Research Topics
Genomes and GenesSpecies | Michelle ArkinSummaryAffiliation: Sunesis Pharmaceuticals Country: USA Publications
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Detail Information
Publications
Binding of small molecules to an adaptive protein-protein interfaceMichelle R Arkin
Department of Biology, Sunesis Pharmaceuticals, South San Francisco, CA 94080 1913, USA
Proc Natl Acad Sci U S A 100:1603-8. 2003..Thus, the adaptive nature of a protein-protein interface provides sites for small molecules to bind and underscores the challenge of applying structure-based design strategies that cannot accurately predict a dynamic protein surface...
Small-molecule inhibitors of protein-protein interactions: progressing towards the dreamMichelle R Arkin
Sunesis Pharmaceuticals, 341 Oyster Point Boulevard, South San Francisco, California 94080, USA
Nat Rev Drug Discov 3:301-17. 2004
Protein-protein interactions and cancer: small molecules going in for the killMichelle Arkin
Sunesis Pharmaceuticals, 341 Oyster Point Blvd, South San Francisco, California 94080, USA
Curr Opin Chem Biol 9:317-24. 2005..Not only is the list of protein-protein inhibitors growing, but the inhibitors themselves are moving closer to treating disease...
Discovery of a potent small molecule IL-2 inhibitor through fragment assemblyAndrew C Braisted
Sunesis Pharmaceuticals, 341 Oyster Point Boulevard, South San Francisco, California 94080, USA
J Am Chem Soc 125:3714-5. 2003..This method of coupling selected fragments with a low micromolar hit shows great potential for generating high-affinity lead compounds...
Discovery and characterization of cooperative ligand binding in the adaptive region of interleukin-2Jennifer Hyde
Sunesis Pharmaceuticals, 341 Oyster Point Boulevard, South San Francisco, California 94080, USA
Biochemistry 42:6475-83. 2003..The tethering approach provides a novel and general strategy for discovering such cooperative binding interactions in specific, flexible regions of protein structure...
Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein interactionsBrian C Raimundo
Sunesis Pharmaceuticals Inc, 341 Oyster Point Boulevard, South San Francisco, CA 94080, USA
J Med Chem 47:3111-30. 2004..Throughout the discovery process, biophysical methods and structural biology demonstrated that compounds bound reversibly to IL-2 at the IL-2 receptor binding site...
Identification of nonpeptidic small-molecule inhibitors of interleukin-2Nathan D Waal
Sunesis Pharmaceuticals, Inc, 341 Oyster Point Boulevard, South San Francisco, CA 94080, USA
Bioorg Med Chem Lett 15:983-7. 2005..Installation of a furan carboxylic acid fragment onto a low-micromolar sulfamide resulted in a 23-fold improvement in activity, providing a sub-micromolar, nonpeptidic IL-2 inhibitor (IC(50)=0.60 microM)...
