一类新型3,4-二芳基吡唑类Hsp90抑制剂的鉴定、合成、蛋白质晶体结构及体外生化评价
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
作者信息
Cheung Kwai-Ming J, Matthews Thomas P, James Karen, Rowlands Martin G, Boxall Katherine J, Sharp Swee Y, Maloney Alison, Roe S Mark, Prodromou Chrisostomos, Pearl Laurence H, Aherne G Wynne, McDonald Edward, Workman Paul
机构信息
Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK and Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK.
出版信息
Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43. doi: 10.1016/j.bmcl.2005.05.046.
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.
高通量筛选确定3,4 - 二芳基吡唑CCT018159是一种新型且强效的（7.1微摩尔）热休克蛋白90（Hsp90）ATP酶活性抑制剂。在此，我们描述了CCT018159及其一些紧密类似物的合成，以及它们的生化特性数据。讨论了一些初步的构效关系，以及CCT018159与Hsp90结合的晶体结构。
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