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Application of an Integrated GPCR SAR-Modelling Platform to Explain the Activation Selectivity of Human 5-HT2C over 5-HT2B

Abstract:

Agonism of the 5-HT2C serotonin receptor has been associated with the treatment of a number of diseases including obesity, psychiatric disorders, sexual health and urology. However, the development of effective 5-HT2C agonists has been hampered by the difficulty in obtaining selectivity over the closely related 5-HT2B receptor, agonism of which is associated with irreversible cardiac valvulopathy. Understanding how to design selective agonists requires exploration of the structural features g...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acschembio.5b01045

Authors


Publisher:
American Chemical Society
Journal:
ACS Chemical Biology More from this journal
Volume:
11
Issue:
5
Pages:
1372–1382
Publication date:
2016-02-22
Acceptance date:
2016-02-22
DOI:
EISSN:
1554-8937
ISSN:
1554-8929
Language:
English
Keywords:
Pubs id:
pubs:605950
UUID:
uuid:718128d8-2433-468b-92e6-82fadfc5d67d
Local pid:
info:fedora/pubs:605950
Source identifiers:
605950
Deposit date:
2016-03-14

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