Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.

doi:10.1021/acs.jmedchem.7b00385

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Article

Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.

Journal of medicinal chemistry - 27 Jul 2017

Carpenter Joseph, Wang Ying, Wu Gang, Feng Jianxin, Ye Xiang-Yang, Morales Christian L, Broekema Matthias, Rossi Karen A, Miller Keith J, Murphy Brian J, Wu Ginger, Malmstrom Sarah E, Azzara Anthony V, Sher Philip M, Fevig John M, Alt Andrew, Bertekap Robert L, Cullen Mary Jane, Harper Timothy M, Foster Kimberly, Luk Emily, Xiang Qian, Grubb Mary F, Robl Jeffrey A, Wacker Dean A

Abstract excerpt

Agonism of the 5-HT2C receptor represents one of the most well-studied and clinically proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been shown to lead to undesirable side effects and major safety concerns. In this communication, we report the development of a new screening paradigm that utilizes an...

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PMID: 28635286
DOI: 10.1021/acs.jmedchem.7b00385

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