G protein-coupled receptors (GPCRs) constitute the largest single class of receptors and are responsible for mediating much of intracellular mammalian signaling. Indeed, over 40 percent of the pharmacological targets being evaluated by drug companies are related to G protein-coupled receptors. ...
G protein‐coupled receptorgenetic variationoral sensationIn humans, the 25 bitter taste receptors (T2Rs) are activated by hundreds of structurally diverse bitter compounds. However, only 5 antagonists or bitter blockers are known. In this study, using molecular modeling guided site-directed ...
alterations of these receptors in diseases, causes of these alterations, and their relations with the development of diseases are studied only in few cases. This review considers some mechanisms of regulation of activity and expression of G-protein-coupled receptors (GPCRs) that comprise the largest...
G protein-coupled receptors (GPCRs) are transmembrane proteins that participate in many physiological processes and represent major pharmacological targets. Recent advances in structural biology of GPCRs have enabled the development of drugs based on the receptor structure (structure-based drug design, SB...
The past decade has seen tremendous advances in the study of G protein-coupled receptors (GPCRs), including the molecular cloning and identification of more than 100 hundred GPCR genes. But while GPCRs serve as targets for more than 300 medicines in the modern pharmacopoeia, the shrinking pool...
G protein-coupled receptors and their effectors can now be released directly from a lipid bilayer using infrared irradiation for proteoform-level characterization by native top-down mass spectrometry. This represents a critical development for drug discovery, as the direct role of post-translational modi...
一个激素分子与受体蛋白的结合,导致数百个G变成GTP结合型,这就是信号放大。由于它们用G蛋白传递信号,7TM受体常称为G-蛋白偶联受体(G-protein-coupled receptors, GPCRs)。 图14.7腺苷酸环化酶活化。(A)腺苷酸环化酶是膜蛋白,胞内结构域大,有催化活性。(B)与GTP结合的G,能够与腺苷酸环化酶催化结构域结合...
Bitter taste receptors (TAS2Rs) are a subfamily of G-protein coupled receptors (GPCRs). Here, the authors report a cryo-EM structure of the human TAS2R14 in complex with its signaling partner gustducin, and bound to an anti-inflammatory drug flufenamic acid (FFA). Lior Peri Donna Matzo...
The large superfamily of G-protein-coupled receptors (GPCRs) comprises important targets for many (>30%) marketed drugs. Biochemical knowledge on the adhesion-GPCR subfamily is yet in its infancy compared to our understanding of many of the well-studied GPCR drug targets. Adhesion-GPCRs mediate...
Function-based high-throughput screening for antibody antagonists and agonists against G protein-coupled receptors Commun. Biol, 3 (2020), p. 146 10.1038/s42003-020-0867-7 32218528 Google Scholar 26 R.H. Reader, R.G. Workman, B.C. Maddison, K.C. Gough Advances in the production and batc...