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Allosteric Regulation: Mechanism Study and Applications in Drug Discovery
Wang Chengxiang, Zhang Jian*
Key Laboratory of Cell Differentiation and Apoptosis of Chinese Ministry of Education,Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China
Abstract: Allosteric regulation is that allosteric modulator binds at an allosteric site， a site distinct from the orthosteric site， inducing the change in conformation of protein to regulate its function activity. Allosteric regulation has many advantages due to specific features of allosteric sites， including structural diversity and flexibility. Then allosteric modulators show high selectivity， low toxicity and a ceiling effect on target， which presents a novel approach to drug discovery. In addition， allosteric modulator is able to trigger the communication between their binding allosteric site and corresponding functional site， as well as act in synergy with cofactors or endogenous ligands. This review focuses on the history， mechanism， methods of allostery， the progress of allosteric modulators and the outlook of allosteric drugs in drug discovery.
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