Throughput Screen. 2014 May; 17(4):333-42.
Flygare JA, Arkin MR. Inhibiting caspase-6 activation and catalytic activity for neurodegenerative diseases. Curr Top Med Chem. 2014; 14(3):319-25.
Jeremy Murray, Anthony M. Giannetti, Micah Steffek, Paul Gibbons, Brian R. Hearn, Frederick Cohen, Christine Tam, Christine Pozniak, Brandon Bravo, Joe Lewcock, Priyadarshini Jaishankar, Cuong Q. Ly, Xianrui Zhao, Yinyan Tang, Preeti Chugha, Michelle R. Arkin, John Flygare, Adam R. Renslo. Inside Cover: Tailoring Small Molecules for an Allosteric Site on Procaspase-6 (ChemMedChem 1/2014). ChemMedChem. 2014 Jan 1; 9(1):2-2.
Wilson CG, Arkin MR. Probing structural adaptivity at PPI interfaces with small molecules. Drug Discov Today Technol. 2013 Dec; 10(4):e501-8.
Murray J, Giannetti AM, Steffek M, Gibbons P, Hearn BR, Cohen F, Tam C, Pozniak C, Bravo B, Lewcock J, Jaishankar P, Ly CQ, Zhao X, Tang Y, Chugha P, Arkin MR, Flygare J, Renslo AR. Tailoring small molecules for an allosteric site on procaspase-6. ChemMedChem. 2014 Jan; 9(1):73-7, 2.
Slusher BS, Conn PJ, Frye S, Glicksman M, Arkin M. Bringing together the academic drug discovery community. Nat Rev Drug Discov. 2013 Nov; 12(11):811-2.
Sun Y, Dong Z, Jin T, Ang KH, Huang M, Haston KM, Peng J, Zhong TP, Finkbeiner S, Weiss WA, Arkin MR, Jan LY, Guo S. Imaging-based chemical screening reveals activity-dependent neural differentiation of pluripotent stem cells. Elife. 2013 Sep 10; 2:e00508.
Bagriantsev SN, Ang KH, Gallardo-Godoy A, Clark KA, Arkin MR, Renslo AR, Minor DL. A high-throughput functional screen identifies small molecule regulators of temperature- and mechano-sensitive K2P channels. ACS Chem Biol. 2013 Aug 16; 8(8):1841-51.
Sidrauski C, Acosta-Alvear D, Khoutorsky A, Vedantham P, Hearn BR, Li H, Gamache K, Gallagher CM, Ang KK, Wilson C, Okreglak V, Ashkenazi A, Hann B, Nader K, Arkin MR, Renslo AR, Sonenberg N, Walter P. Pharmacological brake-release of mRNA translation enhances cognitive memory. Elife. 2013 May 28; 2:e00498.
Wan Xing Hong, Jon Akutagawa, Steven Chen, Michelle Arkin, Benjamin S. Braun. Abstract 5524: Library screen to rapidly determine activity against normal and mutant bone marrow progenitor cells. Cancer Research. 2013 Apr 15; 73(8_Supplement):5524-5524.
Choy JW, Bryant C, Calvet CM, Doyle PS, Gunatilleke SS, Leung SS, Ang KK, Chen S, Gut J, Oses-Prieto JA, Johnston JB, Arkin MR, Burlingame AL, Taunton J, Jacobson MP, McKerrow JM, Podust LM, Renslo AR. Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target. Beilstein J Org Chem. 2013; 9:15-25.
