Page last updated: 2024-10-24

positive regulation of cyclic nucleotide-gated ion channel activity

Definition

Target type: biologicalprocess

Any process that activates or increases the frequency, rate or extent of cyclic nucleotide-gated ion channel activity. [GOC:TermGenie, PMID:11420311]

Positive regulation of cyclic nucleotide-gated ion channel activity is a biological process that enhances the activity of cyclic nucleotide-gated ion channels (CNGCs). CNGCs are membrane-bound proteins that allow the passage of ions across the cell membrane, specifically in response to the binding of cyclic nucleotides, such as cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). These channels are crucial for a variety of physiological processes, including sensory perception, neuronal signaling, and muscle contraction.

The positive regulation of CNGCs can occur through various mechanisms. One common mechanism involves the binding of intracellular signaling molecules, such as Ca2+ or protein kinases, to the channel protein. This binding can trigger conformational changes in the channel, leading to increased channel opening probability. Another mechanism involves the modulation of the channel's sensitivity to cyclic nucleotides. For instance, some proteins can directly interact with CNGCs and increase their affinity for cyclic nucleotides, leading to a greater response to a given concentration of cyclic nucleotides.

Positive regulation of CNGCs can also occur at the level of gene expression. Some transcription factors can bind to the promoters of CNGC genes and increase their expression, leading to an overall increase in the number of CNGCs in the cell. This can result in enhanced sensitivity to cyclic nucleotides and increased channel activity.

The precise mechanisms of positive regulation of CNGCs vary depending on the specific channel and the cell type in which it is expressed. However, all of these mechanisms ultimately contribute to an increase in CNGC activity, leading to changes in ion permeability and cellular function.

Positive regulation of CNGCs plays a critical role in various physiological processes. For example, in sensory neurons, positive regulation of CNGCs is essential for the detection of light, smell, and taste. In the nervous system, positive regulation of CNGCs is important for synaptic transmission and neuronal excitability. In muscle cells, positive regulation of CNGCs contributes to muscle contraction. Dysregulation of CNGC activity has been implicated in various diseases, including retinal degeneration, epilepsy, and cancer.'
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Proteins (1)

ProteinDefinitionTaxonomy
Cystic fibrosis transmembrane conductance regulatorA cystic fibrosis transmembrane conductance regulator that is encoded in the genome of human. [PRO:CNA, UniProtKB:P13569]Homo sapiens (human)

Compounds (13)

CompoundDefinitionClassesRoles
glyburideglyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.

Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide
monochlorobenzenes;
N-sulfonylurea
anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
methyl anthranilatemethyl anthranilate : A benzoate ester that is the methyl ester of anthranilic acid.benzoate esterflavouring agent;
metabolite
telmisartantelmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.

Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.
benzimidazoles;
biphenyls;
carboxybiphenyl
angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
tadalafilbenzodioxoles;
pyrazinopyridoindole
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine
3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone: a cystic fibrosis transmembrane conductance regulator inhibitor; structure in first source
uccf-029organic heterotricyclic compound;
organooxygen compound
quercetin7-hydroxyflavonol;
pentahydroxyflavone
antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
apigeninChamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.trihydroxyflavoneantineoplastic agent;
metabolite
rutinHydroxyethylrutoside: Monohydroxyethyl derivative of rutin. Peripheral circulation stimulant used in treatment of venous disorders.disaccharide derivative;
quercetin O-glucoside;
rutinoside;
tetrahydroxyflavone
antioxidant;
metabolite
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
vx-770ivacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with the amino group of 5-amino-2,4-di-tert-butylphenol. Used for the treatment of cystic fibrosis.

ivacaftor: a CFTR potentiator; structure in first source
aromatic amide;
monocarboxylic acid amide;
phenols;
quinolone
CFTR potentiator;
orphan drug
lumacaftorlumacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropane-1-carboxylic acid with the aromatic amino group of 3-(6-amino-3-methylpyridin-2-yl)benzoic acid. Used for the treatment of cystic fibrosis.

lumacaftor: a corrector of CF transmembrane conductance regulator (CTFR); structure in first source
aromatic amide;
benzodioxoles;
benzoic acids;
cyclopropanes;
organofluorine compound;
pyridines
CFTR potentiator;
orphan drug