Target intelligence / Profile preview

Cyclic GMP-dependent Protein Kinase (PKG)

Target
PKG
Molecular classification
Enzyme, Protein Kinase, Serine/Threonine Kinase
01

Overview

Cyclic GMP-dependent protein kinase (PKG) is a serine/threonine-specific protein kinase activated by cyclic guanosine monophosphate (cGMP). It plays a central role in mediating the effects of cGMP signaling within cells and regulates various physiological processes including smooth muscle relaxation, platelet function, sperm metabolism, cell division, nucleic acid synthesis, and focal adhesion disassembly. There are two main types of PKG in mammals: Type I (PRKG1) and Type II (PRKG2). Type I exists as two isoforms—PKGIα and PKGIβ—produced via alternative splicing. PKG subunits consist of an N-terminal domain for homodimerization and autoinhibition, a regulatory domain with two nonidentical cGMP-binding sites, and a catalytic/kinase domain.

Other names
Protein kinase GcGKPRKG1PRKG2PRKGR1BPRKG1B
02

Mechanism of action

cGMP binding and activation of kinase activity

03

Biological functions

Smooth muscle relaxationPlatelet inhibitionSperm metabolismCell division regulationFocal adhesion disassemblyRegulation of vascular toneModulation of cardiac contractilitySignal transduction
04

Disease associations

Cardiovascular diseaseVascular disordersFamilial thoracic aortic aneurysms/dissections

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