Target intelligence / Profile preview

Protein Kinase G Pathway Activation via cGMP Elevation Leading to Apoptosis Induction (PKG Pathway Activation)

Target
PKG Pathway Activation
Molecular classification
Signal Transduction Pathway, Protein Kinase, Second Messenger System
01

Overview

Activation of the protein kinase G (PKG) pathway via elevation of cyclic guanosine monophosphate (cGMP) aims to induce apoptosis in neoplastic cells. This pathway is initiated by increased intracellular cGMP, which activates PKG. PKG then phosphorylates downstream targets, regulating cell proliferation and survival, often leading to growth inhibition or programmed cell death in certain cancer types. Strategies to activate this pathway include using NO donors, natriuretic peptides, guanylyl cyclase activators, and PDE5 inhibitors.

Other names
cGMP/PKG Pathway ActivationCyclic GMP-dependent Protein Kinase ActivationPKG SignalingcGMP Signaling
02

Mechanism of action

Elevation of intracellular cGMP levels activates Protein Kinase G (PKG), leading to phosphorylation of downstream targets involved in cell proliferation and survival, ultimately resulting in apoptosis in neoplastic cells.

03

Biological functions

ApoptosisCell Growth InhibitionSignal TransductionRegulation of Cell ProliferationVascular Tone RegulationCardiac Function Regulation
04

Disease associations

CancerCardiovascular Disease
05

Safety considerations

Potential for off-target effects due to broad PKG substrate specificityCardiovascular effects related to vasodilationDrug interactions with other vasodilators or antihypertensive medicationsPotential for resistance development in cancer cellsSelectivity towards cancer cells versus normal cells
06

Interacting drugs

Nitric Oxide Donors

3 more in the full profile.

07

Biomarkers

cGMP levelsPKG ActivityPDE5 ExpressionExpression levels of PKG downstream targetsGuanylyl cyclase expression

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