University of California San Francisco
Helen Diller Family Comprehensive Cancer Center
Adam Renslo, PhD

Adam Renslo, PhD

Associate Professor of Pharmaceutical Chemistry, UCSF

Cancer Center Program Memberships

Experimental Therapeutics

Research Summary

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. Using such small molecule probes, we are exploring the mechanisms underlying the action of artemisinin and related antimalarial drugs. Finally, we are inventing and employing new platform technologies in an effort to expand the realm of druggable target space and drug-like chemical space. These technologies include fragment-based approaches to target protein-protein interfaces and allosteric modulation of enzymes, the use of novel unnatural amino acids to discover cell-permeable peptides, and new targeted prodrug approaches in cancer and infectious disease.

Education

St. Olaf College, Northfield, MN, B.A., 05/1993, Chemistry
Massachusetts Institute of Technology, Ph.D., 05/1998, Organic Chemistry
The Scripps Research Institute, La Jolla, CA, Postdoctoral, 12/2000, Molecular Recognition


Professional Experience

  • 2000-2003
    Sr. Scientist, Group Leader, Medicinal Chemistry, Vicuron Pharmaceuticals
  • 2004-2005
    Associate Director, Medicinal Chemistry, Vicuron Pharmaceuticals (later Pfizer)
  • 2006-2011
    Assistant Adjunct Professor, Department of Pharmaceutical Chemistry, UCSF
  • 2011-2013
    Associate Adjunct Professor, Department of Pharmaceutical Chemistry, UCSF
  • 2006-present
    Associate Director, Small Molecule Discovery Center, UCSF
  • 2014-present
    Associate Professor, Department of Pharmaceutical Chemistry, UCSF

Selected Publications

  1. 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 Nov 14.
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  2. 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 Oct 26; 550(7677):534-538.
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  3. 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 Sep 19.
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  4. 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. 2017 Sep 01; 2472555217732072.
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  5. 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 Aug 30; 139(34):11650-11653.
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  6. 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 Jul 27; 60(14):6400-6407.
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  7. 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 Jul; 61(7).
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  8. 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.
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  9. 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 Dec 22; 59(24):11161-11170.
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  10. 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 ATF6a branch. Elife. 2016 Jul 20; 5.
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  11. 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 Sep; 12(9):680-5.
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  12. 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.
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  13. 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.
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  14. 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.
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  15. 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.
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  16. 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.
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  17. Neitz RJ, Bryant C, Chen S, Gut J, Caselli EH, 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):4834-7.
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  18. 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.
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  19. 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.
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  20. 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.
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