Michelle Arkin, PhD

A B C D E F G H I J K L M N O P Q R S T U V W X Y Z
Michelle Arkin, PhD

Associate Professor, Department of Pharmaceutical Chemistry, UCSF

michelle.arkin@ucsf.edu

Box 2552, UCSF
San Francisco, CA 94143-2552

UCSF Profiles | Lab Website

Cancer Center Membership

Member » Developmental 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, San Francisco, CA
  • 2007 - 2013
    Assistant Adjunct Professor, Pharmaceutical Chemistry, UCSF, San Francisco, CA
  • 2011 - 2013
    Associate Adjunct Professor, Pharmaceutical Chemistry, UCSF, San Francisco, CA
  • 2014 - present
    Associate Professor in Residence, Pharmaceutical Chemistry, UCSF, San Francisco, CA

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. Pappalardo Z, Chopra DG, 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 Feb 28.
    View on PubMed
  2. 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. J Biomol Screen. 2016 Dec 08.
    View on PubMed
  3. 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.
    View on PubMed
  4. 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; 5.
    View on PubMed
  5. Hallenbeck KK, Turner DM, Renslo AR, Arkin MR. Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery. Curr Top Med Chem. 2016 Jul 19.
    View on PubMed
  6. Bulfer SL, Chou TF, Arkin MR. p97 Disease Mutations Modulate Nucleotide-Induced Conformation to Alter Protein-Protein Interactions. ACS Chem Biol. 2016 Jun 13.
    View on PubMed
  7. 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.
    View on PubMed
  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.
    View on PubMed
  9. 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; 4.
    View on PubMed
  10. Visscher M, Arkin MR, Dansen TB. Covalent targeting of acquired cysteines in cancer. Curr Opin Chem Biol. 2016 Feb; 30:61-7.
    View on PubMed
  11. 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.
    View on PubMed
  12. 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 Nov; 14(11):733-4.
    View on PubMed
  13. 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.
    View on PubMed
  14. 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 Jun; 9(6):e0003878.
    View on PubMed
  15. 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 1; 25(21):4834-7.
    View on PubMed
  16. 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 7; 112(14):E1705-14.
    View on PubMed
  17. Tran K, Arkin MR, Beal PA. Tethering in RNA: an RNA-binding fragment discovery tool. Molecules. 2015; 20(3):4148-61.
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  18. 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.
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  19. 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.
    View on PubMed
  20. 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 1; 465(1):149-61.
    View on PubMed

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