Richard J. Evans, Ivano Bertini, Giacomo Parigi, Noel Wyn Davies, Victor J. Morris, Marc Willem van der Kamp, Kuniaki Nagayama, Rumiana Koynova, Boris Tenchov, Marc Willem van der Kamp, Abhinav Nath, Elizabeth Rhoades, Marc Willem van der Kamp, Julie S. Biteen, Ranieri Bizzarri, Kuo-Hsiang Tang, Robert E. Blankenship, Ingo Grotjohann, Petra Fromme, Iain L. McConnell, Gary W. Brudvig, Xiaojing Yang, Jacqueline M. Matthews, Derek Marsh, Alison Rodger, Benyamin Rahmani, Hossein Ghanbari, Spyridon Tzamtzis, Gaetano Burriesci, Alexander M. Seifalian, Matt J. Kipper, Stephen E. Harding, Terry Jones, Vivien Jane Coulson-Thomas, Tarsis F. Gesteira, Yvette May Coulson-Thomas, Helena B. Nader, Eija Lehtomaki, Joel P. Mackay, Simon Bernèche, Shi-Bing Yang, Lily Y. Jan, Sami Yunus, Alain M. Jonas, Boris Lakard, Roland Winter, Roland Winter, Assaf Friedler, Chen Katz, Lee Whitmore, Robert W. Janes, Jonathan Hirst, Jacqueline M. Matthews, Alison Rodger, Mikael Akke, Patrik Lundström, Gianfranco Gilardi, Andrew L. Lee, Jamie L. Kear, Gail E. Fanucci, Marc Willem van der Kamp, David R. Skoff, Martin T. Zanni, Robert H. Callender, R. Brian Dyer, Vijay Pande, Clare-Louise Towse, Valerie Daggett, Marc Willem van der Kamp, Gordon C. K. Roberts, Fuyuhiko Inagaki, Jonathan J. Ellis, Boštjan Kobe, Edda Kloppmann, Peter Hoenigschmid, Burkhard Rost, Ertan Eryilmaz, Dongsheng Liu, David Cowburn, Jon I. Mujika, Xabier Lopez, Anna Tramontano, Michael I. Sadowski, Daniel Barry Roche, Maria Teresa Buenavista, Liam James McGuffin, Michael I. Sadowski, Marina V. Rodnina, Jeffrey W. Peng, Marc R. Wilkins, Kleitos Sokratous, José P. Afonso, Preeti Chugha, Michelle Arkin, Gideon Schreiber, Arthur M. Lesk, Barbara Mulloy, Jeffrey J. Warren, James M. Mayer, Inés García-Rubio, Inés García-Rubio, Kandala V. R. Chary, Atul K. Srivastava, Chad Schwartz, Hui Zhang, Peixuan Guo, Russ Hille. P2X Receptors for ATP: Molecular Properties and Functional Roles. . 2013 Jan 1; 1819-1824.
Preeti Chugha, Michelle Arkin. Protein–Protein Interactions – Inhibition. Encyclopedia of Biophysics. 2013 Jan 1; 2093-2098.
Heise CE, Murray J, Augustyn KE, Bravo B, Chugha P, Cohen F, Giannetti AM, Gibbons P, Hannoush RN, Hearn BR, Jaishankar P, Ly CQ, Shah K, Stanger K, Steffek M, Tang Y, Zhao X, Lewcock JW, Renslo AR, Flygare J, Arkin MR. Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6. PLoS One. 2012; 7(12):e50864.
Wan Xing Hong, Steven Chen, Jon Akutagawa, Michelle Arkin, Benjamin S. Braun. An In Vitro Library Screen to Rapidly Determine Activity Against Normal and Mutant Bone Marrow Progenitor Cells. Blood. 2012 Nov 16; 120(21):4916-4916.
Wu VM, Chen SC, Arkin MR, Reiter JF. Small molecule inhibitors of Smoothened ciliary localization and ciliogenesis. Proc Natl Acad Sci U S A. 2012 Aug 21; 109(34):13644-9.
Gunatilleke SS, Calvet CM, Johnston JB, Chen CK, Erenburg G, Gut J, Engel JC, Ang KK, Mulvaney J, Chen S, Arkin MR, McKerrow JH, Podust LM. Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51. PLoS Negl Trop Dis. 2012; 6(7):e1736.
Pu M, Hayashi T, Cottam H, Mulvaney J, Arkin M, Corr M, Carson D, Messer K. Analysis of high-throughput screening assays using cluster enrichment. Stat Med. 2012 Dec 30; 31(30):4175-89.
Rogers KE, Keränen H, Durrant JD, Ratnam J, Doak A, Arkin MR, McCammon JA. Novel cruzain inhibitors for the treatment of Chagas' disease. Chem Biol Drug Des. 2012 Sep; 80(3):398-405.
Debnath A, Parsonage D, Andrade RM, He C, Cobo ER, Hirata K, Chen S, García-Rivera G, Orozco E, Martínez MB, Gunatilleke SS, Barrios AM, Arkin MR, Poole LB, McKerrow JH, Reed SL. A high-throughput drug screen for Entamoeba histolytica identifies a new lead and target. Nat Med. 2012 Jun; 18(6):956-60.
Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J, Arkin MR, Evanchik MJ, Flanagan WM, Hoch U, Hyde J, Prabhu S, Silverman JA, Wright J. Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye. ACS Med Chem Lett. 2012 Mar 08; 3(3):203-6.
