GPCRs: lipid-dependent membrane receptors that act as drug targets. Adv. Biol. 2014, 143023.Chattopadhyay, A. 2014. GPCRs: lipid-dependent membrane receptors that act as drug targets. Adv. Bio. P. 2014:1-12.A. Chattopadhyay, GPCRs: Lipid-dependent membrane receptors that act as drug ...
and thus have long been attractive as drug targets. With crystal structure determinations of more than 50 different human GPCRs during the last decade, an initial platform for structure-based rational design has been established for drugs that target GPCRs, which is currently being...
GPCRs have long been targets for drug discovery research, although most successful drugs that target GPCRs were found serendipitously. The sequencing of the human genome, however, has revealed an abundance of new nonsensory receptors that could serve as therapeutic targets, and this finding has ...
GPCRs represent the largest family of genes expressed in the human genome, according to Jeremy Richman, Ph.D., associate director, cardiovascular biology, at Arena Pharmaceuticals (www.arenapharm.com). "Their cell membrane localization, the diversityof tissue expression, and the fact that they ...
1 Consequently, drugs that target multiple targets are often more effective, highlighting the importance of polypharmacology for achieving superior efficacy.2 For instance, antipsychotics such as clozapine (Clozaril) and aripiprazole (Abilify) exert their therapeutic effects by interacting with multiple G...
Only a small proportion of known GPCRs are currently targeted by therapeutics. This provides a great number of promising targets for the development of new medicines. The nuclear receptors are ligand-gated transcription factors that modulate gene expression. Membrane transporters constitute a rather ...
We also discuss current data regarding novel GPCR targets that may provide promising opportunities for drug discovery in cancer prevention and treatment.Lappano RMaggiolini MNature reviews Drug discoveryLappano R, Maggiolini M (2011). G protein-coupled receptors: novel targets for drug discovery in...
G protein-coupled receptors (GPCRs) can affect insulin action, insulin secretion and β-cell expansion, and certain GPCRs have emerged as potential drug targets for the development of anti-diabetic therapeutics. Decreased insulin sensitivity is a major metabolic defect in the great majority of indiv...
X-Ray Structure Developments for GPCR Drug Targets (Michael Sabio and Sidney W. Topiol).Sabio, M.; Topiol, S. W. X-ray Structure Developments for GPCR Drug Targets. In GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions; Gilchrist, A., Ed.; John Wiley ...
Y. (2012). Orphan G protein-coupled receptors (GPCRs): biological functions and poten- tial drug targets. Acta Pharmacol. Sin. 33, 363-371. doi: 10.1038/aps. 2011.210Tang XL, Wang Y, Li DL, Luo J, Liu MY (2012) Orphan G protein- coupled receptors (GPCRs): biological functions ...