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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
Version:
Accepted manuscript

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Publisher copy:
10.1021/acschembio.5b01045

Authors


Heifetz, A More by this author
Storer, RI More by this author
McMurray, G More by this author
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Publisher:
American Chemical Society Publisher's website
Journal:
ACS Chemical Biology Journal website
Volume:
11
Issue:
5
Pages:
1372–1382
Publication date:
2016-02-22
Acceptance date:
2016-02-22
DOI:
EISSN:
1554-8937
ISSN:
1554-8929
URN:
pubs:718128d8-2433-468b-92e6-82fadfc5d67d
Source identifiers:
605950
Local pid:
info:fedora/pubs:605950
Language:
English
Keywords:

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