Page last updated: 2024-10-24

negative regulation of mitochondrial fission

Definition

Target type: biologicalprocess

Any process that decreases the rate, frequency or extent of mitochondrial fission. Mitochondrial fission is the division of a mitochondrion within a cell to form two or more separate mitochondrial compartments. [GOC:sl, GOC:tb]

Mitochondrial fission is a fundamental process in which mitochondria, the powerhouses of the cell, divide into smaller units. This process is tightly regulated to ensure proper mitochondrial function and distribution within the cell. Negative regulation of mitochondrial fission involves a complex interplay of molecular mechanisms that suppress or inhibit the fission process.

One key regulatory mechanism involves the control of the activity of dynamin-related protein 1 (Drp1), a GTPase that acts as a master regulator of mitochondrial fission. Drp1 oligomerizes and forms constricting rings around mitochondria, leading to their division. Several factors negatively regulate Drp1 activity:

* **Phosphorylation:** Drp1 can be phosphorylated at specific residues by kinases such as PKA and AKT, leading to its inactivation and inhibition of fission.
* **Binding to Inhibitory Proteins:** Proteins like Mfn2 (mitofusin 2) and FIS1 (fission 1) bind to Drp1, preventing its assembly and activity.
* **Ubiquitination:** Drp1 can undergo ubiquitination, a process that targets proteins for degradation, leading to its removal from mitochondria.

Another level of negative regulation involves the involvement of other proteins that directly inhibit fission machinery:

* **Mitochondrial Fusion Proteins:** Proteins like Mfn1 (mitofusin 1) and OPA1 (optic atrophy 1) promote mitochondrial fusion, the opposite of fission. By promoting fusion, these proteins indirectly inhibit fission.
* **Specific Inhibitors:** Proteins like GDAP1 (ganglioside-induced differentiation-associated protein 1) have been shown to directly inhibit Drp1-mediated fission.

The balance between positive and negative regulators of mitochondrial fission is crucial for maintaining mitochondrial health and cellular function. Dysregulation of these pathways can lead to mitochondrial dysfunction and contribute to various diseases. For instance, excessive mitochondrial fission has been linked to neurodegenerative diseases like Parkinson's disease and Alzheimer's disease. Conversely, reduced fission can contribute to diseases like cancer and diabetes.

In summary, negative regulation of mitochondrial fission involves a complex and intricate network of molecular mechanisms, including Drp1 phosphorylation, binding to inhibitory proteins, ubiquitination, and the involvement of fusion proteins and specific inhibitors. These mechanisms are critical for maintaining mitochondrial homeostasis and preventing pathological consequences.'
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Proteins (2)

ProteinDefinitionTaxonomy
Peroxisome proliferator-activated receptor gammaA peroxisome proliferator-activated receptor gamma that is encoded in the genome of human. [PRO:DNx, UniProtKB:P37231]Homo sapiens (human)
Microtubule-associated protein tauA microtubule-associated protein tau that is encoded in the genome of human. [PRO:DAN]Homo sapiens (human)

Compounds (128)

CompoundDefinitionClassesRoles
gw 2433GW 2433: binds peroxisome proliferator-activated receptor alpha (PPARalpha); structure in first source
2,2-bis(4-glycidyloxyphenyl)propane2,2-bis(4-glycidyloxyphenyl)propane: structurediarylmethane
candesartan cilexetilcandesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effectsbiphenyls
cannabinolCannabinol: A physiologically inactive constituent of Cannabis sativa L.dibenzopyran
chelerythrinechelerythrine : A benzophenanthridine alkaloid isolated from the root of Zanthoxylum simulans, Chelidonium majus L., and other Papaveraceae.benzophenanthridine alkaloid;
organic cation
antibacterial agent;
antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor
ciglitazoneciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist.

ciglitazone: structure given in second source; PPAR agonist used for type II diabetes
aromatic ether;
thiazolidinone
antineoplastic agent;
insulin-sensitizing drug
clofibrateangiokapsul: contains clofibrate & insoitolnicotinatearomatic ether;
ethyl ester;
monochlorobenzenes
anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clofibric acidclofibric acid : A monocarboxylic acid that is isobutyric acid substituted at position 2 by a p-chlorophenoxy group. It is a metabolite of the drug clofibrate.

