Target type: biologicalprocess
Any process that stops, prevents or reduces the frequency, rate or extent of cation channel activity. [GOC:BHF]
Negative regulation of cation channel activity is a fundamental biological process that involves the modulation of ion permeability across cell membranes. This regulation is crucial for maintaining cellular homeostasis, coordinating physiological responses, and ensuring proper neuronal signaling. Cation channels are transmembrane proteins that form pores through which positively charged ions, such as sodium (Na+), potassium (K+), calcium (Ca2+), and magnesium (Mg2+), can traverse the cell membrane. The opening and closing of these channels are tightly controlled by various mechanisms, including:
1. **Voltage-dependent gating:** Some cation channels are sensitive to changes in the membrane potential. When the membrane potential reaches a certain threshold, the channel opens or closes. This mechanism is particularly important in excitable cells like neurons and muscle cells.
2. **Ligand-gated gating:** Other cation channels are regulated by the binding of specific molecules, called ligands, to the channel protein. Ligands can be neurotransmitters, hormones, or other signaling molecules. Binding of a ligand can either activate or inhibit channel activity.
3. **Phosphorylation:** The activity of cation channels can also be modulated by phosphorylation, a process in which phosphate groups are added to the channel protein. Phosphorylation can either increase or decrease channel activity, depending on the specific site of phosphorylation.
4. **Second messenger signaling:** Intracellular signaling pathways, triggered by various stimuli, can lead to the activation or inhibition of cation channels. These pathways often involve the production of second messengers, such as cyclic AMP (cAMP) or diacylglycerol (DAG), which interact with channel proteins to alter their activity.
5. **Mechanical stimuli:** Certain cation channels are sensitive to mechanical stress or deformation of the cell membrane. These channels are important in sensory systems, such as touch and hearing.
Negative regulation of cation channel activity is a complex process that involves a wide range of molecular mechanisms. This regulation is essential for maintaining the proper balance of ion fluxes across the cell membrane, which is critical for cellular function. For example, negative regulation of sodium channels is crucial for controlling the duration and amplitude of action potentials in neurons. Negative regulation of potassium channels plays a critical role in repolarizing the membrane after an action potential, allowing for the generation of new action potentials. Similarly, the negative regulation of calcium channels is crucial for controlling the influx of calcium ions into cells, which is essential for a wide range of cellular processes, including muscle contraction, neurotransmitter release, and gene expression.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Matrix metalloproteinase-9 | A matrix metalloproteinase-9 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P14780] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| catechol | catechols | allelochemical; genotoxin; plant metabolite | |
| busulfan | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent | |
| econazole | 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 4-chlorobenzyl group. econazole : A racemate composed of equimolar amounts of (R)- and (S)-econazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. Econazole: An imidazole derivative that is commonly used as a topical antifungal agent. | dichlorobenzene; ether; imidazoles; monochlorobenzenes | |
| way 151693 | |||
| nafamostat | nafamostat: inhibitor of trypsin, plasmin, pancreatic kallikrein, plasma kallikrein & thrombin; strongly inhibits esterolytic activities of C1r & C1 esterase complement-mediated hemolysis; antineoplastic | benzoic acids; guanidines | |
| prazosin | prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively. Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION. | aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| secobarbital | secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups. Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity. | barbiturates | anaesthesia adjuvant; GABA modulator; sedative |
| clodronic acid | clodronic acid : An organochlorine compound that is methylene chloride in which both hydrogens are replaced by phosphonic acid groups. It inhibits bone resorption and soft tissue calcification, and is used (often as the disodium salt tetrahydrate) as an adjunct in the treatment of severe hypercalcaemia associated with malignancy, and in the management of osteolytic lesions and bone pain associated with skeletal metastases. Clodronic Acid: A diphosphonate which affects calcium metabolism. It inhibits bone resorption and soft tissue calcification. | 1,1-bis(phosphonic acid); one-carbon compound; organochlorine compound | antineoplastic agent; bone density conservation agent |
| tiludronic acid | tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source | organochlorine compound | |