Lee H, Moody-Davis A, Saha U, Suzuki BM, Asarnow D, Chen S, Arkin M, Caffrey CR, Singh R. Quantification and clustering of phenotypic screening data using time-series analysis for chemotherapy of schistosomiasis. BMC Genomics. 2012; 13 Suppl 1:S4.
Tang Y, Wells JA, Arkin MR. Structural and enzymatic insights into caspase-2 protein substrate recognition and catalysis. J Biol Chem. 2011 Sep 30; 286(39):34147-54.
De Muylder G, Ang KK, Chen S, Arkin MR, Engel JC, McKerrow JH. A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit. PLoS Negl Trop Dis. 2011 Jul; 5(7):e1253.
Ang KK, Ratnam J, Gut J, Legac J, Hansell E, Mackey ZB, Skrzypczynska KM, Debnath A, Engel JC, Rosenthal PJ, McKerrow JH, Arkin MR, Renslo AR. Mining a cathepsin inhibitor library for new antiparasitic drug leads. PLoS Negl Trop Dis. 2011 May 03; 5(5):e1023.
Michelle R. Arkin, Steven Chen, Brian Suzuki, Vlad Popescu, Adam Renslo, Jim A Wells, Rahul Singh, Conor R. Caffrey. Screening technologies for unusual and challenging targets. The FASEB Journal. 2011 Apr 1; 25:314.1-314.1.
Ben Khalaf N, De Muylder G, Ratnam J, Kean-Hooi Ang K, Arkin M, McKerrow J, Chenik M. A high-throughput turbidometric assay for screening inhibitors of Leishmania major protein disulfide isomerase. J Biomol Screen. 2011 Jun; 16(5):545-51.
Gut J, Ang KK, Legac J, Arkin MR, Rosenthal PJ, McKerrow JH. An image-based assay for high throughput screening of Giardia lamblia. J Microbiol Methods. 2011 Mar; 84(3):398-405.
Wilson CG, Arkin MR. Small-molecule inhibitors of IL-2/IL-2R: lessons learned and applied. Curr Top Microbiol Immunol. 2011; 348:25-59.
Zhong M, Hanan EJ, Shen W, Bui M, Arkin MR, Barr KJ, Evanchik MJ, Hoch U, Hyde J, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM. Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists. Bioorg Med Chem Lett. 2011 Jan 01; 21(1):307-10.
Zhong M, Shen W, Barr KJ, Arbitrario JP, Arkin MR, Bui M, Chen T, Cunningham BC, Evanchik MJ, Hanan EJ, Hoch U, Huen K, Hyde J, Kumer JL, Lac T, Lawrence CE, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM. Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists. Bioorg Med Chem Lett. 2010 Sep 01; 20(17):5269-73.
Engel JC, Ang KK, Chen S, Arkin MR, McKerrow JH, Doyle PS. Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. Antimicrob Agents Chemother. 2010 Aug; 54(8):3326-34.
Hawtin RE, Stockett DE, Byl JA, McDowell RS, Nguyen T, Arkin MR, Conroy A, Yang W, Osheroff N, Fox JA. Voreloxin is an anticancer quinolone derivative that intercalates DNA and poisons topoisomerase II. PLoS One. 2010 Apr 15; 5(4):e10186.
Mott BT, Ferreira RS, Simeonov A, Jadhav A, Ang KK, Leister W, Shen M, Silveira JT, Doyle PS, Arkin MR, McKerrow JH, Inglese J, Austin CP, Thomas CJ, Shoichet BK, Maloney DJ. Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. J Med Chem. 2010 Jan 14; 53(1):52-60.
Michelle Arkin. Finding Small Molecule Ligands for Protein-Protein Interactions and Other “Undruggable” Targets. Biophysical Journal. 2010 Jan 1; 98(3):411a.
Bryant C, Kerr ID, Debnath M, Ang KK, Ratnam J, Ferreira RS, Jaishankar P, Zhao D, Arkin MR, McKerrow JH, Brinen LS, Renslo AR. Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases. Bioorg Med Chem Lett. 2009 Nov 01; 19(21):6218-21.
McKerrow JH, Doyle PS, Engel JC, Podust LM, Robertson SA, Ferreira R, Saxton T, Arkin M, Kerr ID, Brinen LS, Craik CS. Two approaches to discovering and developing new drugs for Chagas disease. Mem Inst Oswaldo Cruz. 2009 Jul; 104 Suppl 1:263-9.