Clofibric Acid: An antilipemic agent that is the biologically active metabolite of CLOFIBRATE.
aromatic ether;
monocarboxylic acid;
monochlorobenzenes
anticholesteremic drug;
antilipemic drug;
antineoplastic agent;
herbicide;
marine xenobiotic metabolite;
PPARalpha agonist
decanoic aciddecanoate : A fatty acid anion 10:0 that is the conjugate base of decanoic acid.

decanoic acid : A C10, straight-chain saturated fatty acid.
medium-chain fatty acid;
straight-chain saturated fatty acid
algal metabolite;
anti-inflammatory agent;
antibacterial agent;
human metabolite;
plant metabolite;
volatile oil component
fenofibratePharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINEaromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes
antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
gemfibrozilaromatic etherantilipemic drug
gentian violetcrystal violet cation : An iminium ion that is malachite green cation in which the hydrogen at the para- psition of the monosubstituted phenyl group is replaced by a dimethylamino group.iminium ionantibacterial agent;
antifungal agent
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
indomethacinindometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.

Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.
aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole
analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic;
xenobiotic metabolite
lansoprazoleLansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.benzimidazoles;
pyridines;
sulfoxide
anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
lg 100268LG 100268: a retinoid X receptor (RXR) selective compound; structure given in first source
3,7-bis(dimethylamino)phenothiazin-5-ium3,7-bis(dimethylamino)phenothiazin-5-ium : An organic cation that is phenothiazin-5-ium substituted by dimethylamino groups at positions 3 and 7. The chloride salt is the histological dye 'methylene blue'.organic cation
pioglitazonepioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.

Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.
aromatic ether;
pyridines;
thiazolidinediones
antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
aurinaurin: structurediarylmethane
troglitazoneTroglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.chromanes;
thiazolidinone
anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent
pirinixic acidpirinixic acid: structurearyl sulfide;
organochlorine compound;
pyrimidines
ici 204,219zafirlukast: a leukotriene D4 receptor antagonistcarbamate ester;
indoles;
N-sulfonylcarboxamide
anti-asthmatic agent;
leukotriene antagonist
3,3',5-triiodothyroacetic acidtiratricol : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)acetic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxy-3-iodophenoxy group. It is a thyroid hormone analogue that has been used in the treatment of thyroid hormone resistance syndrome.
thyroxinethyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.

Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.
2-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine;
thyroxine zwitterion
antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
triiodothyronine3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism.

Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.
2-halophenol;
amino acid zwitterion;
iodophenol;
iodothyronine
human metabolite;
mouse metabolite;
thyroid hormone
methylene bluemethylene blue : An organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.

Methylene Blue: A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.
organic chloride saltacid-base indicator;
antidepressant;
antimalarial;
antimicrobial agent;
antioxidant;
cardioprotective agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 4.6.1.2 (guanylate cyclase) inhibitor;
fluorochrome;
histological dye;
neuroprotective agent;
physical tracer
tolonium chloridetolonium chloride : An organic chloride salt having 3-amino-7-(dimethylamino)-2-methylphenothiazin-5-ium (tolonium) as the counterion. It is a blue nuclear counterstain that can be used to demonstrate Nissl substance and is also useful for staining mast cell granules, both in metachromatic and orthochromatic techniques.

Tolonium Chloride: A phenothiazine that has been used as a hemostatic, a biological stain, and a dye for wool and silk. Tolonium chloride has also been used as a diagnostic aid for oral and gastric neoplasms and in the identification of the parathyroid gland in thyroid surgery.
methyleugenolmethyleugenol: structurephenylpropanoid
azure aazure A : An organic chloride salt having 3-amino-7-(dimethylamino)phenothiazin-5-ium as the counterion. It is used in making azure eosin stains for blood smear staining.

