Chinese Academy of Sciences discovers a new mechanism for interaction between GPCR and GPCR kinase
China Pharmaceutical Science & Technology [Network] GPCR (G Protein-Coupled Receptor G protein-coupled receptor), which is important in cell signaling proteins, topological conformation seven transmembrane receptor. GPCR is one of the target enzymes. A total of about 500 have been identified as therapeutic drug targets to date, and G-protein coupled receptor (GPCR) targets account for the vast majority of receptors.
GPCR (G-protein coupled receptor) has become one of the most successful drug targets. To date, about 40% of marketed drugs have been targeted by GPCRs. Therefore, in the field of drug discovery, the structure of GPCRs and how they are downstream The deeper the understanding and understanding of signal pathway interactions, the more promising it is to develop more efficient and less toxic drugs. Since the successful analysis of the crystal structure of GPCR and downstream G protein and repressor complexes, another important issue in the field of GPCR signal transduction is how GPCR interacts with GRK (G protein coupled receptor kinase) to cause GPCR Min has been plagued by biological and pharmacologists.
Xu Huaqiang, research group of Shanghai Institute of Materia Medica, Chinese Academy of Sciences, studied the classical GPCR, Rhodopsin, and solved how the activated rhodopsin protein is phosphorylated by interaction with GRK, which triggers downstream signals. The key issue of rapid deactivation of the pathway. The team found that the interaction of rhodopsin with rhodopsin kinase I (GRK1) is mediated by the regulatory G protein signaling homology region (RH region) of GRK1, and that the kinase region of GRK1 is required to be active. The Q41L function-acquired mutation in the corresponding RH region of kinase 5 (GRK5) promotes receptor desensitization by enhancing receptor interaction and phosphorylation with GRK, and finally reconstructs rhodopsin by electron microscopy. The three-dimensional structure of the kinase complex. In summary, this part of the work identified a key part of the interaction between rhodopsin and GRK1, providing a new idea for further understanding of kinase-mediated GPCR desensitization. The research was published online May 27 in the international academic journal Cell Research.
The article was jointly completed by Xu Yanqiang, Ph.D. student of Xu Huaqiang, assistant researcher Hou Li, and Dr. He Yuanzheng, Ph.D. The research work has received strong support from the national “973†project, the national special drug creation special project, the Chinese Academy of Sciences strategic pilot science and technology project (category B), the US NIH fund project and the US Wen'an Luo fund project.
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GPCR (G-protein coupled receptor) has become one of the most successful drug targets. To date, about 40% of marketed drugs have been targeted by GPCRs. Therefore, in the field of drug discovery, the structure of GPCRs and how they are downstream The deeper the understanding and understanding of signal pathway interactions, the more promising it is to develop more efficient and less toxic drugs. Since the successful analysis of the crystal structure of GPCR and downstream G protein and repressor complexes, another important issue in the field of GPCR signal transduction is how GPCR interacts with GRK (G protein coupled receptor kinase) to cause GPCR Min has been plagued by biological and pharmacologists.
Xu Huaqiang, research group of Shanghai Institute of Materia Medica, Chinese Academy of Sciences, studied the classical GPCR, Rhodopsin, and solved how the activated rhodopsin protein is phosphorylated by interaction with GRK, which triggers downstream signals. The key issue of rapid deactivation of the pathway. The team found that the interaction of rhodopsin with rhodopsin kinase I (GRK1) is mediated by the regulatory G protein signaling homology region (RH region) of GRK1, and that the kinase region of GRK1 is required to be active. The Q41L function-acquired mutation in the corresponding RH region of kinase 5 (GRK5) promotes receptor desensitization by enhancing receptor interaction and phosphorylation with GRK, and finally reconstructs rhodopsin by electron microscopy. The three-dimensional structure of the kinase complex. In summary, this part of the work identified a key part of the interaction between rhodopsin and GRK1, providing a new idea for further understanding of kinase-mediated GPCR desensitization. The research was published online May 27 in the international academic journal Cell Research.
The article was jointly completed by Xu Yanqiang, Ph.D. student of Xu Huaqiang, assistant researcher Hou Li, and Dr. He Yuanzheng, Ph.D. The research work has received strong support from the national “973†project, the national special drug creation special project, the Chinese Academy of Sciences strategic pilot science and technology project (category B), the US NIH fund project and the US Wen'an Luo fund project.
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