The mechanism of interaction between globin and GRK1.

GPCR (G protein concatenation recepor) has become one of the most successful drug targets, so far about 40% of the listed drugs to GPCR as the target, therefore, in the field of drug discovery, the more understanding and understanding of the GPCR structure and how to interact with downstream signaling path, the more promising it is to develop more efficient and low-toxic drugs.
Since the successful analysis of GPCR and downstream G protein and inhibitor protein complex crystal structure, another outstanding problem in the field of GPCR signal transdation, namely, how GPCR interacts with GRK (G protein contric receptamination kinase), has been bothering biological and pharmacologists.
Xu Huaqiang of the Shanghai Institute of Pharmaceutical Research of the Chinese Academy of Sciences solved the key problem of how activated visual erythropopopolytin interacts with GRK and phosphorylation, which in turn leads to rapid inactivation of downstream signaling paths.
The team found that the interaction between visual hemoglobin and retinoprotein kinase I (GRK1) was mediated by GRK1's regulatory G protein signal homogeneity region (RH region), and that the kinase region requiring GRK1 was active.
The Q41L function-obtained mutation on the corresponding RH region of kinase 5 (GRK5) promotes receptural desensitization by enhancing the interaction and phosphorylation of the receptacle with GRK, and eventually reconstructs the three-dimensional structure of the visual purple hemoglobin/kinase complex by electro-mirror negative dyeing technology.
, this part of the work identifies the key parts of the interaction between visual hemoglobin and GRK1, which provides a new way of thinking for further understanding the GCR desensitism of kinase mediated.
the study was published online May 27 in cell research, an international academic journal.
article was written by Yin Yanxuan, Ph.D. student in Xu Huaqiang's research group, Hou Li, an assistant researcher, and He Yuanzheng, Ph.D., Ofan Lo Research Institute in the United States.
the research work has been the national "973" topic, the national new drug creation of major special projects, the Chinese Academy of Sciences strategic pilot science and technology special (class B), as well as the United States NIH Fund project and the United States Wen'anlo Fund project and other strong support.
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