We describe a novel method for predicting G-protein coupled receptor (GPCR) G-protein coupling selectivity using amino acid properties of specific residues in GPCR sequences. We have evaluated various amino acid properties obtained with experimental or theoretical studies. The GPCRs having reliable G-protein binding information were collected from Guide to Receptors and Channels (GRAC) and gpDB...

G protein-coupled receptors (GPCRs) constitute a large family of receptors that sense molecules outside the cell and activate inside signal transduction pathways and cellular responses. GPCR are involved in a wide variety of physiological processes, including in the neuroendocrine system. GPCR are also involved in many diseases and are the target of 30% of marketed medicinal drugs. Whereas the ...

Purpose: Epidermal growth factor receptor (EGFR) overexpression is correlated with decreased survival in head and neck cancer (HNC) where the addition of EGFR inhibition to standard chemoradiation approaches has improved treatment responses. However, the basis for the limited efficacy of EGFR inhibitors in HNC is incompletely understood. G-protein–coupled receptors (GPCR) have been shown to be ...

G protein-coupled receptors (GPCRs) play crucial roles in cell physiology and pathophysiology. There is increasing interest in using structural information for virtual screening (VS) of libraries and for structure-based drug design to identify novel agonist or antagonist leads. However, the sparse availability of experimentally determined GPCR/ligand complex structures with diverse ligands impe...

ABSTRACT Animal steroid hormones initiate signaling by passive diffusion into cells and binding to their nuclear receptors regulate gene expression. can via G protein-coupled (GPCRs); however, the underlying mechanisms are unclear. Here, we show that a newly discovered ecdysone-responsive GPCR, ErGPCR-3, transmits hormone 20-hydroxyecdysone (20E) signal 20E promoting its entry in lepidopteran i...

G protein-coupled receptors (GPCRs) comprise the largest family of membrane receptors that control many cellular processes and consequently often serve as drug targets. These receptors undergo a strict regulation by mechanisms such as internalization and desensitization, which are strongly influenced by posttranslational modifications. Ubiquitination is a posttranslational modification with a b...