Adam Renslo, PhD

Professor
Department of Pharmaceutical Chemistry
[email protected]
Phone: +1 415 514-9698
600 16th Street, Rm N572B
UCSF Box 2280
San Francisco, CA 94158
United States

Links

Renslo Lab UCSF Profiles

Affiliations

Education programs

PharmD Degree Program
Chemistry and Chemical Biology Graduate Program (CCB)

UCSF centers, institutes, and research programs

Codirector, Small Molecule Discovery Center (SMDC)
Quantitative Biosciences Institute (QBI)

What I do

I am the School’s representative in collaborations between our academic scientists and industry, aiming to translate the most promising discoveries and technologies from our research into therapies that reach patients.

My research group is engaged at the interface of chemistry and biology. As medicinal chemists, we design and synthesize small molecules that modulate disease pathology at the level of the enzyme, cell, and whole animal, with current projects in cancer, infectious disease, and neurodegeneration. As chemical biologists, we employ novel small molecule probes to better understand biological pathways and the mechanisms of small molecule therapeutics.

Departmental research area

chemical biology and medicinal chemistry

My research expertise

targeted drug-delivery, understanding and improving the cell permeability of peptide therapeutics, fragment-based drug discovery, identifying and characterizing the targets of novel small molecules

Professional background

Degrees

PhD, Organic Chemistry, Massachusetts Institute of Technology (MIT), 1998
BA, Chemistry, St. Olaf College, 1993

Biography

My research group is engaged at the interface of chemistry and biology. As medicinal chemists, we design and synthesize small molecules that modulate disease pathology at the level of the enzyme, cell, and whole animal, with active projects in cancer, infectious disease, and neurodegeneration. Our group also developed a parallel synthetic methodology to produce a library of disulfide 'fragments', thereby enabling cysteine-disulfide (Tethering) screening at UCSF. Finally, we design, synthesize and validate novel small molecule probes for the study of labile ferrous iron in biology and disease. Most recently, we described the first of a new class of activity-based probes for proximity labelling of proteins in an iron-dependent fashion, thus enabling the first chemoproteomic studies of the labile iron 'interactome'.

Research keywords

  • Antimalarials
  • caspases
  • Caspase 6
  • Iron
  • Anti-Bacterial Agents
  • Heterocyclic Compounds, 1-Ring
  • Spiro Compounds
  • Oxazolidinones
  • Prion Diseases
  • Trypanocidal Agents
  • Protease Inhibitors
  • Peroxides
  • Ferrous Compounds
  • Structure-Activity Relationship
  • Preclinical Drug Evaluation

