Michelle R Arkin

Summary

Affiliation: University of California
Country: USA

Publications

  1. doi request reprint The road less traveled: modulating signal transduction enzymes by inhibiting their protein-protein interactions
    Michelle R Arkin
    Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, United States
    Curr Opin Chem Biol 13:284-90. 2009
  2. ncbi request reprint Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery
    Kenneth K Hallenbeck
    Department of Pharmaceutical Chemistry, University of California, San Francisco, Box 2552, San Francisco, CA 94158
    Curr Top Med Chem . 2016
  3. pmc Small-molecule inhibitors of protein-protein interactions: progressing toward the reality
    Michelle R Arkin
    Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco, San Francisco, CA 94158, USA Electronic address
    Chem Biol 21:1102-14. 2014
  4. ncbi request reprint UCSF Small Molecule Discovery Center: innovation, collaboration and chemical biology in the Bay Area
    Michelle R Arkin
    Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco 1700 4th St, Box 2552, San Francisco, CA 94158, USA
    Comb Chem High Throughput Screen 17:333-42. 2014
  5. ncbi request reprint Inhibiting caspase-6 activation and catalytic activity for neurodegenerative diseases
    John A Flygare
    Small Molecule Discovery Center, University of California San Francisco, San Francisco, CA, 94158, USA
    Curr Top Med Chem 14:319-25. 2014
  6. pmc Mining a cathepsin inhibitor library for new antiparasitic drug leads
    Kenny K H Ang
    The Small Molecule Discovery Center, University of California San Francisco, San Francisco, California, United States of America
    PLoS Negl Trop Dis 5:e1023. 2011
  7. pmc Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target
    Jonathan W Choy
    Small Molecule Discovery Center, University of California San Francisco, 1700 4th Street, San Francisco, CA, 94158, USA Department of Pharmaceutical Chemistry, University of California San Francisco, 1700 4th Street, San Francisco, CA, 94158, USA Department of Cellular and Molecular Pharmacology, University of California San Francisco, 1700 4th Street, San Francisco, CA, 94158, USA
    Beilstein J Org Chem 9:15-25. 2013
  8. pmc A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit
    Géraldine De Muylder
    Department of Pathology, Sandler Center for Drug Discovery, University of California San Francisco, San Francisco, California, United States of America
    PLoS Negl Trop Dis 5:e1253. 2011
  9. pmc Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51
    Shamila S Gunatilleke
    Sandler Center for Drug Discovery, University of California San Francisco, San Francisco, California, United States of America
    PLoS Negl Trop Dis 6:e1736. 2012
  10. pmc Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease
    R Jeffrey Neitz
    Small Molecule Discovery Center, and Department of Pharmaceutical Chemistry, University of California, San Francisco, San Francisco, CA 94158, United States
    Bioorg Med Chem Lett 25:4834-7. 2015

Research Grants

Collaborators

  • Adam R Renslo
  • R Jeffrey Neitz
  • Anjan Debnath
  • Larissa M Podust
  • Philip J Rosenthal
  • James McKerrow
  • Jonathan A Winger
  • Tsui Fen Chou
  • Jiri Gut
  • Peter Walter
  • Juan C Engel
  • Adrian Whitty
  • Zachary B Mackey
  • Brian R Hearn
  • Esther Orozco
  • Kenny K H Ang
  • Steven Chen
  • Stacie L Bulfer
  • Christopher G Wilson
  • Shamila S Gunatilleke
  • Clifford Bryant
  • Kenneth K Hallenbeck
  • Ciara M Gallagher
  • Patrick R Visperas
  • Miyuki Suzawa
  • Michael S Chimenti
  • John A Flygare
  • Matthew P Jacobson
  • Sviatoslav N Bagriantsev
  • Jonathan W Choy
  • Claudia M Calvet
  • Priyadarshini Jaishankar
  • Jonathan B Johnston
  • Yinyan Tang
  • Géraldine De Muylder
  • Joseline Ratnam
  • David M Turner
  • John Kuriyan
  • Carolina Garri
  • Kenny Kean Hooi Ang
  • Qingrong Yan
  • Andrés Aranda-Díaz
  • Kevin Lin
  • Arthur Weiss
  • Erica L Cain
  • John S Schneekloth
  • Mark J S Kelly
  • Diego A Miranda
  • Emily J Faivre
  • Thomas L James
  • Karmela A Ramos
  • Yeong Sang Kim
  • Aaron Diaz
  • Holly A Ingraham
  • Laura Caboni
  • Robert J Fletterick
  • Alma L Burlingame
  • Daniel L Minor
  • Kean Hooi Ang
  • Siegfried S F Leung
  • Jack Taunton
  • Kimberly A Clark
  • Patricia S Doyle
  • Juan A Oses-Prieto
  • Alejandra Gallardo-Godoy
  • Chiung Kuang Chen
  • Grigori Erenburg
  • Joseph Mulvaney
  • Elizabeth Hansell
  • James A Wells
  • Katarzyna M Skrzypczynska
  • Jennifer Legac
  • Moumita Debnath
  • Linda S Brinen
  • Iain D Kerr
  • Rafaela S Ferreira
  • Dongmei Zhao

