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Protein expression and purification of G-protein coupled receptor kinase 6 (GRK6), toward structure-based drug design and discovery for multiple myeloma

Protein Expr Purif. 2021-05; 
Tien L Olson, Shangji Zhang, Dillon Labban, Emily Kaschner, Manuel Aceves, Srivatsan Iyer, Jose Domingo Meza-Aguilar, James D Zook, Eugene Chun, Felicia M Craciunescu, Wei Liu, Chang-Xin Shi, A Keith Stewart, Debra T Hansen, Nathalie Meurice, Petra Fromme
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Proteins, Expression, Isolation and Analysis … purification processes associated with these constructs. The GRK6 construct that did not contain any affinity purification tag had been used in protein expression and purification … S1), we used the BamHI and HindIII sites in the parent vector pFastBac1 (obtained from GenScript). … Get A Quote

Abstract

Human G-protein coupled receptor kinase 6 (GRK6) belongs to the GRK4 kinase subfamily of the G protein-coupled receptor kinase family which comprises of GRK1, GRK2, and GRK4. These kinases phosphorylate ligand-activated G-protein coupled receptors (GPCRs), driving heterotrimeric G protein coupling, desensitization of GPCR, and β-arrestin recruitment. This reaction series mediates cellular signal pathways for cell survival, proliferation, migration and chemotaxis. GRK6 is a kinase target in multiple myeloma since it is highly expressed in myeloma cells compared to epithelial cells and has a significant role in mediating the chemotactic responses of T and B-lymphocytes. To support structure-based drug design, we... More

Keywords

Crystallography, G-protein coupled receptor kinase 6, Multiple myeloma, Palmitoylation, Structure-guided drug design