Publications

Flowers J, Echols N, Correy G, Jaishankar P, Togo T, Renslo AR, van den Bedem H, Fraser JS, Wankowicz SA. Expanding Automated Multiconformer Ligand Modeling to Macrocycles and Fragments. bioRxiv. 2024 Sep 23.
Klope MT, Tapia Cardona JA, Chen J, Gonciarz RL, Cheng K, Jaishankar P, Kim J, Legac J, Rosenthal PJ, Renslo AR. Synthesis and In Vivo Profiling of Desymmetrized Antimalarial Trioxolanes with Diverse Carbamate Side Chains. ACS Med Chem Lett. 2024 Oct 10; 15(10):1764-1770.
Suryawanshi RK, Jaishankar P, Correy GJ, Rachman MM, O'Leary PC, Taha TY, Zapatero-Belinchón FJ, McCavittMalvido M, Doruk YU, Stevens MGV, Diolaiti ME, Jogalekar MP, Richards AL, Montano M, Rosecrans J, Matthay M, Togo T, Gonciarz RL, Gopalkrishnan S, Neitz RJ, Krogan NJ, Swaney DL, Shoichet BK, Ott M, Renslo AR, Ashworth A, Fraser JS. The Mac1 ADP-ribosylhydrolase is a Therapeutic Target for SARS-CoV-2. bioRxiv. 2024 Aug 29.
Correy GJ, Rachman M, Togo T, Gahbauer S, Doruk YU, Stevens M, Jaishankar P, Kelley B, Goldman B, Schmidt M, Kramer T, Ashworth A, Riley P, Shoichet BK, Renslo AR, Walters WP, Fraser JS. Extensive exploration of structure activity relationships for the SARS-CoV-2 macrodomain from shape-based fragment merging and active learning. bioRxiv. 2024 Aug 26.
Deal PE, Lee H, Mondal A, Lolicato M, Mendonça PRF, Black H, Jang S, El-Hilali X, Bryant C, Isacoff EY, Renslo AR, Minor DL. Development of covalent chemogenetic K2P channel activators. Cell Chem Biol. 2024 Jul 18; 31(7):1305-1323.e9.
Pezacki AT, Gonciarz RL, Okamura T, Matier CD, Torrente L, Cheng K, Miller SG, Ralle M, Ward NP, DeNicola GM, Renslo AR, Chang CJ. A tandem activity-based sensing and labeling strategy reveals antioxidant response element regulation of labile iron pools. Proc Natl Acad Sci U S A. 2024 Jul 09; 121(28):e2401579121.
Deal PE, Lee H, Mondal A, Lolicato M, de Mendonca PRF, Black H, El-Hilali X, Bryant C, Isacoff EY, Renslo AR, Minor DL. Development of covalent chemogenetic K2P channel activators. bioRxiv. 2023 Oct 18.
Gonciarz RL, Jiang H, Tram L, Hugelshofer CL, Ekpenyong O, Knemeyer I, Aron AT, Chang CJ, Flygare JA, Collisson EA, Renslo AR. In vivo bioluminescence imaging of labile iron in xenograft models and liver using FeAL-1, an iron-activatable form of D-luciferin. Cell Chem Biol. 2023 11 16; 30(11):1468-1477.e6.
Foss CA, Renslo AR. Imaging-Selected Host Responses in the Context of Infections. J Infect Dis. 2023 10 03; 228(Suppl 4):S302-S310.
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.
Fink EA, Bardine C, Gahbauer S, Singh I, Detomasi TC, White K, Gu S, Wan X, Chen J, Ary B, Glenn I, O'Connell J, O'Donnell H, Fajtová P, Lyu J, Vigneron S, Young NJ, Kondratov IS, Alisoltani A, Simons LM, Lorenzo-Redondo R, Ozer EA, Hultquist JF, O'Donoghue AJ, Moroz YS, Taunton J, Renslo AR, Irwin JJ, García-Sastre A, Shoichet BK, Craik CS. Large library docking for novel SARS-CoV-2 main protease non-covalent and covalent inhibitors. Protein Sci. 2023 08; 32(8):e4712.
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.
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.
Blank BR, Gut J, Rosenthal PJ, Renslo AR. Artefenomel Regioisomer RLA-3107 Is a Promising Lead for the Discovery of Next-Generation Endoperoxide Antimalarials. ACS Med Chem Lett. 2023 Apr 13; 14(4):493-498.
Admasu TD, Kim K, Rae M, Avelar R, Gonciarz RL, Rebbaa A, Pedro de Magalhães J, Renslo AR, Stolzing A, Sharma A. Selective ablation of primary and paracrine senescent cells by targeting iron dyshomeostasis. Cell Rep. 2023 02 28; 42(2):112058.
Gonciarz RL, Sakhamuri S, Hooshdaran N, Kumar G, Kim H, Evans MJ, Renslo AR. Elevated labile iron in castration-resistant prostate cancer is targetable with ferrous iron-activatable antiandrogen therapy. Eur J Med Chem. 2023 Mar 05; 249:115110.
Gahbauer S, Correy GJ, Schuller M, Ferla MP, Doruk YU, Rachman M, Wu T, Diolaiti M, Wang S, Neitz RJ, Fearon D, Radchenko DS, Moroz YS, Irwin JJ, Renslo AR, Taylor JC, Gestwicki JE, von Delft F, Ashworth A, Ahel I, Shoichet BK, Fraser JS. Iterative computational design and crystallographic screening identifies potent inhibitors targeting the Nsp3 macrodomain of SARS-CoV-2. Proc Natl Acad Sci U S A. 2023 01 10; 120(2):e2212931120.
