期刊
BIOORGANIC CHEMISTRY
卷 126, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2022.105920
关键词
Cancer; Carbonic anhydrase inhibitors; Tail-approach; hCA IX; hCA XII; Selective inhibitors; Potent inhibitors; SLC-0111
资金
- Council of Scientific and Industrial Research, New Delhi, India
- Italian Ministry for Education and Science (MIUR) [PRIN: rot. 2017XYBP2R]
- Ente Cassa di Risparmio di Firenze (ECRF) [CRF2020.1395]
This study reviews the research in the past decade (2010-2020) focusing on the selective and potent inhibitors of tumor-associated isoforms hCA IX and hCA XII. The tail-approach has been identified as a promising method for designing selective inhibitors.
Human carbonic anhydrase (hCA) isoforms hCA IX and hCA XII are well established anticancer drug targets and their selective inhibition is highly desired for the proper treatment of cancer. Lack of isoform-selectivity in current clinically used CA inhibitors (CAIs) is a major concern as it leads to undesired side effects, associated with off-target inhibition. Thus, there is need to explore alternative approaches for the design of isoform-selective inhibitors and the leading promising approach for the design of isoform-selective CAIs is the tail-approach. Virtually, most drug design studies in the last decade were done by considering the tail-approach reported in 1999. The past decade of 2010-2020 witnessed progressive maturation of this approach as a large number of CAIs have been designed and synthesised based on it, many of which turned out to be effective as well as selective hCA IX and hCA XII inhibitors. This review covers the past decade (2010-2020) research, considering selective as well as potent inhibitors of tumor associated isoforms, hCA IX and hCA XII, which include newer generation inhibitors containing sulfonamides or their bioisosteres, non-classical inhibitors (including carboxylic acid/ester, coumarin and sulfocoumarin classes) and various other novel classes of inhibitors belonging to newly identified chemotypes/scaffolds.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据