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33645015129
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note
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The values obtained for the ATPase and the FP assay differ between compounds as they measure different aspects of compound activities. The ATPase assay measures a compound's ability to inhibit ATPase functionality of yeast Hsp90. In comparison, the FP assay measures the ability of a compound to compete with a small molecule for binding to human Hsp90. Therefore, some compounds may compete for binding to Hsp90 with this small molecule poorly due to their kinetic properties (e.g., fast-on, fast-off) but may still retain the ability to inhibit the ATPase activity.
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17
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3042637928
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L. Wright, X. Barril, B. Dymock, L. Sheridan, A. Surgenor, M. Beswick, M. Drysdale, A. Collier, A. Massey, N. Davies, A. Fink, C. Fromont, W. Aherne, K. Boxall, S. Sharp, P. Workman, and R.E. Hubbard Chem. Biol. 11 2004 775
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Collier, A.8
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Davies, N.10
Fink, A.11
Fromont, C.12
Aherne, W.13
Boxall, K.14
Sharp, S.15
Workman, P.16
Hubbard, R.E.17
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18
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33644995102
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note
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3 and alkyl halide. Regioisomers were separated by preparative HPLC-MS and regiochemistry was determined by NOE spectroscopy.
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19
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84893169025
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Montgomery, J.A.13
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21
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33645012275
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Atomic coordinates have been deposited with the Protein Data Bank at Rutgers University (http://rscb.rutgers.edu/pdb/index.html). PDB id codes for 2, 6 and 17 co-crystallised with Hsp90 are 2CCS, 2CCU and 2CCT, respectively.
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