Azure A: RN given refers to chloride
cannabichromene1-benzopyran
halofenateHalofenate: An antihyperlipoproteinemic agent and uricosuric agent.
bezafibratearomatic ether;
monocarboxylic acid;
monocarboxylic acid amide;
monochlorobenzenes
antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
pioglitazone hydrochloridearomatic ether
mifobatemifobate: has antiatherosclerotic propertiestrialkyl phosphate
fenofibric acidfenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.

fenofibric acid: RN given refers to parent cpd without isomeric designation; structure
aromatic ketone;
chlorobenzophenone;
monocarboxylic acid
drug metabolite;
marine xenobiotic metabolite
thioninethionine : An organic chloride salt composed of 3,7-diaminophenothiazin-5-ium and chloride ions in a 1:1 ratio. A strongly metachromatic dye, useful for the staining of acid mucopolysaccharides. It is also a common nuclear stain and can be used for the demonstration of Nissl substance in nerve cells of the CNS.

thionine: do not confuse with the thionins which is a class of polypeptides; RN above is for the chloride;
epigallocatechin gallate(-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin.

epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis)
flavans;
gallate ester;
polyphenol
antineoplastic agent;
antioxidant;
apoptosis inducer;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent;
plant metabolite
tetraiodothyroacetic acid3,3',5,5'-tetraiodothyroacetic acid : A monocarboxylic acid that is thyroacetic acid carrying four iodo substituents at positions 3, 3', 5 and 5'.

tetraiodothyroacetic acid: RN given refers to parent cpd; structure
2-halophenol;
aromatic ether;
iodophenol;
monocarboxylic acid
apoptosis inducer;
human metabolite;
thyroid hormone
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
azure bazure B : An organic chloride salt having 3-(dimethylamino)-7-(methylamino)phenothiazin-5-ium as the counterion. It is used in making azure eosin stains for blood smear staining and is an active metabolite of methylene blue.

Azure B: RN given refers to chloride
epicatechin(-)-epicatechin : A catechin with (2R,3R)-configuration.catechin;
polyphenol
antioxidant
xanthomicrolxanthomicrol : A trimethoxyflavone that is flavone substituted by methoxy groups at positions 6, 7 and 8 and hydroxy groups at positions 5 and 4'.

xanthomicrol: structure in first source
dihydroxyflavone;
trimethoxyflavone
antineoplastic agent;
plant metabolite
rosiglitazoneaminopyridine;
thiazolidinediones
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
gardenin bgardenin B : A tetramethoxyflavone that is tangeretin in which the methoxy group at position 5 has been replaced by a hydroxy group.

gardenin B: has antineoplastic activity; structure in first source
monohydroxyflavone;
tetramethoxyflavone
plant metabolite
mk 7675-((2,4-dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide: an antihyperlipidemic agent that also functions as an insulin sensitizer, PPARalpha agonist, and PPARgamma agonist; structure in first source
jtt 501JTT 501: an insulin sensitizer; structure in first source
anacardic acidanacardic acid : A hydroxybenzoic acid that is salicylic acid substituted by a pentadecyl group at position 6. It is a major component of cashew nut shell liquid and exhibits an extensive range of bioactivities.

anacardic acid: isolated from Anacardium occidentale; monophenol monooxygenase inhibitor
hydroxy monocarboxylic acid;
hydroxybenzoic acid
anti-inflammatory agent;
antibacterial agent;
anticoronaviral agent;
apoptosis inducer;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
neuroprotective agent;
plant metabolite
farglitazarfarglitazar: a non-thiazolidinedione insulin sensitiser and PPARgamma agonist
l 158809L 158809: RN & structure given in first source; angiotensin receptor antagonist
muraglitazarmuraglitazar: has glucose- and lipid-lowering activities; structure in first source; molecule composed of benzyloxazole-phenoxy-oxybenzylglycine-phenoxyl having structural analogy to PHENOXYBENZAMINE1,3-oxazoles
tesaglitazartesaglitazar: structure in first source
2-(2-phenylethyl)chromone2-(2-phenylethyl)chromone : A member of the class of chromones that is chromone which is substituted by a 2-phenylethyl group at position 2. It is found in agarwood, a fragrant resinous heartwood obtained from certain trees in the genus Aquilaria.