Gahbauer S, Correy GJ, Schuller M, Ferla MP, Doruk YU, Rachman M, Wu T, Diolaiti M, Wang S, Neitz RJ, Fearon D, Radchenko D, Moroz Y, Irwin JJ, Renslo AR, Taylor JC, Gestwicki JE, von Delft F, Ashworth A, Ahel I, Shoichet BK, Fraser JS. Iterative computational design and crystallographic screening identifies potent inhibitors targeting the Nsp3 Macrodomain of SARS-CoV-2. bioRxiv. 2022 Jul 28.
Shimizu H, Renslo AR. Systematic Exploration of Passive Permeability in Tetrapeptides with Hydrogen-Bond-Accepting Amino Acid Side Chains. ChemMedChem. 2022 08 17; 17(16):e202200204.
Sacco MD, Defrees K, Zhang X, Lawless W, Nwanochie E, Balsizer A, Darch SE, Renslo AR, Chen Y. Structure-Based Ligand Design Targeting Pseudomonas aeruginosa LpxA in Lipid A Biosynthesis. ACS Infect Dis. 2022 07 08; 8(7):1231-1240.
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.
Jiang H, Muir RK, Gonciarz RL, Olshen AB, Yeh I, Hann BC, Zhao N, Wang YH, Behr SC, Korkola JE, Evans MJ, Collisson EA, Renslo AR. Ferrous iron-activatable drug conjugate achieves potent MAPK blockade in KRAS-driven tumors. J Exp Med. 2022 04 04; 219(4).
Gunderson EL, Bryant C, Bulman CA, Fischer C, Luo M, Vogel I, Lim KC, Jawahar S, Tricoche N, Voronin D, Corbo C, Ayiseh RB, Manfo FPT, Mbah GE, Cho-Ngwa F, Beerntsen B, Renslo AR, Lustigman S, Sakanari JA. Pyrvinium Pamoate and Structural Analogs Are Early Macrofilaricide Leads. Pharmaceuticals (Basel). 2022 Feb 02; 15(2).
Chen J, Gonciarz RL, Renslo AR. Correction: Expanded scope of Griesbaum co-ozonolysis for the preparation of structurally diverse sensors of ferrous iron. RSC Adv. 2021 Nov 10; 11(58):36625.
Kemp MT, Nichols DA, Zhang X, Defrees K, Na I, Renslo AR, Chen Y. Mutation of the conserved Asp-Asp pair impairs the structure, function, and inhibition of CTX-M Class A β-lactamase. FEBS Lett. 2021 12; 595(24):2981-2994.
Chen J, Gonciarz RL, Renslo AR. Expanded scope of Griesbaum co-ozonolysis for the preparation of structurally diverse sensors of ferrous iron. RSC Adv. 2021 Oct 18; 11(54):34338-34342.
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.
Gonciarz RL, Renslo AR. Emerging role of ferrous iron in bacterial growth and host-pathogen interaction: New tools for chemical (micro)biology and antibacterial therapy. Curr Opin Chem Biol. 2021 04; 61:170-178.
Gonciarz RL, Collisson EA, Renslo AR. Ferrous Iron-Dependent Pharmacology. Trends Pharmacol Sci. 2021 01; 42(1):7-18.
Zhao N, Huang Y, Wang YH, Muir RK, Chen YC, Wei J, Hooshdaran N, Viswanath P, Seo Y, Ruggero D, Renslo AR, Evans MJ. Ferronostics: Measuring Tumoral Ferrous Iron with PET to Predict Sensitivity to Iron-Targeted Cancer Therapies. J Nucl Med. 2021 Jul 01; 62(7):949-955.
Jílková A, Rubešová P, Fanfrlík J, Fajtová P, Rezácová P, Brynda J, Lepšík M, Mertlíková-Kaiserová H, Emal CD, Renslo AR, Roush WR, Horn M, Caffrey CR, Mareš M. Druggable Hot Spots in the Schistosomiasis Cathepsin B1 Target Identified by Functional and Binding Mode Analysis of Potent Vinyl Sulfone Inhibitors. ACS Infect Dis. 2021 05 14; 7(5):1077-1088.
Chen YC, Oses-Prieto JA, Pope LE, Burlingame AL, Dixon SJ, Renslo AR. Reactivity-Based Probe of the Iron(II)-Dependent Interactome Identifies New Cellular Modulators of Ferroptosis. J Am Chem Soc. 2020 11 11; 142(45):19085-19093.
Blank BR, Gonciarz RL, Talukder P, Gut J, Legac J, Rosenthal PJ, Renslo AR. Antimalarial Trioxolanes with Superior Drug-Like Properties and In Vivo Efficacy. ACS Infect Dis. 2020 07 10; 6(7):1827-1835.
Bashore C, Jaishankar P, Skelton NJ, Fuhrmann J, Hearn BR, Liu PS, Renslo AR, Dueber EC. Cyanopyrrolidine Inhibitors of Ubiquitin Specific Protease 7 Mediate Desulfhydration of the Active-Site Cysteine. ACS Chem Biol. 2020 06 19; 15(6):1392-1400.
Huff TC, Camarena V, Sant DW, Wilkes Z, Van Booven D, Aron AT, Muir RK, Renslo AR, Chang CJ, Monje PV, Wang G. Oscillatory cAMP signaling rapidly alters H3K4 methylation. Life Sci Alliance. 2020 01; 3(1).
Pemberton OA, Jaishankar P, Akhtar A, Adams JL, Shaw LN, Renslo AR, Chen Y. Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases. J Med Chem. 2019 09 26; 62(18):8480-8496.
