NDLI: Subtleties in GPCR drug discovery: a medicinal chemistry perspective.

Content Provider	Semantic Scholar
Author	Fujioka, Masahiko Omori, Naoki
Copyright Year	2012
Abstract	Therapeutic effects through G protein-coupled receptors (GPCRs) are promoted by a full agonist, partial agonist, neutral antagonist or inverse agonist. Dramatic change of function such as from a neutral antagonist to a full agonist with minimal variation of ligand structure is a phenomenon that medicinal chemists often encounter. This is also influenced by a change of assay format. The subtle nature of structure-function relationships is difficult to grasp unless carefully considered from both chemistry and assay perspectives. In this article we discuss the subtle aspects of GPCR drug discovery from the medicinal chemistry perspective.
File Format	PDF HTM / HTML
DOI	10.1016/j.drudis.2012.06.010
PubMed reference number	22732182
Journal	Medline
Volume Number	17
Issue Number	19-20
Alternate Webpage(s)	http://csmres.co.uk/cs.public.upd/article-downloads/Fujioka_2012_Drug-Discovery-Today.pdf
Alternate Webpage(s)	https://doi.org/10.1016/j.drudis.2012.06.010
Journal	Drug discovery today
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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