2-(2-phenylethyl)chromone: from Aquilaria sinensis; structure given in first source
benzenes;
chromones
plant metabolite
eicosapentaenoic acidall-cis-5,8,11,14,17-icosapentaenoic acid : An icosapentaenoic acid having five cis-double bonds at positions 5, 8, 11, 14 and 17.

icosapentaenoic acid : Any straight-chain, C20 polyunsaturated fatty acid having five C=C double bonds.
icosapentaenoic acid;
omega-3 fatty acid
anticholesteremic drug;
antidepressant;
antineoplastic agent;
Daphnia galeata metabolite;
fungal metabolite;
micronutrient;
mouse metabolite;
nutraceutical
mycophenolic acidmycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.

mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.

Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.
2-benzofurans;
gamma-lactone;
monocarboxylic acid;
phenols
anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
environmental contaminant;
immunosuppressive agent;
mycotoxin;
Penicillium metabolite;
xenobiotic
gw 409544GW 409544: a PPARalpha agonist; structure in first sourcemonocarboxylic acid
drf 2725ragaglitazar: a phenoxazine analogue of phenyl propanoic acid; Ragaglitazar is a coligand of PPARalpha and PPARgamma
epipinoresinolepipinoresinol : An enantiomer of pinoresinol having (+)-(1R,3aR,4S,6aR)-configuration.pinoresinolmarine metabolite;
plant metabolite
cannabidiolcannabidiol : An cannabinoid that is cyclohexene which is substituted by a methyl group at position 1, a 2,6-dihydroxy-4-pentylphenyl group at position 3, and a prop-1-en-2-yl group at position 4.

Cannabidiol: Compound isolated from Cannabis sativa extract.
olefinic compound;
phytocannabinoid;
resorcinols
antimicrobial agent;
plant metabolite
gw96622-chloro-5-nitrobenzanilide: pretreatment of peroxisome proliferator activated receptors with GW9662 results in the irreversible loss of ligand bindingbenzamides
triiodothyronine, reverse3,3',5'-triiodothyronine;
amino acid zwitterion
curcumincurcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.

Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.
aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol
anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
sulindacsulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.

Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.
monocarboxylic acid;
organofluorine compound;
sulfoxide
analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent
t 0070907T 0070907: a PPARgamma antagonist; structure in first sourcecarbonyl compound;
organohalogen compound
gsk 3787
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide: structure given in first source
rivoglitazonerivoglitazone: structure in first source
gw 7647GW 7647 : A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group.

GW 7647: a PPAR-alpha agonist; structure in first source
aryl sulfide;
monocarboxylic acid;
ureas
PPARalpha agonist
Angolensinketone
hydroxypioglitazonehydroxypioglitazone : A member of the class of thiazolidenediones that is the hydroxy derivative of pioglitazone.

leriglitazone: PPAR gamma agonist
aromatic ether;
pyridines;
thiazolidinediones
human xenobiotic metabolite
gossypetingossypetin : A hexahydroxyflavone having the hydroxy groups placed at the 3-, 3'-, 4'-, 5- 7- and 8-positions.

gossypetin: inhibits activity of penicillinase enzyme in E coli
7-hydroxyflavonol;
hexahydroxyflavone
plant metabolite
alpha-linolenic acidlinolenate : A polyunsaturated fatty acid anion obtained by deprotonation of the carboxy group of either alpha- or gamma-linolenic acid.

linolenic acid : A two-membered subclass of octadecatrienoic acid comprising the (9Z,12Z,15Z)- and (6Z,9Z,12Z)-isomers. Linolenic acids are nutrients essential to the formation of prostaglandins and are also used in making paints and synthetic resins.
linolenic acid;
omega-3 fatty acid
micronutrient;
mouse metabolite;
nutraceutical
clothiapinemaleate salt
galangin5,7-dihydroxyflavonol: antimicrobial from the twigs of Populus nigra x Populus deltoides; structure in first source