Griffin AL, Jaishankar P, Grandjean JM, Olson SH, Renslo AR, Baraban SC. Zebrafish studies identify serotonin receptors mediating antiepileptic activity in Dravet syndrome. Brain Commun. 2019; 1(1):fcz008.
Ehrnhoefer DE, Skotte NH, Reinshagen J, Qiu X, Windshügel B, Jaishankar P, Ladha S, Petina O, Khankischpur M, Nguyen YTN, Caron NS, Razeto A, Meyer Zu Rheda M, Deng Y, Huynh KT, Wittig I, Gribbon P, Renslo AR, Geffken D, Gul S, Hayden MR. Activation of Caspase-6 Is Promoted by a Mutant Huntingtin Fragment and Blocked by an Allosteric Inhibitor Compound. Cell Chem Biol. 2019 09 19; 26(9):1295-1305.e6.
Blank BR, Talukder P, Muir RK, Green ER, Skaar EP, Renslo AR. Targeting Mobilization of Ferrous Iron in Pseudomonas aeruginosa Infection with an Iron(II)-Caged LpxC Inhibitor. ACS Infect Dis. 2019 08 09; 5(8):1366-1375.
DeFrees K, Kemp MT, ElHilali-Pollard X, Zhang X, Mohamed A, Chen Y, Renslo AR. An Empirical Study of Amide-Heteroarene π-Stacking Interactions Using Reversible Inhibitors of a Bacterial Serine Hydrolase. Org Chem Front. 2019 Jun 07; 6(11):1749-1756.
Torelli NJ, Akhtar A, DeFrees K, Jaishankar P, Pemberton OA, Zhang X, Johnson C, Renslo AR, Chen Y. Active-Site Druggability of Carbapenemases and Broad-Spectrum Inhibitor Discovery. ACS Infect Dis. 2019 06 14; 5(6):1013-1021.
Muir RK, Zhao N, Wei J, Wang YH, Moroz A, Huang Y, Chen YC, Sriram R, Kurhanewicz J, Ruggero D, Renslo AR, Evans MJ. Measuring Dynamic Changes in the Labile Iron Pool in Vivo with a Reactivity-Based Probe for Positron Emission Tomography. ACS Cent Sci. 2019 Apr 24; 5(4):727-736.
Raleigh DR, Sever N, Choksi PK, Sigg MA, Hines KM, Thompson BM, Elnatan D, Jaishankar P, Bisignano P, Garcia-Gonzalo FR, Krup AL, Eberl M, Byrne EFX, Siebold C, Wong SY, Renslo AR, Grabe M, McDonald JG, Xu L, Beachy PA, Reiter JF. Cilia-Associated Oxysterols Activate Smoothened. Mol Cell. 2018 10 18; 72(2):316-327.e5.
Pope L, Arrigoni C, Lou H, Bryant C, Gallardo-Godoy A, Renslo AR, Minor DL. Protein and Chemical Determinants of BL-1249 Action and Selectivity for K2P Channels. ACS Chem Neurosci. 2018 12 19; 9(12):3153-3165.
Pemberton OA, Zhang X, Nichols DA, DeFrees K, Jaishankar P, Bonnet R, Adams J, Shaw LN, Renslo AR, Chen Y. Antibacterial Spectrum of a Tetrazole-Based Reversible Inhibitor of Serine β-Lactamases. Antimicrob Agents Chemother. 2018 08; 62(8).
Tsai JC, Miller-Vedam LE, Anand AA, Jaishankar P, Nguyen HC, Renslo AR, Frost A, Walter P. Structure of the nucleotide exchange factor eIF2B reveals mechanism of memory-enhancing molecule. Science. 2018 03 30; 359(6383).
Spangler B, Kline T, Hanson J, Li X, Zhou S, Wells JA, Sato AK, Renslo AR. Toward a Ferrous Iron-Cleavable Linker for Antibody-Drug Conjugates. Mol Pharm. 2018 05 07; 15(5):2054-2059.
Camarena V, Sant DW, Huff TC, Mustafi S, Muir RK, Aron AT, Chang CJ, Renslo AR, Monje PV, Wang G. cAMP signaling regulates DNA hydroxymethylation by augmenting the intracellular labile ferrous iron pool. Elife. 2017 12 14; 6.
Aron AT, Heffern MC, Lonergan ZR, Vander Wal MN, Blank BR, Spangler B, Zhang Y, Park HM, Stahl A, Renslo AR, Skaar EP, Chang CJ. In vivo bioluminescence imaging of labile iron accumulation in a murine model of Acinetobacter baumannii infection. Proc Natl Acad Sci U S A. 2017 11 28; 114(48):12669-12674.
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.
Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM. Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States. Cell Chem Biol. 2017 12 21; 24(12):1455-1466.e14.
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.
Acker TM, Gable JE, Bohn MF, Jaishankar P, Thompson MC, Fraser JS, Renslo AR, Craik CS. Allosteric Inhibitors, Crystallography, and Comparative Analysis Reveal Network of Coordinated Movement across Human Herpesvirus Proteases. J Am Chem Soc. 2017 08 30; 139(34):11650-11653.
Blank BR, Gut J, Rosenthal PJ, Renslo AR. Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane. J Med Chem. 2017 07 27; 60(14):6400-6407.
