作者
Amol B Khade, Sidhartha S Kar, Cinu T Alummoottil, Ashutosh Tiwari, Mradul Tiwari, Vandana K Eshwara, Pritesh Bhat, Varadaraj B Giliyar, Gurupur G Shenoy
发表日期
2020/3/1
期刊
Medicinal Chemistry
卷号
16
期号
2
页码范围
256-270
出版商
Bentham Science Publishers
简介
Background
The well-known antibacterial agent Triclosan (TCL) that targets bacterial enoylacyl protein reductase has been described to inhibit human fatty acid synthase (FASN) via the enoylacyl reductase domain. A Literature survey indicates that TCL is selectively toxic to cancer cells and furthermore might indeed reduce cancer incidence in vivo. A recent study found that TCL inhibits FASN by acting as an allosteric protein-protein interface (PPI) inhibitor. It induces dimer orientation changes that effect in a downstream reorientation of catalytic residues in the NADPH binding site proposing TCL as a viable scaffold to design a superior molecule that might have more inhibitory potential. This unveils tons of potential interaction space to take advantage of future inhibitor design.
Objectives
Synthesis of TCL mimicking novel diphenyl ether derivatives, biological evaluation as potential antiproliferative agents and …
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