View source for 2brc

[[Image:2brc.gif|left|200px]]<br />
<applet load="2brc" size="450" color="white" frame="true" align="right" spinBox="true" 
caption="2brc, resolution 1.60&Aring;" />
'''STRUCTURE OF A HSP90 INHIBITOR BOUND TO THE N-TERMINUS OF YEAST HSP90.'''<br />

==Overview==
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 Structure==
2BRC is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]] with CT5 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BRC OCA]]. 

==Reference==
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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15955698 15955698]
[[Category: Saccharomyces cerevisiae]]
[[Category: Single protein]]
[[Category: Pearl, L.H.]]
[[Category: Prodromou, C.]]
[[Category: Roe, S.M.]]
[[Category: CT5]]
[[Category: 3d-structure]]
[[Category: atp-binding]]
[[Category: chaperone]]
[[Category: chaperone/complex]]
[[Category: heat shock]]
[[Category: inhibitor]]
[[Category: multigene family]]

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