Nakamura RL, Burlingame MA, Yang S, Crosby DC, Talbot DJ, Chui K, Frankel AD, Renslo AR. Identification and Optimization of Thienopyridine Carboxamides as Inhibitors of HIV Regulatory Complexes. Antimicrob Agents Chemother. 2017 07; 61(7).
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.
Spangler B, Fontaine SD, Shi Y, Sambucetti L, Mattis AN, Hann B, Wells JA, Renslo AR. A Novel Tumor-Activated Prodrug Strategy Targeting Ferrous Iron Is Effective in Multiple Preclinical Cancer Models. J Med Chem. 2016 12 22; 59(24):11161-11170.
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.
Spangler B, Morgan CW, Fontaine SD, Vander Wal MN, Chang CJ, Wells JA, Renslo AR. A reactivity-based probe of the intracellular labile ferrous iron pool. Nat Chem Biol. 2016 09; 12(9):680-5.
Hearn BR, Jaishankar P, Sidrauski C, Tsai JC, Vedantham P, Fontaine SD, Walter P, Renslo AR. Structure-Activity Studies of Bis-O-Arylglycolamides: Inhibitors of the Integrated Stress Response. ChemMedChem. 2016 Apr 19; 11(8):870-80.
Lauterwasser EM, Fontaine SD, Li H, Gut J, Katneni K, Charman SA, Rosenthal PJ, Bogyo M, Renslo AR. Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria. ACS Med Chem Lett. 2015 Nov 12; 6(11):1145-9.
Mott BT, Eastman RT, Guha R, Sherlach KS, Siriwardana A, Shinn P, McKnight C, Michael S, Lacerda-Queiroz N, Patel PR, Khine P, Sun H, Kasbekar M, Aghdam N, Fontaine SD, Liu D, Mierzwa T, Mathews-Griner LA, Ferrer M, Renslo AR, Inglese J, Yuan J, Roepe PD, Su XZ, Thomas CJ. High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations. Sci Rep. 2015 Sep 25; 5:13891.
Peniche AG, Renslo AR, Melby PC, Travi BL. Antileishmanial Activity of Disulfiram and Thiuram Disulfide Analogs in an Ex Vivo Model System Is Selectively Enhanced by the Addition of Divalent Metal Ions. Antimicrob Agents Chemother. 2015 Oct; 59(10):6463-70.
Giles K, Berry DB, Condello C, Hawley RC, Gallardo-Godoy A, Bryant C, Oehler A, Elepano M, Bhardwaj S, Patel S, Silber BM, Guan S, DeArmond SJ, Renslo AR, Prusiner SB. Different 2-Aminothiazole Therapeutics Produce Distinct Patterns of Scrapie Prion Neuropathology in Mouse Brains. J Pharmacol Exp Ther. 2015 Oct; 355(1):2-12.
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.
Nichols DA, Hargis JC, Sanishvili R, Jaishankar P, Defrees K, Smith EW, Wang KK, Prati F, Renslo AR, Woodcock HL, Chen Y. Ligand-Induced Proton Transfer and Low-Barrier Hydrogen Bond Revealed by X-ray Crystallography. J Am Chem Soc. 2015 Jul 01; 137(25):8086-95.
Sidrauski C, Tsai JC, Kampmann M, Hearn BR, Vedantham P, Jaishankar P, Sokabe M, Mendez AS, Newton BW, Tang EL, Verschueren E, Johnson JR, Krogan NJ, Fraser CS, Weissman JS, Renslo AR, Walter P. Pharmacological dimerization and activation of the exchange factor eIF2B antagonizes the integrated stress response. Elife. 2015 Apr 15; 4:e07314.
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.
Zhou Y, Vedantham P, Lu K, Agudelo J, Carrion R, Nunneley JW, Barnard D, Pöhlmann S, McKerrow JH, Renslo AR, Simmons G. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Res. 2015 Apr; 116:76-84.
Turner DM, Tom CT, Renslo AR. Simple plate-based, parallel synthesis of disulfide fragments using the CuAAC click reaction. ACS Comb Sci. 2014 Dec 08; 16(12):661-4.
Fontaine SD, DiPasquale AG, Renslo AR. Efficient and stereocontrolled synthesis of 1,2,4-trioxolanes useful for ferrous iron-dependent drug delivery. Org Lett. 2014 Nov 07; 16(21):5776-9.
Fontaine SD, Spangler B, Gut J, Lauterwasser EM, Rosenthal PJ, Renslo AR. Drug delivery to the malaria parasite using an arterolane-like scaffold. ChemMedChem. 2015 Jan; 10(1):47-51.
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.
Gable JE, Lee GM, Jaishankar P, Hearn BR, Waddling CA, Renslo AR, Craik CS. Broad-spectrum allosteric inhibition of herpesvirus proteases. Biochemistry. 2014 Jul 22; 53(28):4648-60.
Debnath A, Shahinas D, Bryant C, Hirata K, Miyamoto Y, Hwang G, Gut J, Renslo AR, Pillai DR, Eckmann L, Reed SL, McKerrow JH. Hsp90 inhibitors as new leads to target parasitic diarrheal diseases. Antimicrob Agents Chemother. 2014 Jul; 58(7):4138-44.
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.
