Page last updated: 2024-10-24

monoatomic ion channel complex

Definition

Target type: cellularcomponent

A protein complex that spans a membrane and forms a water-filled channel across the phospholipid bilayer allowing selective monoatomic ion transport down its electrochemical gradient. [GOC:mah, ISBN:071673706X]

A monoatomic ion channel complex is a specialized cellular structure that facilitates the selective and controlled passage of single ions across cell membranes. These complexes are typically formed by transmembrane proteins that assemble into intricate structures, creating a pore through which ions can flow. The key components of this structure are as follows:

1. **Pore Domain:** This is the central component of the channel, forming the pathway through which ions traverse the membrane. The pore is highly selective, allowing only specific ions to pass, such as sodium (Na+), potassium (K+), calcium (Ca2+), or chloride (Cl-).

2. **Selectivity Filter:** Located within the pore domain, this region determines the specificity of the channel. It's composed of amino acid residues that interact with ions based on their charge, size, and hydration shell. This interaction ensures that only the appropriate ions can pass through.

3. **Gating Mechanism:** This mechanism controls the opening and closing of the pore, regulating ion flow across the membrane. Gating can be triggered by various factors, including voltage changes, ligand binding, or mechanical forces.

4. **Transmembrane Domains:** These regions of the channel proteins span the cell membrane, anchoring the complex within the lipid bilayer. They are often composed of alpha helices that interact with the surrounding lipids, ensuring stability and structural integrity.

5. **Cytosolic and Extracellular Domains:** These domains extend into the cytoplasm and extracellular space, respectively. They often play a role in signal transduction, mediating interactions with other cellular components or external stimuli.

The cellular component of a monoatomic ion channel complex is essential for maintaining cell homeostasis, regulating membrane potential, and facilitating signal transduction. It's a highly dynamic and complex structure, with its function tightly controlled by various factors. Understanding the organization and function of this complex is crucial for understanding cellular physiology and developing therapeutic strategies targeting ion channel dysfunction.'
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Proteins (9)

ProteinDefinitionTaxonomy
Potassium voltage-gated channel subfamily H member 3A voltage-gated potassium channel KCNH3 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9ULD8]Homo sapiens (human)
Potassium voltage-gated channel subfamily H member 7A voltage-gated potassium channel KCNH7 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9NS40]Homo sapiens (human)
Potassium voltage-gated channel subfamily H member 6A voltage-gated potassium channel KCNH6 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9H252]Homo sapiens (human)
Potassium channel subfamily K member 17A potassium channel subfamily K member 17 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q96T54]Homo sapiens (human)
Potassium voltage-gated channel subfamily H member 8A voltage-gated potassium channel KCNH8 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q96L42]Homo sapiens (human)
Potassium channel subfamily K member 10A potassium channel subfamily K member 10 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P57789]Homo sapiens (human)
Potassium voltage-gated channel subfamily KQT member 1A voltage-gated potassium channel subunit KCNQ1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P51787]Homo sapiens (human)
ATP-sensitive inward rectifier potassium channel 1An ATP-sensitive inward rectifier potassium channel 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P48048]Homo sapiens (human)
Potassium channel subfamily K member 5A potassium channel subfamily K member 5 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O95279]Homo sapiens (human)

Compounds (44)

CompoundDefinitionClassesRoles
N-(2-aminoethyl)-5-chloro-1-naphthalenesulfonamidenaphthalenes;
sulfonic acid derivative
alfuzosinalfuzosin: structure given in first sourcemonocarboxylic acid amide;
quinazolines;
tetrahydrofuranol
alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
carvedilolcarbazoles;
secondary alcohol;
secondary amino compound
alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
lamotrigine1,2,4-triazines;
dichlorobenzene;
primary arylamine
anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
duloxetineduloxetine
nelfinavirnelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.

Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound
antineoplastic agent;
HIV protease inhibitor
nebivolol2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group.chromanes;
diol;
organofluorine compound;
secondary alcohol;
secondary amino compound
uk 68798aromatic ether;
sulfonamide;
tertiary amino compound
anti-arrhythmia drug;
potassium channel blocker
doripenemDoripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.carbapenems
tadalafilbenzodioxoles;
pyrazinopyridoindole
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
paliperidone3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.

paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia.
1,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine;
secondary alcohol
293b cpd6-cyano-4-(N-ethylsulfonyl-N-methylamino)-3-hydroxy-2,2-dimethylchromane: RN given for (trans-(+-))-isomer1-benzopyran
moxifloxacinmoxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.

Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.
aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone;
quinolone antibiotic
antibacterial drug
solifenacinisoquinolines
telbivudinepyrimidine 2'-deoxyribonucleosideantiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
etravirineaminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound
antiviral agent;
HIV-1 reverse transcriptase inhibitor
lapatinibfurans;
organochlorine compound;
organofluorine compound;
quinazolines
antineoplastic agent;
tyrosine kinase inhibitor
darunavirdarunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.

Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.
carbamate ester;
furofuran;
sulfonamide
antiviral drug;
HIV protease inhibitor
senicapocsenicapoc: a Gardos channel blocker; structure in first source
lacosamideLacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES.N-acyl-amino acid
tolterodinetertiary amineantispasmodic drug;
muscarinic antagonist;
muscle relaxant
darifenacindarifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence.1-benzofurans;
monocarboxylic acid amide;
pyrrolidines
antispasmodic drug;
muscarinic antagonist
s 1033(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
maraviroctropane alkaloid
dasatinibdasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).

N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source
1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
n-(6-chloropyridin-3-yl)-4-fluorobenzamideN-(6-chloropyridin-3-yl)-4-fluorobenzamide: structure in first source
sitagliptinsitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.triazolopyrazine;
trifluorobenzene
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
7,13-bis(4-nitrobenzyl)-1,4,10-trioxa-7,13-diazacyclopentadecane7,13-bis(4-nitrobenzyl)-1,4,10-trioxa-7,13-diazacyclopentadecane: Potassium channel blocker; structure in first source
acacetin5,7-dihydroxy-4'-methoxyflavone : A monomethoxyflavone that is the 4'-methyl ether derivative of apigenin.dihydroxyflavone;
monomethoxyflavone
anticonvulsant;
plant metabolite
mdl 100907Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
silodosinsilodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first sourceindolecarboxamide
su 11248monocarboxylic acid amide;
pyrroles
angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
alvimopan anhydrousalvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for painpeptide
palonosetronpalonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.

Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.
azabicycloalkane;
delta-lactam;
organic heterotricyclic compound
antiemetic;
serotonergic antagonist
everolimuscyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol
anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
6-cyano-4-(n-ethylsulfonyl-n-methylamino)-3-hydroxy-2,2-dimethylchromane, (trans-(+))-isomer
lu 208075ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertensiondiarylmethane
a 1899A 1899: a TASK-1 potassium channel blocker; structure in first source
hmr 1556HMR 1556: an I(Ks) channel blocker; structure in first source
ica 27243N-(6-Chloropyridin-3-yl)-3,4-difluorobenzamide: a KCNQ2/3 channel activator; structure in first source
(r)-n-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide(R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide: structure in first source
raltegravir1,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide
antiviral drug;
HIV-1 integrase inhibitor
sildenafilsildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position.piperazines;
pyrazolopyrimidine;
sulfonamide
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
vardenafilvardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine.imidazotriazine;
N-alkylpiperazine;
N-sulfonylpiperazine
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent