Target intelligence / Profile preview

cAMP-dependent protein kinase type I-alpha regulatory subunit (PRKAR1A)

Target
PRKAR1A
Molecular classification
Enzyme, Regulatory subunit, Protein kinase regulatory subunit, Signal transduction protein
01

Overview

The cAMP-dependent protein kinase type I-alpha regulatory subunit (PRKAR1A) is a regulatory component of the cAMP-dependent protein kinase A (PKA) holoenzyme, itself a central mediator of cAMP signaling in cells[1][3][6]. When cAMP binds to regulatory subunits like PRKAR1A, it leads to release and activation of catalytic subunits that phosphorylate downstream targets, affecting processes such as metabolism, gene expression, cell proliferation, and hormonal signaling[1][3][6]. Mutations in the PRKAR1A gene can cause Carney complex, a syndrome of multiple endocrine tumors, and the gene acts as a tumor suppressor in some contexts, such as thyroid cancer[1][5]. PRKAR1A is also known to interact with numerous A-kinase anchoring proteins (AKAPs) and other regulatory proteins[1].

Other names
PKR1PRKAR1Tissue-specific extinguisher 1TSE1
02

Mechanism of action

Competitive inhibition of cAMP binding, allosteric modulation of kinase activity, negative regulation of cAMP/PKA signal transduction

03

Biological functions

cAMP bindingcAMP-dependent protein kinase inhibitor activitySignal transductionRegulation of gene expressionRegulation of insulin secretionCardiac muscle cell proliferationCellular response to glucagon stimulus
04

Disease associations

Cancer (notably Carney complex, thyroid cancer)Endocrine neoplasiaTumor-suppressor gene
05

Safety considerations

Loss-of-function mutations cause Carney complex (multiple endocrine neoplasia)oncogenic fusions (RET-PRKAR1A) in thyroid cancer
06

Interacting drugs

(Rp)-cAMPS

3 more in the full profile.

07

Biomarkers

PRKAR1A genetic mutations (for Carney complex, certain endocrine tumors)

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