Target type: molecularfunction
Removes cholesterol from a membrane or a monolayer lipid particle, transports it through the aqueous phase while protected in a hydrophobic pocket, and brings it to an acceptor membrane or lipid particle. [GOC:krc, PMID:20823909, PMID:24220498, PMID:25797198]
Cholesterol transfer activity is a molecular function that describes the ability of proteins to move cholesterol molecules between different cellular compartments or between different cells. Cholesterol is a vital lipid molecule that plays critical roles in cell membrane structure, signaling pathways, and steroid hormone synthesis. The transfer of cholesterol is essential for maintaining the appropriate levels of cholesterol in different cellular locations, ensuring proper membrane fluidity and function.
Cholesterol transfer proteins can be categorized into several families, including:
* **Steroidogenic Acute Regulatory Protein (StAR):** StAR facilitates the movement of cholesterol from the outer mitochondrial membrane to the inner mitochondrial membrane, where it is used for steroid hormone synthesis.
* **ATP-binding cassette (ABC) Transporters:** Some ABC transporters, such as ABCA1 and ABCG1, are involved in the export of cholesterol from cells.
* **Scavenger Receptor Class B, Type I (SR-BI):** SR-BI mediates selective uptake of cholesterol from high-density lipoprotein (HDL) particles.
* **Niemann-Pick C1 (NPC1) and NPC2 Proteins:** These proteins are involved in intracellular cholesterol trafficking and delivery to lysosomes for degradation.
These cholesterol transfer proteins utilize diverse mechanisms to facilitate cholesterol movement. Some proteins bind cholesterol directly, while others act as chaperones, assisting in the transport of cholesterol by other proteins. The specific mechanism of cholesterol transfer often involves interactions with specific lipid binding sites on the protein and may be influenced by factors such as the concentration of cholesterol, the presence of other lipids, and the cellular environment.
Dysregulation of cholesterol transfer activity can have significant implications for health. Mutations in genes encoding cholesterol transfer proteins can lead to various diseases, including Niemann-Pick disease, Tangier disease, and familial hypercholesterolemia. Additionally, alterations in cholesterol transfer pathways can contribute to the development of cardiovascular disease, neurodegenerative disorders, and cancer.
In summary, cholesterol transfer activity is a critical molecular function that ensures the proper distribution and utilization of cholesterol within cells. Understanding the mechanisms and regulation of cholesterol transfer is crucial for developing therapeutic strategies to treat diseases associated with cholesterol dysregulation.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Translocator protein | [no definition available] | Homo sapiens (human) |
| Niemann-Pick C1-like 1 protein | [no definition available] | Canis lupus familiaris (dog) |
| Microsomal triglyceride transfer protein large subunit | A microsomal triglyceride transfer protein large subunit that is encoded in the genome of human. [PRO:HJD, UniProtKB:P55157] | Homo sapiens (human) |
| Translocator protein | [no definition available] | Homo sapiens (human) |
| Cholesteryl ester transfer protein | A cholesteryl ester transfer protein that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11597] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| niacin | Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms). | pyridine alkaloid; pyridinemonocarboxylic acid; vitamin B3 | antidote; antilipemic drug; EC 3.5.1.19 (nicotinamidase) inhibitor; Escherichia coli metabolite; human urinary metabolite; metabolite; mouse metabolite; plant metabolite; vasodilator agent |
| pk 11195 | PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine | aromatic amide; isoquinolines; monocarboxylic acid amide; monochlorobenzenes | antineoplastic agent |
| ro 5-4864 | 4'-chlorodiazepam: selectively binds peripheral benzodiazepine receptor | ||
| clonazepam | clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses. | 1,4-benzodiazepinone; monochlorobenzenes | anticonvulsant; anxiolytic drug; GABA modulator |
| nordazepam | nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety. Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam. | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator; human metabolite; sedative |