Ghaemmaghami S, Russo M, Renslo AR. Successes and challenges in phenotype-based lead discovery for prion diseases. J Med Chem. 2014 Aug 28; 57(16):6919-29.
Nichols DA, Renslo AR, Chen Y. Fragment-based inhibitor discovery against β-lactamase. Future Med Chem. 2014 Mar; 6(4):413-27.
Silber BM, Gever JR, Rao S, Li Z, Renslo AR, Widjaja K, Wong C, Giles K, Freyman Y, Elepano M, Irwin JJ, Jacobson MP, Prusiner SB. Novel compounds lowering the cellular isoform of the human prion protein in cultured human cells. Bioorg Med Chem. 2014 Mar 15; 22(6):1960-72.
Renslo AR. Antimalarial Drug Discovery: From Quinine to the Dream of Eradication. ACS Med Chem Lett. 2013 Dec 12; 4(12):1126-1128.
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.
Murray J, Renslo AR. Modulating caspase activity: beyond the active site. Curr Opin Struct Biol. 2013 Dec; 23(6):812-9.
Deu E, Chen IT, Lauterwasser EM, Valderramos J, Li H, Edgington LE, Renslo AR, Bogyo M. Ferrous iron-dependent drug delivery enables controlled and selective release of therapeutic agents in vivo. Proc Natl Acad Sci U S A. 2013 Nov 05; 110(45):18244-9.
Berry DB, Lu D, Geva M, Watts JC, Bhardwaj S, Oehler A, Renslo AR, DeArmond SJ, Prusiner SB, Giles K. Drug resistance confounding prion therapeutics. Proc Natl Acad Sci U S A. 2013 Oct 29; 110(44):E4160-9.
Peniche AG, Osorio Y, Renslo AR, Frantz DE, Melby PC, Travi BL. Development of an ex vivo lymph node explant model for identification of novel molecules active against Leishmania major. Antimicrob Agents Chemother. 2014; 58(1):78-87.
Silber BM, Gever JR, Li Z, Gallardo-Godoy A, Renslo AR, Widjaja K, Irwin JJ, Rao S, Jacobson MP, Ghaemmaghami S, Prusiner SB. Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells. Bioorg Med Chem. 2013 Dec 15; 21(24):7999-8012.
Lu D, Giles K, Li Z, Rao S, Dolghih E, Gever JR, Geva M, Elepano ML, Oehler A, Bryant C, Renslo AR, Jacobson MP, Dearmond SJ, Silber BM, Prusiner SB. Biaryl amides and hydrazones as therapeutics for prion disease in transgenic mice. J Pharmacol Exp Ther. 2013 Nov; 347(2):325-38.
Nishino M, Choy JW, Gushwa NN, Oses-Prieto JA, Koupparis K, Burlingame AL, Renslo AR, McKerrow JH, Taunton J. Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei [corrected]. Elife. 2013 Jul 09; 2:e00712.
Fan P, Manoli DS, Ahmed OM, Chen Y, Agarwal N, Kwong S, Cai AG, Neitz J, Renslo A, Baker BS, Shah NM. Genetic and neural mechanisms that inhibit Drosophila from mating with other species. Cell. 2013 Jul 03; 154(1):89-102.
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.
Li Z, Silber BM, Rao S, Gever JR, Bryant C, Gallardo-Godoy A, Dolghih E, Widjaja K, Elepano M, Jacobson MP, Prusiner SB, Renslo AR. 2-Aminothiazoles with improved pharmacotherapeutic properties for treatment of prion disease. ChemMedChem. 2013 May; 8(5):847-57.
Silber BM, Rao S, Fife KL, Gallardo-Godoy A, Renslo AR, Dalvie DK, Giles K, Freyman Y, Elepano M, Gever JR, Li Z, Jacobson MP, Huang Y, Benet LZ, Prusiner SB. Pharmacokinetics and metabolism of 2-aminothiazoles with antiprion activity in mice. Pharm Res. 2013 Apr; 30(4):932-50.
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.
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.
Mahajan SS, Gut J, Rosenthal PJ, Renslo AR. Ferrous iron-dependent delivery of therapeutic agents to the malaria parasite. Future Med Chem. 2012 Dec; 4(18):2241-9.
Rafi SB, Hearn BR, Vedantham P, Jacobson MP, Renslo AR. Predicting and improving the membrane permeability of peptidic small molecules. J Med Chem. 2012 Apr 12; 55(7):3163-9.
Nichols DA, Jaishankar P, Larson W, Smith E, Liu G, Beyrouthy R, Bonnet R, Renslo AR, Chen Y. Structure-based design of potent and ligand-efficient inhibitors of CTX-M class A β-lactamase. J Med Chem. 2012 Mar 08; 55(5):2163-72.
Hartwig CL, Lauterwasser EM, Mahajan SS, Hoke JM, Cooper RA, Renslo AR. Investigating the antimalarial action of 1,2,4-trioxolanes with fluorescent chemical probes. J Med Chem. 2011 Dec 08; 54(23):8207-13.
Robertson SA, Renslo AR. Drug discovery for neglected tropical diseases at the Sandler Center. Future Med Chem. 2011 Aug; 3(10):1279-88.
Dolghih E, Bryant C, Renslo AR, Jacobson MP. Predicting binding to p-glycoprotein by flexible receptor docking. PLoS Comput Biol. 2011 Jun; 7(6):e1002083.