Arkin MR, Whitty A. The road less traveled: modulating signal transduction enzymes by inhibiting their protein-protein interactions. Curr Opin Chem Biol. 2009 Jun; 13(3):284-90.
Rubio BK, Tenney K, Ang KH, Abdulla M, Arkin M, McKerrow JH, Crews P. The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness. J Nat Prod. 2009 Feb 27; 72(2):218-22.
Conroy A, Stockett DE, Walker D, Arkin MR, Hoch U, Fox JA, Hawtin RE. SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009 Sep; 64(4):723-32.
Arkin M, Moasser MM. HER-2-directed, small-molecule antagonists. Curr Opin Investig Drugs. 2008 Dec; 9(12):1264-76.
Choong IC, Serafimova I, Fan J, Stockett D, Chan E, Cheeti S, Lu Y, Fahr B, Pham P, Arkin MR, Walker DH, Hoch U. A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties. Bioorg Med Chem Lett. 2008 Nov 01; 18(21):5763-5.
Nathan D. Waal, Wenjin Yang, Johan D. Oslob, Michelle R. Arkin, Jennifer Hyde, Wanli Lu, Robert S. McDowell, Chul H. Yu, Brian C. Raimundo. Identification of Nonpeptidic Small-Molecule Inhibitors of Interleukin-2. ChemInform. 2005 Jul 5; 36(27).
Arkin M. Protein-protein interactions and cancer: small molecules going in for the kill. Curr Opin Chem Biol. 2005 Jun; 9(3):317-24.
Waal ND, Yang W, Oslob JD, Arkin MR, Hyde J, Lu W, McDowell RS, Yu CH, Raimundo BC. Identification of nonpeptidic small-molecule inhibitors of interleukin-2. Bioorg Med Chem Lett. 2005 Feb 15; 15(4):983-7.
Raimundo BC, Oslob JD, Braisted AC, Hyde J, McDowell RS, Randal M, Waal ND, Wilkinson J, Yu CH, Arkin MR. Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein interactions. J Med Chem. 2004 Jun 03; 47(12):3111-30.
Arkin MR, Wells JA. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Discov. 2004 Apr; 3(4):301-17.
Hyde J, Braisted AC, Randal M, Arkin MR. Discovery and characterization of cooperative ligand binding in the adaptive region of interleukin-2. Biochemistry. 2003 Jun 03; 42(21):6475-83.
Braisted AC, Oslob JD, Delano WL, Hyde J, McDowell RS, Waal N, Yu C, Arkin MR, Raimundo BC. Discovery of a potent small molecule IL-2 inhibitor through fragment assembly. J Am Chem Soc. 2003 Apr 02; 125(13):3714-5.
Arkin MR, Randal M, DeLano WL, Hyde J, Luong TN, Oslob JD, Raphael DR, Taylor L, Wang J, McDowell RS, Wells JA, Braisted AC. Binding of small molecules to an adaptive protein-protein interface. Proc Natl Acad Sci U S A. 2003 Feb 18; 100(4):1603-8.
Wells J, Arkin M, Braisted A, DeLano W, McDowell B, Oslob J, Raimundo B, Randal M. Drug discovery at signaling interfaces. Ernst Schering Res Found Workshop. 2003; (42):19-27.
Michelle Arkin, J.D. Lear. A New Data Analysis Method to Determine Binding Constants of Small Molecules to Proteins Using Equilibrium Analytical Ultracentrifugation with Absorption Optics Volume 299, Number 1 (2001), pages 98–107. Analytical Biochemistry. 2002 May 1; 304(2):275.
Arkin M, Lear JD. A new data analysis method to determine binding constants of small molecules to proteins using equilibrium analytical ultracentrifugation with absorption optics. Anal Biochem. 2001 Dec 01; 299(1):98-107.
M. Arkin. In Vitro Mutagenesis. Brenner\u0027s Encyclopedia of Genetics. 2001 Jan 1; (Proceedings of the National Academy of Sciences of the United States of America901993):46-50.
M. Arkin. In vitro Mutagenesis. Encyclopedia of Genetics. 2001 Jan 1; (Proceedings of the National Academy of Sciences, USA901993):1010-1014.
M. Arkin. Mutational Analysis. Encyclopedia of Genetics. 2001 Jan 1; (Biochemistry351996):1279-1284.
Arkin MR, Wells JA. Probing the importance of second sphere residues in an esterolytic antibody by phage display. J Mol Biol. 1998 Dec 11; 284(4):1083-94.
