磺胺
碳酸酐酶
作用机理
临床试验
药理学
药代动力学
医学
癌症
酶
化学
癌症研究
生物
内科学
体外
生物化学
立体化学
标识
DOI:10.1517/13543784.12.2.283
摘要
AbstractIndisulam (N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide, E7070) is a novel sulfonamide anticancer agent in clinical development for the treatment of solid tumours. Its mechanism of action is multifactorial, as indisulam arrests cell cycle in the G1 phase, strongly inhibits carbonic anhydrase, a critical enzyme involved in many physiological processes and whose association with cancer became obvious in the last period, and markedly alters gene expression levels of at least 60 transcripts. Four Phase I clinical trials gave promising results, showing the compound to possess nonlinear pharmacokinetics. Presently this compound is in Phase II trials in Europe and USA for the treatment of solid tumours.Keywordsanticancer agentcarbonic anhydrase inhibitorcell-cycle arrestG1 phasesulfonamide
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