Target intelligence / Profile preview

Cyclic guanosine monophosphate (cGMP)

Target
cGMP
Molecular classification
Other (second messenger; not a receptor, enzyme, transporter, or typical drug target)
01

Overview

Cyclic guanosine monophosphate (cGMP) is a cyclic nucleotide derived from guanosine triphosphate. It acts as an essential intracellular second messenger in many physiological processes. Synthesized primarily by the action of soluble or particulate guanylyl cyclases—activated respectively by nitric oxide and natriuretic peptides—cGMP mediates cellular responses such as smooth muscle relaxation, regulation of ion channels, modulation of protein kinases like PKG, and control over gene expression. Its signaling is terminated through hydrolysis by specific phosphodiesterases. While drugs such as PDE inhibitors and GC stimulators modulate the pathway involving cGMP for therapeutic benefit in cardiovascular diseases and erectile dysfunction among others, cGMP itself is not considered a direct therapeutic target like receptors or enzymes, but rather an intracellular mediator whose concentration is pharmacologically manipulated.

Other names
cGMPCyclic GMPGuanosine 3',5'-cyclic monophosphateGuanosine cyclic monophosphate
02

Mechanism of action

Drugs do not directly bind to cGMP but modulate its levels by affecting enzymes involved in its synthesis or degradation. For example, phosphodiesterase inhibitors prevent the breakdown of cGMP; guanylate cyclase stimulators enhance its production.

03

Biological functions

Signal transduction (as a second messenger)Regulation of ion channelsModulation of protein kinases (notably Protein Kinase G)Regulation of gene expressionSmooth muscle relaxation
04

Disease associations

Cardiovascular disease (e.g., heart failure, myocardial infarction)Neurological disorders (via synaptic plasticity and neurotransmission)Inflammation
05

Safety considerations

Excessive elevation of cGMP can cause hypotension and related adverse effects due to excessive smooth muscle relaxation.
06

Interacting drugs

Phosphodiesterase inhibitors (e.g., sildenafil/Viagra, tadalafil/Cialis) indirectly increase cGMP levels by inhibiting its breakdown

1 more in the full profile.

07

Biomarkers

Urinary or plasma cGMP levels can be used as biomarkers for kidney function and certain cardiovascular conditions

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