Allosteric Modulators: A Side Door

Allosteric modulators of the cannabinoid CB1 receptor were first discovered in 2005. Since then, although both negative and positive allosteric modulators have been uncovered, many questions remain about their site(s) of action, as well as the basis of their signaling. The described covalent probe w...

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Veröffentlicht in:	Journal of medicinal chemistry 2016-01, Vol.59 (1), p.42-43
1. Verfasser:	Abood, Mary E
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation - drug effects Allosteric Site - drug effects Humans Molecular Conformation Receptor, Cannabinoid, CB1 - chemistry Receptor, Cannabinoid, CB1 - drug effects Structure-Activity Relationship
Online-Zugang:	Volltext
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Zusammenfassung:	Allosteric modulators of the cannabinoid CB1 receptor were first discovered in 2005. Since then, although both negative and positive allosteric modulators have been uncovered, many questions remain about their site(s) of action, as well as the basis of their signaling. The described covalent probe with improved potency and efficacy will facilitate these studies.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/acs.jmedchem.5b01824