메뉴 건너뛰기




Volumn 16, Issue 9, 2006, Pages 2543-2548

4-Amino derivatives of the Hsp90 inhibitor CCT018159

Author keywords

Cancer; Hsp90; Pyrazole; Structure based drug design; X ray crystallography

Indexed keywords

ANSAMYCIN DERIVATIVE; CCT 018159; HEAT SHOCK PROTEIN 70; HEAT SHOCK PROTEIN 90 INHIBITOR; UNCLASSIFIED DRUG; VER 49009;

EID: 33645002986     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.01.099     Document Type: Article
Times cited : (79)

References (21)
  • 11
    • 33645015275 scopus 로고    scopus 로고
    • Preparation of pyrazoles as HSp90 inhibitors and their use as antitumor agents. Jpn Kokai Tokkyo Koho JP 2005225787, 2005.
    • Tomura, A.; Odanaka, J.; Takashio, K.; Kuramochi, H. Preparation of pyrazoles as HSp90 inhibitors and their use as antitumor agents. Jpn Kokai Tokkyo Koho JP 2005225787, 2005.
    • Tomura, A.1    Odanaka, J.2    Takashio, K.3    Kuramochi, H.4
  • 16
    • 33645015129 scopus 로고    scopus 로고
    • note
    • 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.
  • 18
    • 33644995102 scopus 로고    scopus 로고
    • note
    • 3 and alkyl halide. Regioisomers were separated by preparative HPLC-MS and regiochemistry was determined by NOE spectroscopy.
  • 21
    • 33645012275 scopus 로고    scopus 로고
    • 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.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.