[4] Zhang B, Xue L, Wu Z B. Structure and function of somatostatin and its receptors in endocrinology. Endocr Rev, 2025, 46(1): 26-42 [5] Lee J, Gonzalez-Hernandez A J, Kristt M, et al. Distinct beta-arrestin coupling and intracellular trafficking of metabotropic glutamate receptor h...
et al. G protein-coupled receptors: structure- and function-based drug discovery. Sig Transduct Target Ther 6, 7 (2021). https://doi.org/10.1038/s41392-020-00435-w [5].https://www.fda.gov [6].Zhang, R., Xie, X. Tools for GPCR drug discovery. Acta Pharmacol Sin 33, 372–384 ...
GPCR structure and function relationship: identification of a biased apelin receptor mutantapelin receptorG protein-coupled receptorsmolecular dynamicspharmacologysignaling biasBiased ligands of G protein-coupled receptors (GPCRs) may have improved therapeutic benefits and safety profiles. However, the ...
GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1-2 September 2014. Naunyn Schmiedebergs Arch Pharmacol. 2015; 388: 883-903.Heifetz A, Schertler GF, Seifert R, Tate CG, Sexton PM, Gurevich VV...
Fig1. Structure of GPCR 图1.GPCR的结构[1] 1.2 GPCR的种类和功能 迄今已鉴定出900多个人类相关的GPCRs[2]。GPCRs的分类依据序列以及结构相似性,主要分为以下5个主要家族:视紫红质受体(A类),分泌素受体(B1类),黏附受体(B2类),谷氨酸盐受体(C类)和卷曲/味觉2(F类)[1]。
5.Yang, D., et al., Yang, D., et al., G protein-coupled receptors: structure-and function-based drug discovery. Signal transduction and targeted therapy, 2021. 6(1): p. 7. 6.Buck, A.K., et al., Buck, A.K., et al., CXCR4-targeted theranostics in oncology. Eur J Nucl Med...
[12] HU, Zhong-ping, et al. "Research Progress on Structure and Function of GLP-1R and Screening for Small Molecule Drugs." Biotechnology Bulletin 33.2 (2017): 30. [13] Meurot, C., et al. "Targeting the GLP-1/GLP-1R axis to treat osteoarthritis: A new opportunity?." Journal of ...
Crystal structure of the β2 adrenergic receptor–Gs protein complex. Nature 477, 549–555 (2011). Article CAS PubMed PubMed Central ADS Google Scholar Rosenbaum, D. M. et al. GPCR engineering yields high-resolution structural insights into β2-adrenergic receptor function. Science 318, 1266...
G proteins can also functionally engage with GPCRs through an extrahelical mode of interaction. It is increasingly clear that understanding of the selectivity and dynamics of G protein binding and activation will need to continually evolve to accommodate the revelations from high-resolution structure ...
1. Rosenbaum, D. M., Rasmussen, S. G. & Kobilka, B. K. The structure and function of G-protein-coupled receptors. Nature 459, 356–363 (2009). 2. Gurevich, V. V. & Gurevich, E. V. GPCR signaling regulation: the role of GRKs and arrestins. Front. Pharmacol. 10, 125 (2019...