3d0b

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3d0b, resolution 1.74Å ()
Ligands:
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

Crystal Structure of Benzamide Tetrahydro-4H-carbazol-4-one bound to Hsp90

Publication Abstract from PubMed

Hsp90 maintains the conformational stability of multiple proteins implicated in oncogenesis and has emerged as a target for chemotherapy. We report here the discovery of a novel small molecule scaffold that inhibits Hsp90. X-ray data show that the scaffold binds competitively at the ATP site on Hsp90. Cellular proliferation and client assays demonstrate that members of the series are able to inhibit Hsp90 at nanomolar concentrations.

Discovery of benzamide tetrahydro-4H-carbazol-4-ones as novel small molecule inhibitors of Hsp90., Barta TE, Veal JM, Rice JW, Partridge JM, Fadden RP, Ma W, Jenks M, Geng L, Hanson GJ, Huang KH, Barabasz AF, Foley BE, Otto J, Hall SE, Bioorg Med Chem Lett. 2008 Jun 15;18(12):3517-21. Epub 2008 May 9. PMID:18511277

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

3d0b is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Barta TE, Veal JM, Rice JW, Partridge JM, Fadden RP, Ma W, Jenks M, Geng L, Hanson GJ, Huang KH, Barabasz AF, Foley BE, Otto J, Hall SE. Discovery of benzamide tetrahydro-4H-carbazol-4-ones as novel small molecule inhibitors of Hsp90. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3517-21. Epub 2008 May 9. PMID:18511277 doi:10.1016/j.bmcl.2008.05.023

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