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• W2789732017 abstract "Overproduction of cortisol by the hypothalamus-pituitary-adrenal hormone system results in the clinical disorder known as Cushing's syndrome. Genomics studies have identified a key mutation (L205R) in the α-isoform of the catalytic subunit of cAMP-dependent protein kinase (PKACα) in adrenal adenomas of patients with adrenocorticotropic hormone-independent Cushing's syndrome. Here, we conducted kinetics and inhibition studies on the L205R-PKACα mutant. We have found that the L205R mutation affects the kinetics of both Kemptide and ATP as substrates, decreasing the catalytic efficiency (kcat/KM) for each substrate by 12-fold and 4.5-fold, respectively. We have also determined the IC 50 and Ki for the peptide substrate-competitive inhibitor PKI(5-24) and the ATP-competitive inhibitor H89. The L205R mutation had no effect on the potency of H89, but causes a > 250-fold loss in potency for PKI(5-24). Collectively, these data provide insights for the development of L205R-PKACα inhibitors as potential therapeutics." @default.
• W2789732017 created "2018-03-29" @default.
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• W2789732017 date "2018-03-11" @default.
• W2789732017 modified "2023-09-23" @default.
• W2789732017 title "Kinetics and inhibition studies of the L205R mutant of<scp>cAMP</scp>‐dependent protein kinase involved in Cushing's syndrome" @default.
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• W2789732017 doi "https://doi.org/10.1002/2211-5463.12396" @default.
• W2789732017 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5881547" @default.
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