| 5,5'-methylenedisalicylic acid | 5,5'-methylenedisalicylic acid: inhibits attachment of ribosomes to microsomal membranes; RN given refers to parent cpd; structure in first source & Merck Index, 9th ed, #5934 | ||
| zoledronic acid | zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS. | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| piloty's acid | Piloty's acid: structure in first source | sulfonamide | |
| aminoquinuride | |||
| marimastat | marimastat : A secondary carboxamide resulting from the foraml condensation of the carboxy group of (2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the alpha-amino group of N,3-dimethyl-L-valinamide. marimastat: a matrix metalloproteinase inhibitor active in patients with advanced carcinoma of the pancreas, prostate, or ovary | hydroxamic acid; secondary carboxamide | antineoplastic agent; matrix metalloproteinase inhibitor |
| n-(2-isobutyl-3-(n'-hydroxycarbonylamido)propanoyl)-o-methyltyrosinemethylamide | N-(2-isobutyl-3-(N'-hydroxycarbonylamido)propanoyl)-O-methyltyrosinemethylamide: RN given refers to the (S-(R*,S*))-isomer | ||
| ilomastat | CS 610: matrix metalloproteinase inhibitor; structure in first source ilomastat : An N-acyl-amino acid obtained by formal condensation of the carboxy group of (2R)-2-[2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the amino group of N-methyl-L-tryptophanamide. A cell permeable broad-spectrum matrix metalloproteinase (MMP) inhibitor | hydroxamic acid; L-tryptophan derivative; N-acyl-amino acid | anti-inflammatory agent; antibacterial agent; antineoplastic agent; EC 3.4.24.24 (gelatinase A) inhibitor; neuroprotective agent |
| procyanidin C1 | procyanidin C1 : A proanthocyanidin consisting of three (-)-epicatechin units joined by two successive (4beta->8)-linkages. procyanidin trimer C1: a flavonoid found in multiple plant sources including grape, apple, and cacao, which has antioxidant and anti-inflammatory properties | hydroxyflavan; polyphenol; proanthocyanidin | anti-inflammatory agent; antioxidant; EC 1.17.3.2 (xanthine oxidase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; lipoxygenase inhibitor; metabolite |
| 3-((benzyl)(methylaminocarbonyl)methylaminocarbonyl)n-hydroxy-5-methylhexanamide | 3-((benzyl)(methylaminocarbonyl)methylaminocarbonyl)N-hydroxy-5-methylhexanamide: structure in first source | ||
| 2-(4-aminophenyl)benzothiazole | 2-(4-aminophenyl)benzothiazole: an agent with selective profile of in vitro anti-tumour activity; structure in first source | ||
| taxifolin | (+)-taxifolin : A taxifolin that has (2R,3R)-configuration. | taxifolin | metabolite |
| cgs 27023a | CGS 27023A: a matrix metalloproteinase inhibitor | ||
| prinomastat | prinomastat : A hydroxamic acid that is (3S)-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide in which the hydrogen attached to the thiomorpholine nitrogen has been replaced by a [4-(pyridin-4-yloxy)phenyl]sulfonyl group. It is a selective inhibitor with of matrix metalloproteinases (MMPs) 2, 3, 9, 13, and 14. prinomastat: a diazepine-based hydroxamic acid inhibitor; matrix metalloproteinase (MMP) inhibitor; angiogenesis inhibitor; | aromatic ether; hydroxamic acid; pyridines; sulfonamide; thiomorpholines | antineoplastic agent; EC 3.4.24.35 (gelatinase B) inhibitor; matrix metalloproteinase inhibitor |
| isoliquiritigenin | chalcones | antineoplastic agent; biological pigment; EC 1.14.18.1 (tyrosinase) inhibitor; GABA modulator; geroprotector; metabolite; NMDA receptor antagonist | |
| 2-[(4-phenylphenyl)sulfonylamino]pentanedioic acid | glutamic acid derivative | ||
| caffeic acid | trans-caffeic acid : The trans-isomer of caffeic acid. | caffeic acid | geroprotector; mouse metabolite |
| rs-130830 | RS-130830: orally-active broad-spectrum matrix metalloproteinase inhibitor | ||
| quercetin | 7-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 | |
| luteolin | 3'-hydroxyflavonoid; tetrahydroxyflavone | angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; c-Jun N-terminal kinase inhibitor; EC 2.3.1.85 (fatty acid synthase) inhibitor; immunomodulator; nephroprotective agent; plant metabolite; radical scavenger; vascular endothelial growth factor receptor antagonist | |
| pulmicort | budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis. Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS. | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone | anti-inflammatory drug; bronchodilator agent; drug allergen |
| amentoflavone | biflavonoid; hydroxyflavone; ring assembly | angiogenesis inhibitor; antiviral agent; cathepsin B inhibitor; P450 inhibitor; plant metabolite | |
| mangiferin | shamimin: isolated from the leaves of Bombax ceiba; structure in first source | C-glycosyl compound; xanthones | anti-inflammatory agent; antioxidant; hypoglycemic agent; plant metabolite |
| robustaflavone | robustaflavone : A biflavonoid that is obtained by oxidative coupling of two molecules of apigenin resulting in a bond between positions C-3 of the hydroxyphenyl ring and C-6 of the chromene ring. Isolated from Thuja orientalis and Rhus succedanea it exhibits antioxidant, cytotoxic and anti-hepatitis B activity. robustaflavone: bis-apigenin coupled at 6 and 3' positions; a potential non-nucleoside anti-hepatitis B agent; | biflavonoid; hydroxyflavone; ring assembly | anti-HBV agent; antineoplastic agent; antioxidant; metabolite |