galangin : A 7-hydroxyflavonol with additional hydroxy groups at positions 3 and 5 respectively; a growth inhibitor of breast tumor cells.
7-hydroxyflavonol;
trihydroxyflavone
antimicrobial agent;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
plant metabolite
myricetin7-hydroxyflavonol;
hexahydroxyflavone
antineoplastic agent;
antioxidant;
cyclooxygenase 1 inhibitor;
food component;
geroprotector;
hypoglycemic agent;
plant metabolite
psi-baptigeninpseudobaptigenin : A member of the class of 7-hydroxyisoflavones that is 7-hydroxyisoflavone and in which the phenyl group at position 3 is replaced by a 1,3-benzodioxol-5-yl group.7-hydroxyisoflavones;
benzodioxoles
antiprotozoal drug;
plant metabolite
9-hydroxy-10,12-octadecadienoic acid9-HODE : A HODE that consists of (10E,12Z)-octadecadienoic acid with the hydroxy substituent located at position 9.

9-hydroxy-10,12-octadecadienoic acid: RN given refers to unspecified stereoisomer
HODE;
octadecadienoic acid
human metabolite;
metabolite;
mouse metabolite;
plant metabolite
15-deoxy-delta(12,14)-prostaglandin j215-deoxy-Delta(12,14)-prostaglandin J2 : A prostaglandin J derivative comprising prostaglandin J2 lacking the 15-hydroxy group and having C=C double bonds at the 12- and 14-positions.

15-deoxy-delta(12,14)-prostaglandin J2: 15-deoxy-PGJ2 is also available; check for double bonds (indicated by delta) at 12 and 14 positions
prostaglandins Jelectrophilic reagent;
insulin-sensitizing drug;
metabolite
cannabigerolcannabigerol : A member of the class of resorcinols that is resorcinol which is substituted by a (2E)-3,7-dimethylocta-2,6-dien-1-yl group at position 2 and by a pentyl group at position 5. It is a natural product found in Cannabis sativa and Helichrysum species.

cannabigerol: RN given refers to (E)-isomer; structure given in first source
phytocannabinoid;
resorcinols
anti-inflammatory agent;
antibacterial agent;
antioxidant;
appetite enhancer;
cannabinoid receptor agonist;
neuroprotective agent;
plant metabolite
sulindac sulfidesulindac sulfide : An aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity.

sulindac sulfide: sulfated analog of indomethacin & inhibitor of prostaglandin synthesis in vitro; RN given refers to cpd without isomeric designation; structure given in first source
aryl sulfide;
monocarboxylic acid;
organofluorine compound
antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug
psammaplin apsammaplin A: isolated from marine sponges Poecillastra and Jaspis; structure in second source
4-o-carboxymethylascochlorin4-O-carboxymethylascochlorin: RN given refers to (1R-(1alpha(2E,4E),2beta,6beta))-isomer
pregna-4,17-diene-3,16-dionepregna-4,17-diene-3,16-dione: steroid from guggulu extract; RN & N1 from C1 Form index; RN given refers to cpd without isomeric designation; structure in first source; antagonist of farnesoid X receptor3-hydroxy steroidandrogen
amorphastilbolamorphastilbol: dual PPARalpha/gamma agonist from Amorpha species
su 4312SU4312 : A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group. SU 4312 is a vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 and platelet derived growth factor (PDGF) receptor inhibitor. It also inhibits the neuronal nitric oxide synthase (NOS) and exhibits neuroprotection against NO-mediated neurotoxicity.
gw 1929GW 1929: activates peroxisome proliferator-activated receptor-gamma; structure in first sourcebenzophenones
l-1650414-(3-(2-propyl-3-hydroxy-4-acetyl)phenoxy)propyloxyphenoxy acetic acid: a PPAR-delta agonist has regulatory effects on a variety of adipokines, and these effects might explain some of their metabolic function.aromatic ketone
alpha-glutamyltryptophanTrp-Glu : A dipeptide formed from L-tryptophan and L-glutamic acid residues.dipeptidemetabolite
gw 501516GW 501516 : An aromatic ether that is phenoxyacetic acid in which the phenyl group is substituted at position 2 by a methyl group and at position 4 by a (1,3-thiazol-5-ylmethyl)sulfanediyl group, and in which the 1,3-thiazolyl group is substituted at positions 2 and 4 by p-trifluoromethylphenyl and methyl groups, respectively.

