2bre
STRUCTURE OF A HSP90 INHIBITOR BOUND TO THE N-TERMINUS OF YEAST HSP90.
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OverviewOverview
High-throughput screening identified the 3,4-diarylpyrazole CCT018159 as a, novel and potent (7.1 microM) inhibitor of Hsp90 ATPase activity. Here, we, describe the synthesis of CCT018159 and a number of close analogues, together with data on their biochemical properties. Some initial, structure-activity relationships are discussed, as well as the crystal, structure of CCT018159 bound to Hsp90.
About this StructureAbout this Structure
2BRE is a [Single protein] structure of sequence from [Saccharomyces cerevisiae] with KJ2 as [ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
ReferenceReference
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors., Cheung KM, Matthews TP, James K, Rowlands MG, Boxall KJ, Sharp SY, Maloney A, Roe SM, Prodromou C, Pearl LH, Aherne GW, McDonald E, Workman P, Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43. PMID:15955698
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