Matches in SemOpenAlex for { <https://semopenalex.org/work/W2022341112> ?p ?o ?g. }
- W2022341112 endingPage "315" @default.
- W2022341112 startingPage "292" @default.
- W2022341112 abstract "Rhodopsin-like (class A) G protein-coupled receptors (GPCRs) are one of the most important classes of drug targets. The discovery that these GPCRs can be allosterically modulated by small drug molecules has opened up new opportunities in drug development. It will allow the drugability of “difficult targets”, such as GPCRs activated by large (glyco)proteins, or by very polar or highly lipophilic physiological agonists. Receptor subtype selectivity should be more easily achievable with allosteric than with orthosteric ligands. Allosteric modulation will allow a broad spectrum of pharmacological effects largely expanding that of orthosteric ligands. Furthermore, allosteric modulators may show an improved safety profile as compared to orthosteric ligands. Only recently, the explicit search for allosteric modulators has been started for only a few rhodopsin-like GPCRs. The first negative allosteric modulators (allosteric antagonists) of chemokine receptors, maraviroc (CCR5 receptor), used in HIV therapy, and plerixafor (CXCR4 receptor) for stem cell mobilization, have been approved as drugs. The development of allosteric modulators for rhodopsin-like GPCRs as novel drugs is still at an early stage; it appears highly promising." @default.
- W2022341112 created "2016-06-24" @default.
- W2022341112 creator A5000284275 @default.
- W2022341112 creator A5017915434 @default.
- W2022341112 creator A5029319508 @default.
- W2022341112 date "2012-09-01" @default.
- W2022341112 modified "2023-10-16" @default.
- W2022341112 title "Allosteric modulators of rhodopsin-like G protein-coupled receptors: Opportunities in drug development" @default.
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