Detail Information

Publications21

  1. doi request reprint The road less traveled: modulating signal transduction enzymes by inhibiting their protein-protein interactions
    Michelle R Arkin
    Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, United States
    Curr Opin Chem Biol 13:284-90. 2009
    ..However, the hypothesis that targeting such sites might confer on the resulting inhibitors improved properties of efficacy and/or tolerability, while appealing, remains largely untested...
  2. ncbi request reprint Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery
    Kenneth K Hallenbeck
    Department of Pharmaceutical Chemistry, University of California, San Francisco, Box 2552, San Francisco, CA 94158
    Curr Top Med Chem . 2016
    ....
  3. pmc Small-molecule inhibitors of protein-protein interactions: progressing toward the reality
    Michelle R Arkin
    Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco, San Francisco, CA 94158, USA Electronic address
    Chem Biol 21:1102-14. 2014
    ..Here, we review the last 10 years of progress, focusing on the properties of PPI inhibitors that have advanced to clinical trials and prospects for the future of PPI drug discovery. ..
  4. ncbi request reprint UCSF Small Molecule Discovery Center: innovation, collaboration and chemical biology in the Bay Area
    Michelle R Arkin
    Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco 1700 4th St, Box 2552, San Francisco, CA 94158, USA
    Comb Chem High Throughput Screen 17:333-42. 2014
    ..The SMDC, located in the biotech-focused Mission Bay neighborhood in San Francisco, is a hub for innovative small-molecule discovery research at UCSF. ..
  5. ncbi request reprint Inhibiting caspase-6 activation and catalytic activity for neurodegenerative diseases
    John A Flygare
    Small Molecule Discovery Center, University of California San Francisco, San Francisco, CA, 94158, USA
    Curr Top Med Chem 14:319-25. 2014
    ..The successful structure of the agreement serves as a model for future collaborations at both institutions...
  6. pmc Mining a cathepsin inhibitor library for new antiparasitic drug leads
    Kenny K H Ang
    The Small Molecule Discovery Center, University of California San Francisco, San Francisco, California, United States of America
    PLoS Negl Trop Dis 5:e1023. 2011
    ..The end products of this effort include the identification of sub-micromolar cell-active leads as well as the elucidation of structure-activity trends that can guide further optimization efforts...
  7. pmc Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target
    Jonathan W Choy
    Small Molecule Discovery Center, University of California San Francisco, 1700 4th Street, San Francisco, CA, 94158, USA Department of Pharmaceutical Chemistry, University of California San Francisco, 1700 4th Street, San Francisco, CA, 94158, USA Department of Cellular and Molecular Pharmacology, University of California San Francisco, 1700 4th Street, San Francisco, CA, 94158, USA
    Beilstein J Org Chem 9:15-25. 2013
    ..Computational docking studies and the evaluation of truncated analogues of 4 reveal structural determinants for TcCYP51 binding, information that will be useful in further optimization of this new class of inhibitors...
  8. pmc A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit
    Géraldine De Muylder
    Department of Pathology, Sandler Center for Drug Discovery, University of California San Francisco, San Francisco, California, United States of America
    PLoS Negl Trop Dis 5:e1253. 2011
    ..This compound affects intracellular but not axenic parasites, suggesting a host cell-dependent mechanism of action, opening new avenues for anti-leishmanial chemotherapy...
  9. pmc Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51
    Shamila S Gunatilleke
    Sandler Center for Drug Discovery, University of California San Francisco, San Francisco, California, United States of America
    PLoS Negl Trop Dis 6:e1736. 2012
    ..The discovery and development of new routes to chemotherapy for Chagas Disease is a clear priority...
  10. pmc Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease
    R Jeffrey Neitz
    Small Molecule Discovery Center, and Department of Pharmaceutical Chemistry, University of California, San Francisco, San Francisco, CA 94158, United States
    Bioorg Med Chem Lett 25:4834-7. 2015
    ..Through modifications of the P1, P2 and/or P3 positions, new analogs have been identified with reduced lipophilicity, enhanced potency, and improved oral exposure and bioavailability. ..
  11. doi request reprint An image-based assay for high throughput screening of Giardia lamblia
    Jiri Gut
    Sandler Center for Drug Discovery, University of California, San Francisco, USA
