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. 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 Sep 26; 62(18):8480-8496.
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  2. 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.
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  3. 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 Sep 19; 26(9):1295-1305.e6.
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  4. 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 Aug 09; 5(8):1366-1375.
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  5. 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 Jun 14; 5(6):1013-1021.
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  6. 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.
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  7. 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.
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  8. 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.
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  9. 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 ß-Lactamases. Antimicrob Agents Chemother. 2018 08; 62(8).
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  10. 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).
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  11. 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.
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  12. 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.
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  13. 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.
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  14. 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.
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  15. 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.
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  16. 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.
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  17. 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.
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  18. 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.
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  19. 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).
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  20. 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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