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.
Burlingame MA, Tom CT, Renslo AR. Simple one-pot synthesis of disulfide fragments for use in disulfide-exchange screening. ACS Comb Sci. 2011 May 09; 13(3):205-8.
Osorio Y, Travi BL, Renslo AR, Peniche AG, Melby PC. Identification of small molecule lead compounds for visceral leishmaniasis using a novel ex vivo splenic explant model system. PLoS Negl Trop Dis. 2011 Feb 15; 5(2):e962.
Mahajan SS, Deu E, Lauterwasser EM, Leyva MJ, Ellman JA, Bogyo M, Renslo AR. A fragmenting hybrid approach for targeted delivery of multiple therapeutic agents to the malaria parasite. ChemMedChem. 2011 Mar 07; 6(3):415-9.
Gallardo-Godoy A, Gever J, Fife KL, Silber BM, Prusiner SB, Renslo AR. 2-Aminothiazoles as therapeutic leads for prion diseases. J Med Chem. 2011 Feb 24; 54(4):1010-21.
Renslo AR. Antibacterial oxazolidinones: emerging structure-toxicity relationships. Expert Rev Anti Infect Ther. 2010 May; 8(5):565-74.
Thomas, RC, Poel, T-J, Barbachyn, MR, Gordeev, MF, Luehr, GW, Renslo, A, Singh, U, Joysula, VPVN. N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 7,645,781. 2010.
Diamond, M, Jones, J, Renslo, A. Small-Molecule Inhibitors of the Androgen Receptor US Patent 7,696,227. 2010.
Ghaemmaghami S, May BC, Renslo AR, Prusiner SB. Discovery of 2-aminothiazoles as potent antiprion compounds. J Virol. 2010 Apr; 84(7):3408-12.
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.
Ferreira RS, Bryant C, Ang KK, McKerrow JH, Shoichet BK, Renslo AR. Divergent modes of enzyme inhibition in a homologous structure-activity series. J Med Chem. 2009 Aug 27; 52(16):5005-8.
Abdulla MH, Ruelas DS, Wolff B, Snedecor J, Lim KC, Xu F, Renslo AR, Williams J, McKerrow JH, Caffrey CR. Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening. PLoS Negl Trop Dis. 2009 Jul 14; 3(7):e478.
Renslo, AR. When Medical Need is not Matched by Market Opportunity. Pharma Focus Asia. 2008; 9:24-26.
Jaishankar P, Hansell E, Zhao DM, Doyle PS, McKerrow JH, Renslo AR. Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes. Bioorg Med Chem Lett. 2008 Jan 15; 18(2):624-8.
Gao H, Renslo AR. A practical synthesis of differentially protected 2-(hydroxymethyl)piperazines. J Org Chem. 2007 Oct 26; 72(22):8591-2.
Renslo AR, Atuegbu A, Herradura P, Jaishankar P, Ji M, Leach KL, Huband MD, Dermyer MR, Wu L, Vara Prasad JV, Gordeev MF. A distal methyl substituent attenuates mitochondrial protein synthesis inhibition in oxazolidinone antibacterials. Bioorg Med Chem Lett. 2007 Sep 15; 17(18):5036-40.
Renslo, AR, Gordeev, MF, Patel, DV, Gao, H, and Josyula, VPVN. Antimicrobial [3.1.0] bicyclohexylphenyl-oxazolidinone derivatives and analogues. US Patent 7,279,494. 2007.
Renslo, AR. The Echinocandins: Total and Semi-Synthetic Approaches in Anti-fungal Drug Discovery. Anti-infective Agents in Medicinal Chemistry. 2007; 6:201-212.
Renslo AR, McKerrow JH. Drug discovery and development for neglected parasitic diseases. Nat Chem Biol. 2006 Dec; 2(12):701-10.
Renslo AR, Luehr GW, Lam S, Westlund NE, Gómez M, Hackbarth CJ, Patel DV, Gordeev MF. Synthesis and structure-activity studies of antibacterial oxazolidinones containing dihydrothiopyran or dihydrothiazine C-rings. Bioorg Med Chem Lett. 2006 Jul 01; 16(13):3475-8.
Renslo AR, Luehr GW, Gordeev MF. Recent developments in the identification of novel oxazolidinone antibacterial agents. Bioorg Med Chem. 2006 Jun 15; 14(12):4227-40.
Renslo AR, Gao H, Jaishankar P, Venkatachalam R, Gómez M, Blais J, Huband M, Vara Prasad JV, Gordeev MF. Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones. Bioorg Med Chem Lett. 2006 Mar 01; 16(5):1126-9.
Gordeev, MF, Renslo, A, Luehr, GW, Lam, S, Westlund, NE, and Patel, DV. Antimicrobial Dihydrothiazine and Dihydrothiopyran Oxazolidinones. US Patent 7,101,874. 2006.
Thomas, RC, Poel, T-J, Barbachyn, MR, Gordeev, MF, Luehr, GW, Renslo, A, Singh, U, Joysula, VPVN. N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 7,141,588. 2006.