    J Microbiol Methods 84:398-405. 2011
    ..lamblia at low- or sub-micromolar concentrations. Our high throughput assay should facilitate evaluation of available chemical libraries for novel drugs to treat giardiasis...
  12. pmc Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases
    Clifford Bryant
    Small Molecule Discovery Center, University of California, San Francisco, CA 94158, USA
    Bioorg Med Chem Lett 19:6218-21. 2009
    ....
  13. pmc Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branch
    Ciara M Gallagher
    Department of Biochemistry and Biophysics, Howard Hughes MedicaI Institute, University of California, San Francisco, United States
    elife 5:. 2016
    ..The discovery of Ceapins now enables pharmacological modulation all three UPR branches either singly or in combination. ..
  14. pmc Structural and enzymatic insights into caspase-2 protein substrate recognition and catalysis
    Yinyan Tang
    Department of Pharmaceutical Chemistry, Small Molecule Discovery Center, University of California, San Francisco, California 94158, USA
    J Biol Chem 286:34147-54. 2011
    ..These findings broaden our understanding of caspase-2 substrate specificity and catalysis...
  15. pmc p97 Disease Mutations Modulate Nucleotide-Induced Conformation to Alter Protein-Protein Interactions
    Stacie L Bulfer
    Department of Pharmaceutical Chemistry, Small Molecule Discovery Center, University of California, San Francisco, California 94143, United States
    ACS Chem Biol 11:2112-6. 2016
    ..However, MSP1 mutants lose this nucleotide-induced conformational coupling because they destabilize the ADP-bound, "down" conformation of the N-domain. Loss in conformation coupling to PPIs could contribute to the mechanism of MSP1. ..
  16. ncbi request reprint Identification of Inhibitors of the Association of ZAP-70 with the T Cell Receptor by High-Throughput Screen
    Patrick R Visperas
    Department of Molecular and Cell Biology and Department of Chemistry, California Institute of Quantitative Biosciences and Howard Hughes Medical Institute, University of California, Berkeley, CA, USA
    J Biomol Screen . 2016
    ..The screen is based on a fluorescence polarization assay for peptide binding to ZAP-70...
  17. doi request reprint A Fragment-Based Ligand Screen Against Part of a Large Protein Machine: The ND1 Domains of the AAA+ ATPase p97/VCP
    Michael S Chimenti
    Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA, USA Co first authors
    J Biomol Screen 20:788-800. 2015
    ..The combination of virtual screening, SPR, and NMR enabled us to find and validate a number of interesting fragment hits and allowed us to gain an understanding of the structural nature of fragment binding. ..
  18. pmc A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver
    Miyuki Suzawa
    Department of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, United States
    elife 4:. 2015
    ..Our findings underscore the benefits of phenotypic screening for targeting post-translational modifications, and illustrate the potential utility of TA for probing the cellular consequences of sumoylation. ..
  19. pmc Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease
    Juan C Engel
    Sandler Center for Basic Research in Parasitic Diseases and Department of Pathology, University of California, San Francisco, UCSF MC 2550, Room 501E, 1700 4th St, San Francisco, CA 94158 2330, USA
    Antimicrob Agents Chemother 54:3326-34. 2010
    ..This high-throughput assay will have an important impact in antiparasitic drug discovery...
  20. pmc A high-throughput drug screen for Entamoeba histolytica identifies a new lead and target
    Anjan Debnath
    Sandler Center for Drug Discovery, University of California San Francisco, San Francisco, California, USA
    Nat Med 18:956-60. 2012
    ..This new use of auranofin represents a promising therapy for amebiasis, and the drug has been granted orphan-drug status from the FDA...
  21. pmc A high-throughput functional screen identifies small molecule regulators of temperature- and mechano-sensitive K2P channels
    Sviatoslav N Bagriantsev
    Cardiovascular Research Institute, University of California, San Francisco, California 94158, United States
    ACS Chem Biol 8:1841-51. 2013
    ..The new K2P modulators presented here, together with the yeast-based assay, should enable both mechanistic and physiological studies of K2P activity and facilitate the discovery and development of other K2P small molecule modulators. ..

Research Grants1

  1. 2008 Biomolecular Interactions and Methods Gordon Research Conference
    Michelle Arkin; Fiscal Year: 2008
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