GW 501516: a selective PPARdelta agonist; structure in first source
1,3-thiazoles;
aromatic ether;
aryl sulfide;
monocarboxylic acid;
organofluorine compound
carcinogenic agent;
PPARbeta/delta agonist
tzd 18
efatutazoneefatutazone: a high-affinity PPARgamma agonist with antineoplastic activity
lg 1506
nrx 194204IRX4204: retinoid X receptor (RXR) agonist; structure in first source
gft505
3-(2,4-dichlorobenzyl)-2-methyl-n-(pentylsulfonyl)-3 h-benzimidazole-5-carboxamide3-(2,4-dichlorobenzyl)-2-methyl-N-(pentylsulfonyl)-3 H-benzimidazole-5-carboxamide: a benzimidazole derivative
gw 9578GW 9578: a peroxisome proliferator-activated receptor alpha agonist; structure in first source
gw 7845GW 7845: ligand of the peroxisome proliferator-activated receptor-gamma; structure in first source
naveglitazarnaveglitazar: LY-519818 is the (alpha-S)-isomer; an antidiabetic agent; structure in first sourcearomatic ether
ly 465608LY 465608: a nonthiazolidinedione agonist of both PPAR-alpha and PPAR-gamma of Ligand Pharm. and Eli Lilly
l 796449L 796449: a peroxisomal proliferator-activated receptor-gamma agonist; structure in first source
gw0742GW 610742: structure in first sourcemonocarboxylic acid
3-chloro-4-(3-(7-propyl-3-trifluoromethyl-6-benzisoxazolyl)propylthio)phenylacetic acid
ns-220
bm 131246
gw 5907352-methyl-2-(4-(((4-methyl-2-(4-trifluoromethylphenyl)-thiazol-5-ylcarbonyl)amino)methyl)phenoxy)propionic acid: an HDLc raising agent; structure in first source
tirotundintirotundin: structure in first source
2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole
int 131INT 131: a hypoglycemic agent; structure in first source
aleglitazaraleglitazar: a dual peroxisome PPAR-alpha and PPAR-gamma agonist for type 2 diabetes
bavachininbavachinin: do not confuse with bavachinflavanones
msdc-0160MSDC-0160: an mTOT (mitochondrial target of thiazolidinediones) modulator for insulin sensitization; structure in first sourcearomatic ether
mbx-8025seladelpar: PPAR-delta agonist
cannabidiol hydroxyquinonecannabidiol hydroxyquinone: structure given in first source; an air oxidation product of cannabidiol; inhibits the hepatic microsomal drug-metabolizing enzymes of mice through the decrease of cytochrome P-450 content; RN given refers to (1R-trans)-isomerprenylquinone
lt175
gw9508GW9508: structure in first sourcearomatic amine
lj 529
arhalofenatearhalofenate: a PPAR-gamma modulator
odoratinodoratin: structure; RN given refers to cpd without isomeric designation
bms 687453
amorfrutin aamorfrutin A: an antidiabetic agent that inhibits NF-kappaB activation; structure in first sourcestilbenoid
amorfrutin bamorfrutin B: structure in first source
ys 1212-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid: inhibits microsomal prostaglanding E2 synthase; structure in first sourcemedium-chain fatty acid
10-nitro-oleic acid(9E)-10-nitrooctadecenoic acid : A nitro fatty acid that is (9E)-octadec-9-enoic (elaidic) acid substituted by a nitro group at position 10.

10-nitro-oleic acid: structure in first source
long-chain fatty acid;
monounsaturated fatty acid;
nitro fatty acid
human metabolite
[5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid[5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid : A sulindac-based non-steroidal anti-inflammatory drug.

K-80003: sulindac derivative that inhibits activation of phosphoinositide 3-kinase (PI3K) by retinoid X receptor alpha (RXRalpha) in tumor cells
organofluorine compoundnon-steroidal anti-inflammatory drug
gsk0660GSK0660: PPAR antagonist; structure in first sourcesulfonamide
sr1664indolecarboxamide
cnb 001
ly 518674LY 518674: a peroxisome proliferator-activated receptor alpha agonist; structure in first source
hydrazinocurcuminhydrazinocurcumin : 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