Renslo AR, Jaishankar P, Venkatachalam R, Hackbarth C, Lopez S, Patel DV, Gordeev MF. Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones. J Med Chem. 2005 Jul 28; 48(15):5009-24.
Renslo AR, Gao H, Jaishankar P, Venkatachalam R, Gordeev MF. Synthesis of aza-, oxa-, and thiabicyclo[3.1.0]hexane heterocycles from a common synthetic intermediate. Org Lett. 2005 Jun 23; 7(13):2627-30.
Gordeev, MF, Renslo, A, and Patel, DV.. Antimicrobial [3.1.0] Bicyclic Oxazolidinone Derivatives. US Patent 6,875,784. 2005.
Gordeev, MF, Renslo, A, Luehr, GW, Lam, S, Westlund, NE, and Patel, DV. Antimicrobial Dihydrothiazine and Dihydrothiopyran Oxazolidinones. US Patent 6,884,813. 2005.
Thomas, RC, Poel, T-J, Barbachyn, MR, Gordeev, MF, Luehr, GW, Renslo, A, and Singh, U. N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 6,919,329. 2005.
Amos DT, Renslo AR, Danheiser RL. Intramolecular [4 + 2] cycloadditions of iminoacetonitriles: a new class of azadienophiles for hetero Diels-Alder reactions. J Am Chem Soc. 2003 Apr 30; 125(17):4970-1.
Danheiser, RL, Renslo, AR, Amos, DT, and Wright, GT. Preparation of Substituted Pyridines via Regiocontrolled [4+2] Cycloadditions of Oximinosulfonates: Methyl 5-Methylpyridine-2-Carboxylate. Org. Syn. 2003; 80:133-143.
Wash PL, Renslo AR, Rebek J. Isolation of an Acid/Base Complex in Solution Puts the Brakes on Nitrogen Inversion We are grateful for financial support from the Skaggs Research Foundation and the National Institutes of Health. We are pleased to acknowledge advice from Professors Stephen Craig and Dmitry Rudkevich. Angew Chem Int Ed Engl. 2001 04 01; 40(7):1221-1222.
Wash, PL, Renslo, AR, and Rebek, J.. Isolation of an Acid/Base Complex in Solution Puts the Brakes on Nitrogen Inversion. Angew. Chem. Int. Ed. 2001; 40:1221-1222.
Renslo AR, Rebek J. Molecular Recognition with Introverted Functionality We are grateful for financial support from the Skaggs Research Foundation and the National Institutes of Health. We thank Prof. Dmitry Rudkevich and Dr. Paul Wash and Dr. Laura Pasternack for helpful advice and instrumental support. Angew Chem Int Ed Engl. 2000 09 15; 39(18):3281-3283.
Tucci FC, Renslo AR, Rudkevich DM, Rebek Jr J. Nanoscale Container Structures and Their Host - Guest Properties We are grateful for financial support from the Skaggs Research Foundation and the National Institutes of Health. Dr. Laura Pasternack and Dr. Takeharu Haino are sincerely acknowledged for assistance with the 2D NMR experiments and experimental advise, respectively. Angew Chem Int Ed Engl. 2000 03; 39(6):1076-1079.
Renslo, AR and Rebek, J.. Molecular Recognition with Introverted Functionality. Angew. Chem. Int. Ed. 2000; 39:3281-3283.
Tucci, FC, Renslo, AR, Rudkevich, DM, and Rebek, J.. Nanoscale Container Structures and their Host¬–Guest Properties. Angew. Chem. Int. Ed. 2000; 39:1076-1079.
Renslo, AR, Tucci, FC, Rudkevich, DM, and Rebek, J. . Synthesis and Assembly of Self-Complementary Cavitands. J. Am. Chem. Soc. 2000; 122:4573-4582.
Lützen, A, Renslo, AR, Schalley, CA, O’Leary, BM, and Rebek, J.. Encapsulation of Ion-Molecule Complexes: Second-Sphere Supramolecular Chemistry. J. Am. Chem. Soc. 1999; 121:7455-7456.
Renslo, AR, Rudkevich, DM, and Rebek, J.. Self-Complementary Cavitands. J. Am. Chem. Soc. 1999; 121:7459-7460.
Weinstein, RD, Renslo, AR, Danheiser, RL, and Tester, JW. Silica-Promoted Diels–Alder Reactions in Carbon Dioxide from Gaseous to Supercritical Conditions. J. Phys. Chem. B. 1999; 103:2878-2887.
Renslo, AR and Danheiser, RL.. Synthesis of Substituted Pyridines via Regiocontrolled [4+2] Cycloadditions of Oximinosulfonates. J. Org. Chem. 1998; 63:7840-7850.
Renslo AR, Weinstein RD, Tester JW, Danheiser RL. Concerning the Regiochemical Course of the Diels-Alder Reaction in Supercritical Carbon Dioxide. J Org Chem. 1997 Jun 27; 62(13):4530-4533.
Renslo, AR, Weinstein, RD, Tester, JW, and Danheiser, RL.. Concerning the Regiochemical Course of the Diels–Alder Reaction in Supercritical Carbon Dioxide. J. Org. Chem. 1997; 62:4530-4533.
Weinstein, RD, Renslo, AR, Danheiser, RL, Harris, JG, and Tester, JW.. Kinetic Correlation of Diels–Alder Reactions in Supercritical Carbon Dioxide. J. Phys. Chem. 1996; 100:12337-12341.