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| | Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1 |
| Description: | University of New Mexico Assay Overview: Assay Support: 1 R03 DA030557-01A1 Project Title: RNA Aptamer-based screen for Selective Inhibitors of GRK2 PI: John Tesmer Assay Implementation: Jun Chen, Pete Simons, Stephanie Chavez, Dominique Perez, Matthew Garcia, Terry Foutz, Anna Waller, Annette Evangelisti, J. Jacob Strouse, Mark Carter, Cristian Bologa, Gergely Zahoransky-Kohalmi Screening Cener PI: Larry Sklar UNMCMD Chemistry Center PI: Craig Lindsley Vanderbilt Specialized Screening Center Assay Background and Significance: A small family of G protein-coupled receptor (GPCR) kinases (GRKs) negatively regulates heterotrimeric G protein signaling by phosphorylating multiple sites in the cytoplasmic loops and tails of activated GPCRs [Krupnick, et al. 1998]. Through this process, cells adapt to persistent stimuli that act at GPCRs and protect themselves from damage incurred by sustained signaling. GRKs can also play maladaptive roles in human disease. GRK2 is overexpressed |
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