| tmi-1 | |||
| benzyloxycarbonyl-phe-ala-fluormethylketone | cathepsin B inhibitor : A cysteine protease inhibitor which inhibits cathepsin B (EC 3.4.22.1). | ||
| bilobetin | bilobetin: a phospholipase A2 antagonist | flavonoid oligomer | |
| batimastat | batimastat : A secondary carboxamide resulting from the formal condensation of the carboxy group of (2S,3R)-5-methyl-3-{[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]carbamoyl}-2-[(thiophen-2-ylsulfanyl)methyl]hexanoic acid with the amino group of hydroxylamine. It a broad-spectrum matrix metalloprotease inhibitor. batimastat: structure given in first source; a synthetic matrix metalloproteinase inhibitor | hydroxamic acid; L-phenylalanine derivative; organic sulfide; secondary carboxamide; thiophenes; triamide | angiogenesis inhibitor; antineoplastic agent; matrix metalloproteinase inhibitor |
| isoacteoside | isoacteoside: a phenylethanoid glycoside isolated from Indian paintbrush (Verbenaceae) Castilleja linariaefolia; also in other plants; structure given in first source | hydroxycinnamic acid | |
| Methyl rosmarinate | hydroxycinnamic acid | ||
| ik 682 | IK 682: inhibits TNF-alpha converting enzyme; structure in first source | hydroxamic acid; pyrrolidin-2-ones; quinolines | |
| bay 12-9566 | Bay 12-9566: an angiogenesis inhibitor with matrix metalloproteinase inhibitory activity | biphenyls; organochlorine compound | |
| chlorhexidine | chlorhexidine : A bisbiguanide compound with a structure consisting of two (p-chlorophenyl)guanide units linked by a hexamethylene bridge. Chlorhexidine: A disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque. | biguanides; monochlorobenzenes | antibacterial agent; antiinfective agent |
| (11c)cgs 25966 | |||
| bb-78485 | BB-78485: structure in first source | ||
| ro 32-3555 | Ro 32-3555: structure given in first source | ||
| ro 28-2653 | Ro 28-2653: a synthetic matrix metalloproteinase inhibitor reduces tumor growth and prolongs survival in a prostate cancer standard rat model | ||
| abt-770 | ABT-770: structure in first source | ||
| sb 3ct compound | SB 3CT compound: a matrix metalloproteinase-2 inhibitor; structure in first source | aromatic ether | |
| pd 166793 | |||
| sc 78080 | |||
| ro 31-9790 | Ro 31-9790: hydroxamic acid derivative | ||
| n-((2s)-2-mercapto-1-oxo-4-(3,4,4- trimethyl-2,5-dioxo-1-imidazolidinyl)butyl)-l-leucyl-n,3- dimethyl-l-valinamide | N-((2S)-2-mercapto-1-oxo-4-(3,4,4- trimethyl-2,5-dioxo-1-imidazolidinyl)butyl)-L-leucyl-N,3- dimethyl-L-Valinamide: matrix metalloproteinase inhibitor | ||
| arp-100 | |||
| kb r8301 | |||
| s 3304 | S 3304: structure in first source | ||
| N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide | N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide : A hydroxamic acid that is N-hydroxy-D-valinamide in which the alpha-amino group has been substituted by isopropoxy and [biphenyl]-4-ylsulfonyl groups. A selective matrix metalloproteinase-2 (MMP-2) inhibitor, it is one of the most potent inducers of autophagy. Its physiological roles include angiogenesis, cancer metastasis, embryogenesis, tissue remodeling in development, and wound healing. | D-valine derivative; hydroxamic acid | antineoplastic agent; autophagy inducer; EC 3.4.24.24 (gelatinase A) inhibitor; melanin synthesis inhibitor |
| bms-566394 | BMS-566394: structure in first source | ||
| ks370g | KS370G: antihyperglycemic; structure in first source | ||
| incb3619 | INCB3619: ADAM inhibitor; structure in first source | ||
| tosedostat | carboxylic ester; hydroxamic acid; secondary carboxamide | ||
| grassystatin a | grassystatin A: isolated from a cyanobacterium, identified as Lyngbya cf.; structure in first source | ||
| minocycline | minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5. Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections. | ||
| dacarbazine | (E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration. | dacarbazine | |
| 2-[(4-chlorophenyl)methylthio]-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-4-one | aryl sulfide | ||
| MMP-9-IN-1 | MMP-9-IN-1 : A secondary carboxamide resulting from the formal condensation of the carboxy group of [(4-oxo-6-propyl-1,4-dihydropyrimidin-2-yl)sulfanyl]acetic acid with the amino group of 4-(difluoromethoxy)aniline. It is a specific matrix metalloproteinase-9 (MMP-9) inhibitor. | aromatic compound; organic sulfide; organofluorine compound; pyrimidone; secondary carboxamide | antineoplastic agent; EC 3.4.24.35 (gelatinase B) inhibitor |
| 2-[(4-methoxyphenyl)methylthio]-6-methyl-1H-pyrimidin-4-one | methoxybenzenes | ||
| hydrazinocurcumin | hydrazinocurcumin : A pyrazole obtained by cyclocodensation of the two carbonyl groups of curcumin with hydrazine. hydrazinocurcumin: structure in first source | aromatic ether; olefinic compound; polyphenol; pyrazoles | angiogenesis modulating agent; antineoplastic agent; EC 2.3.1.48 (histone acetyltransferase) inhibitor; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor |