Page last updated: 2024-10-24

channel regulator activity

Definition

Target type: molecularfunction

Binds to and modulates the activity of a channel. A channel catalyzes energy-independent facilitated diffusion, mediated by passage of a solute through a transmembrane aqueous pore or channel. [GOC:mah]

Channel regulator activity involves the modulation of the activity of ion channels, which are integral membrane proteins that form pores through which ions can pass across the cell membrane. Ion channels play critical roles in a wide range of cellular processes, including nerve impulse transmission, muscle contraction, and hormone secretion. Channel regulators can either enhance or inhibit channel activity, thereby fine-tuning cellular responses to stimuli.

There are several mechanisms by which channel regulators can modulate channel activity:

1. **Direct Binding:** Channel regulators can directly bind to the channel protein, altering its conformation and affecting its ability to open or close. This binding can be either to the channel's pore region, affecting ion permeability, or to other regions, altering the channel's gating properties.
2. **Indirect Interactions:** Some channel regulators act indirectly by interacting with other proteins that influence channel function. For example, they can interact with scaffolding proteins that organize channel complexes, or with signaling molecules that activate or inhibit channel activity.
3. **Modulation of Membrane Environment:** Channel regulators can influence the lipid environment surrounding the channel, thereby affecting its activity. For example, changes in membrane fluidity or lipid composition can affect the channel's stability or its response to stimuli.

Channel regulator activity is essential for proper cellular function. Dysregulation of channel regulator activity can contribute to a variety of human diseases, including neurological disorders, cardiovascular diseases, and cancer.'
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Proteins (8)

ProteinDefinitionTaxonomy
Voltage-dependent calcium channel gamma-7 subunitA voltage-dependent calcium channel gamma-7 subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:P62955]Homo sapiens (human)
Voltage-dependent calcium channel gamma-3 subunitA voltage-dependent calcium channel gamma-3 subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60359]Homo sapiens (human)
Voltage-dependent calcium channel gamma-8 subunitA voltage-dependent calcium channel gamma-8 subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8WXS5]Homo sapiens (human)
Voltage-dependent calcium channel gamma-5 subunitA voltage-dependent calcium channel gamma-5 subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UF02]Homo sapiens (human)
Voltage-dependent calcium channel gamma-2 subunitA voltage-dependent calcium channel gamma-2 subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y698]Homo sapiens (human)
Voltage-dependent calcium channel gamma-4 subunitA voltage-dependent calcium channel gamma-4 subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UBN1]Homo sapiens (human)
Peptidyl-prolyl cis-trans isomerase FKBP1BA peptidyl-prolyl cis-trans isomerase FKBP1B that is encoded in the genome of human. [PRO:DNx, UniProtKB:P68106]Homo sapiens (human)
Peptidyl-prolyl cis-trans isomerase FKBP1AA peptidyl-prolyl cis-trans isomerase FKBP1A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P62942]Homo sapiens (human)

Compounds (14)

CompoundDefinitionClassesRoles
tacrinetacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.

Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.
acridines;
aromatic amine
EC 3.1.1.7 (acetylcholinesterase) inhibitor
nimodipinenimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.

Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.
2-methoxyethyl ester;
C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
isopropyl ester
antihypertensive agent;
calcium channel blocker;
cardiovascular drug;
vasodilator agent
thiabendazoleTresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate1,3-thiazoles;
benzimidazole fungicide;
benzimidazoles
antifungal agrochemical;
antinematodal drug
cycloheximidecycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.

Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.
antibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol
anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor
3-(3-pyridyl)-1-propyl-(2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate
tacrolimustacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.

Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.
macrolide lactambacterial metabolite;
immunosuppressive agent
N-(2-fluorophenyl)-2-[2-(4-thiazolyl)-1-benzimidazolyl]acetamidebenzimidazoles
biricodarbiricodar: a non-macrocyclic ligand for FKBP12; structure in first sourcealpha-amino acid ester
l 683590immunomycin: from Streptomyces hygroscopicus; structure given in first sourceether;
lactol;
macrolide;
secondary alcohol
antifungal agent;
bacterial metabolite;
immunosuppressive agent
cyclosporineramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MFhomodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
sirolimussirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.

Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol
antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
ith 4012
bastadin 5
timcodartimcodar: a mutlidrug resistance inhibitor; structure in first source