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 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
  3. 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
  4. 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
  5. 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
  6. 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
  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 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

Collaborators

  • Adam R Renslo
  • Jiri Gut
  • Juan C Engel
  • Anjan Debnath
  • Larissa M Podust
  • Philip J Rosenthal
  • James McKerrow
  • Adrian Whitty
  • Esther Orozco
  • Zachary B Mackey
  • Kenny K H Ang
  • Shamila S Gunatilleke
  • Steven Chen
  • Clifford Bryant
  • John A Flygare
  • Jonathan W Choy
  • Sviatoslav N Bagriantsev
  • Claudia M Calvet
  • Jonathan B Johnston
  • Géraldine De Muylder
  • Yinyan Tang
  • Joseline Ratnam
  • Siegfried S F Leung
  • Kean Hooi Ang
  • Alma L Burlingame
  • Daniel L Minor
  • Patricia S Doyle
  • Alejandra Gallardo-Godoy
  • Juan A Oses-Prieto
  • Jack Taunton
  • Matthew P Jacobson
  • Kimberly A Clark
  • Chiung Kuang Chen
  • Grigori Erenburg
  • Joseph Mulvaney
  • Jennifer Legac
  • Elizabeth Hansell
  • Katarzyna M Skrzypczynska
  • James A Wells
  • Linda S Brinen
  • Priyadarshini Jaishankar
  • Moumita Debnath
  • Rafaela S Ferreira
  • Dongmei Zhao
  • Iain D Kerr

Detail Information

Publications13

  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 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. ..
  3. 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...
  4. 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...
  5. 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...
  6. 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...
  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 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
    ....
  11. 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...
  12. 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. ..
  13. 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...