E. J. C. Olson, D. Hu, A. Hörmann, A. M. Jonkman, M. R. Arkin, E. D. A. Stemp, J. K. Barton, P. F. Barbara. First Observation of the Key Intermediate in the “Light-Switch” Mechanism of [Ru(phen) 2 dppz] 2+. Journal of the American Chemical Society. 1997 Nov 1; 119(47):11458-11467.
Arkin MR, Stemp ED, Pulver SC, Barton JK. Long-range oxidation of guanine by Ru(III) in duplex DNA. Chem Biol. 1997 May; 4(5):389-400.
E. D. A. Stemp, M. R. Arkin, J. K. Barton. Oxidation of Guanine in DNA by Ru(phen) 2 (dppz) 3+ Using the Flash-Quench Technique. Journal of the American Chemical Society. 1997 Mar 1; 119(12):2921-2925.
Arkin MR, Stemp ED, Holmlin RE, Barton JK, Hörmann A, Olson EJ, Barbara PF. Rates of DNA-mediated electron transfer between metallointercalators. Science. 1996 Jul 26; 273(5274):475-80.
Michelle R. Arkin, Yonchu Jenkins, Catherine J. Murphy, Nicholas J. Turro, Jacqueline K. Barton. Metallointercalators as Probes of the DNA p-way. . 1996 May 5; 246:449-469.
M. R. Arkin, E. D. A. Stemp, C. Turro, N. J. Turro, J. K. Barton. Luminescence Quenching in Supramolecular Systems: A Comparison of DNA- and SDS Micelle-Mediated Photoinduced Electron Transfer between Metal Complexes. Journal of the American Chemical Society. 1996 Jan 1; 118(9):2267-2274.
A. Hörmann, E. J. C. Olson, P. F. Barbara, M. R. Arkin, E. D. A. Stemp, R. E. Holmlin, J. K. Barton. Time Resolved Electron Transfer Studies Between Metallointercalators in DNA. . 1996 Jan 1; 62:359-360.
Jacqueline K. Barton, Michelle R. Arkin, Eric D.A. Stemp, R.Erik Holmlin, Yonchu Jenkins. DNA-mediated electron transfer. Journal of Inorganic Biochemistry. 1995 Aug 1; 59(2-3):132.
Michelle R. Arkin, Eric D.A. Stemp, R.Erik Holmin, Aldo Hoermann, Eric Olson, Paul F. Barbara, Jacqueline K. Barton. Rates of electron transfer reactions between metallointercalators. Journal of Inorganic Biochemistry. 1995 Aug 1; 59(2-3):266.
Sharon J. Nieter Burgmayer, Michelle R. Arkin, Laura Bostick, Sara Dempster, Kristin M. Everett, Heather L. Layton, Kateri E. Paul, Cory Rogge, Arnold L. Rheingold. Tetrahydropterin Reactions of Dioxo-Molybdenum(6+) Complexes: Does Redox Occur?. Journal of the American Chemical Society. 1995 May 1; 117(21):5812-5823.
Eric D. A. Stemp, Michelle R. Arkin, Jacqueline K. Barton. Electron transfer between metallointercalators bound to DNA: Spectral identification of the transient intermediate. Journal of the American Chemical Society. 1995 Mar 1; 117(8):2375-2376.
Murphy CJ, Arkin MR, Ghatlia ND, Bossmann S, Turro NJ, Barton JK. Fast photoinduced electron transfer through DNA intercalation. Proc Natl Acad Sci U S A. 1994 Jun 07; 91(12):5315-9.
Murphy CJ, Arkin MR, Jenkins Y, Ghatlia ND, Bossmann SH, Turro NJ, Barton JK. Long-range photoinduced electron transfer through a DNA helix. Science. 1993 Nov 12; 262(5136):1025-9.
M. Arkin, C.J. Murphy, Y.C. Jenkins, N.J. Turro, J.K. Barton. Evidence for photoelectron transfer through DNA intercalation. Journal of Inorganic Biochemistry. 1993 Jul 1; 51(1-2):526.
S.J.N. Burgmayer, K. Everett, M. Arkin, K. Mosny. Redox reactions of reduced pterins with copper and molybdenum complexes. Journal of Inorganic Biochemistry. 1991 Aug 1; 43(2-3):581.