University of California San Francisco
Helen Diller Family Comprehensive Cancer Center
Michelle Arkin, PhD

Michelle Arkin, PhD

Professor, Department of Pharmaceutical Chemistry, UCSF

Cancer Center Program Memberships

Experimental Therapeutics

Research Summary

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 Associate Director of the Small Molecule Discovery Center, a collaborative research and core lab that includes a high-throughput screening facility (smdc.ucsf.edu).

Education

1990, Bryn Mawr College, Bryn Mawr, PA, B.A., Chemistry
1997, California Institute of Technology, Pasadena, CA, Ph.D., Chemistry
1999, Genentech, Inc, South San Francisco, CA and Sunesis Pharmaceuticals, Redwood City, CA, Postdoctoral fellowship, Protein Engineering


Professional Experience

  • 1999 - 2007
    Scientist, Staff Scientist, Senior Scientist, Associate Director of Cell Biology, Sunesis Pharmaceuticals, South San Francisco, CA
  • 2007 - present
    Associate Director, Biology, Small Molecule Discovery Center, UCSF
  • 2007 - 2013
    Assistant Adjunct Professor, Pharmaceutical Chemistry, UCSF
  • 2011 - 2013
    Associate Adjunct Professor, Pharmaceutical Chemistry, UCSF
  • 2014 - 2017
    Associate Professor in Residence, Pharmaceutical Chemistry, UCSF
  • 2017 - present
    Professor in Residence, Pharmaceutical Chemistry, UCSF

Honors & Awards

  • 1991
    European Traveling Fellowship, Bryn Mawr College
  • 1991-1992
    Blodgett Fellowship, General Electric Foundation
  • 1992-1995
    National Science Foundation Predoctoral Fellowship
  • 1995-1997
    National Institutes of Health Traineeship
  • 1997-1999
    Daymon Runyon-Walter Winchell Cancer Research Postdoctoral Fellowship
  • 2010
    Keynote address, Drug Discovery Chemistry, Protein-Protein Interactions (San Diego)
  • 2012
    Keynote speaker, EFMC-ISMC (Berlin)
  • 2013
    Keynote speaker, PPI-NET (London)
  • 2013
    Finalist, SLAS Innovation Award

Selected Publications

  1. Zhong M, Lee GM, Sijbesma E, Ottmann C, Arkin MR. Modulating protein-protein interaction networks in protein homeostasis. Curr Opin Chem Biol. 2019 Mar 23; 50:55-65.
    View on PubMed
  2. Sijbesma E, Hallenbeck KK, Leysen S, de Vink P, Skora 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 Feb 01.
    View on PubMed
  3. 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.
    View on PubMed
  4. 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 Oct 30; 9(5).
    View on PubMed
  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.
    View on PubMed
  6. 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.
    View on PubMed
  7. 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 Sep 01; 159(9):3321-3330.
    View on PubMed
  8. 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).
    View on PubMed
  9. 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 Sep; 11(5):461-470.
    View on PubMed
  10. Markossian S, Ang KK, Wilson CG, Arkin MR. Small-Molecule Screening for Genetic Diseases. Annu Rev Genomics Hum Genet. 2018 Aug 31; 19:263-288.
    View on PubMed
  11. 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.
    View on PubMed
  12. 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 Feb; 23(2):183-192.
    View on PubMed
  13. 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.
    View on PubMed
  14. 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.
    View on PubMed
  15. 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.
    View on PubMed
  16. 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.
    View on PubMed
  17. 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.
    View on PubMed
  18. 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.
    View on PubMed
  19. 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.
    View on PubMed
  20. 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.
    View on PubMed

Go to UCSF Profiles, powered by CTSI