Mechanisms of Aberrant PKA Activation by Cα Subunit Mutations

Horm Metab Res. 2017 Apr;49(4):307-314. doi: 10.1055/s-0042-112817. Epub 2016 Nov 3.

Abstract

Somatic mutations in PRKACA, coding for the catalytic α subunit of protein kinase A (PKA), have been recently identified as the most frequent genetic alteration in cortisol-secreting adrenocortical adenomas, which are responsible for adrenal Cushing's syndrome. The mutations identified so far lie at the interface between the catalytic (C) and regulatory (R) subunit of PKA. Detailed functional studies of the most frequent of these mutations (L206R) as well as of another one in the same region of the C subunit (199_200insW) have revealed that these mutations cause constitutive activation of PKA and lack of regulation by cAMP. This is due to interference with the binding of the R subunit, which keeps the C subunit inactive in the absence of cyclic AMP. Here, we review these recent findings, with a particular focus on the mechanisms of action of PRKACA mutations.

Publication types

  • Review

MeSH terms

  • Adrenal Cortex Neoplasms* / enzymology
  • Adrenal Cortex Neoplasms* / genetics
  • Adrenal Cortex Neoplasms* / pathology
  • Adrenocortical Adenoma* / enzymology
  • Adrenocortical Adenoma* / genetics
  • Adrenocortical Adenoma* / pathology
  • Amino Acid Substitution
  • Animals
  • Cushing Syndrome* / epidemiology
  • Cushing Syndrome* / genetics
  • Cushing Syndrome* / pathology
  • Cyclic AMP / genetics
  • Cyclic AMP / metabolism
  • Cyclic AMP-Dependent Protein Kinase Catalytic Subunits* / genetics
  • Cyclic AMP-Dependent Protein Kinase Catalytic Subunits* / metabolism
  • Enzyme Activation
  • Humans
  • Mutation, Missense*
  • Neoplasm Proteins* / genetics
  • Neoplasm Proteins* / metabolism
  • Second Messenger Systems / genetics

Substances

  • Neoplasm Proteins
  • Cyclic AMP
  • Cyclic AMP-Dependent Protein Kinase Catalytic Subunits
  • PRKACA protein, human