通过吸水链霉菌基因工程获得的强效非苯醌安莎霉素热休克蛋白90抑制剂。
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
作者信息
Menzella Hugo G, Tran Thomas-Toan, Carney John R, Lau-Wee Janice, Galazzo Jorge, Reeves Christopher D, Carreras Christopher, Mukadam Sophie, Eng Sara, Zhong Ziyang, Timmermans Pieter B M W M, Murli Sumati, Ashley Gary W
机构信息
Kosan Biosciences Incorporated, 3832 Bay Center Place, Hayward, California 94545, USA.
出版信息
J Med Chem. 2009 Mar 26;52(6):1518-21. doi: 10.1021/jm900012a.
Inhibition of the protein chaperone Hsp90 is a promising new approach to cancer therapy. We describe the preparation of potent non-benzoquinone ansamycins. One of these analogues, generated by feeding 3-amino-5-chlorobenzoic acid to a genetically engineered strain of Streptomyces hygroscopicus, shows high accumulation and long residence time in tumor tissue, is well-tolerated upon intravenous dosing, and is highly efficacious in the COLO205 mouse tumor xenograft model.
抑制蛋白伴侣Hsp90是一种很有前景的癌症治疗新方法。我们描述了强效非苯醌安莎霉素的制备。通过向基因工程改造的吸水链霉菌菌株投喂3-氨基-5-氯苯甲酸产生的其中一种类似物，在肿瘤组织中显示出高积累和长停留时间，静脉给药时耐受性良好，并且在COLO205小鼠肿瘤异种移植模型中具有高效性。
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