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- W4377029257 abstract "<b>Abstract ID 52134</b> <b>Poster Board 154</b> 3′,5′-cyclic monophosphate (cAMP)–dependent protein kinase A (PKA) dysfunction underlies a number of human diseases, including a recently identified rare gene fusion which acts as an oncogene for fibrolamellar hepatocellular carcinoma (FLHCC). These important disease associations have led to a renaissance in drug development interest targeting this kinase. We therefore have established a suite of biochemical, cell-based, and structural biology assays for identifying and evaluating new pharmacophores for PKA inhibition. This discovery process entails a 384-well high throughput screen of more than 300,000 substances, focusing on fractionated natural product extracts. Validated active compounds were subsequently characterized using biochemical, biophysical, and cell-based assays. This detailed assessment identified several previously unrecognized PKA pharmacophores and led to the generation of new x-ray crystallography structures demonstrating unique interactions between PKA and bound inhibitor molecules. This research was supported in whole or in part with Federal Funds from National Cancer Institute, Center for Cancer Research, National Institutes of Health, Department of Health and Human Services, Intramural Program, under project number ZIA BC 011744 (P.Z.), contract number 75N91019D00024 (M.D., E.A.S., and A.W.), the Cancer Moonshot Program- NCI Program for Natural Product Discovery (ZIA BC 011854 (B.R.O.)), Cell-free assay technologies for the identification of active compounds (ZIA BC 011471, (B.R.O.)), and Assay development and screening for molecular targets and discovery (ZIA BC 011904 (B.R.O.))." @default.
- W4377029257 created "2023-05-19" @default.
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- W4377029257 date "2023-05-18" @default.
- W4377029257 modified "2023-09-29" @default.
- W4377029257 title "Natural Products as a Source of Chemical Diversity in cyclic-AMP dependent Protein Kinase A (PKA) Inhibitor Discovery" @default.
- W4377029257 doi "https://doi.org/10.1124/jpet.122.521340" @default.
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