| diazepam | diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| flunitrazepam | flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia. Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug. | 1,4-benzodiazepinone; C-nitro compound; monofluorobenzenes | anxiolytic drug; GABAA receptor agonist; sedative |
| lorazepam | Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. | benzodiazepine | |
| nevirapine | nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS. | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nitrazepam | nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome). Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic. | 1,4-benzodiazepinone; C-nitro compound | anticonvulsant; antispasmodic drug; drug metabolite; GABA modulator; sedative |
| cm 7116 | norflutoprazepam: structure | benzodiazepine | |
| oxazepam | oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5. Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia. | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| temazepam | Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | benzodiazepine | |
| chlordesmethyldiazepam | benzodiazepine | ||
| halazepam | halazepam: structure | organic molecular entity | |
| alpidem | imidazoles | ||
| efavirenz | efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. efavirenz: HIV-1 reverse transcriptase inhibitor | acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| ursolic acid | hydroxy monocarboxylic acid; pentacyclic triterpenoid | geroprotector; plant metabolite | |
| n-desmethylflunitrazepam | |||
| 7-aminonitrazepam | 7-aminonitrazepam: urinary metabolite of nitrazepam | benzodiazepine | |
| ro 20-1815 | 7-aminoflunitrazepam: flunitrazepam metabolite; structure given in first source | benzodiazepine | |
| dx 9065 | |||
| ro 11-6893 | Ro 11-6893: RN given refers to (R)-isomer | ||
| n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide | N,N-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide: binds with high affinity to glial mitochondrial diazepam binding inhibitor receptors & increases mitochondrial steroidogenesis | phenylindole | |
| torcetrapib | (trifluoromethyl)benzenes; carbamate ester; quinolines | anticholesteremic drug; CETP inhibitor | |
| sb 203580 | imidazoles; monofluorobenzenes; pyridines; sulfoxide | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent | |
| 7-aminoclonazepam | benzodiazepine | ||
| ro 5-3438 | Ro 5-3438: structure | ||
| n-desmethylflunitrazepam | N-desmethylflunitrazepam: metabolite of flunitrazepam | ||
| ro 05-4082 | ID 690: methyl deriv of clonazepam; structure | ||
| delta-8-tetrahydrocannabinol | 1-benzopyran | ||
| 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: structure in first source alvespimycin : A 19-membered macrocyle that is geldanamycin in which the methoxy group attached to the benzoquinone moiety has been replaced by a 2-(N,N-dimethylamino)ethylamino group. | 1,4-benzoquinones; ansamycin; carbamate ester; secondary amino compound; tertiary amino compound | Hsp90 inhibitor |
| ac-5216 | |||
| tanespimycin | CP 127374: analog of herbimycin A | 1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound; secondary amino compound | antineoplastic agent; apoptosis inducer; Hsp90 inhibitor |
| cb 34 | CB 34: ligand for peripheral benzodiazepine receptors; structure in first source | ||
| dalcetrapib | dalcetrapib: inhibits cholesteryl ester transfer protein (CETP) | anilide | |
| am-411 | |||
| sc 795 | |||
| 3-((3-(4-chloro-3-ethylphenoxy)phenyl)(3-(1,1,2,2-tetrafluoroethoxy)benzyl)amino)-1,1,1-trifluoropropan-2-ol | 3-((3-(4-chloro-3-ethylphenoxy)phenyl)(3-(1,1,2,2-tetrafluoroethoxy)benzyl)amino)-1,1,1-trifluoropropan-2-ol: inhibits cholesteryl ester transfer protein; structure in first source | ||
| n-(2-methoxybenzyl)-n-(4-phenoxypyridin-3-yl)acetamide | N-(2-methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide: for imaging brain peripheral benzodiazepine receptors; structure in first source | ||
| bms201038 | BMS201038: an anticholesteremic agent and microsomal triglycide transfer protein inhibitor lomitapide : A member of the class of benzamides obtained by formal condensation of the carboxy group of 4'-(trifluoromethyl)biphenyl-2-carboxylic acid with the primary amino group of 9-[4-(4-aminopiperidin-1-yl)butyl]-N-(2,2,2-trifluoroethyl)-9H-fluorene-9-carboxamide. Used (as its mesylate salt) as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia. | (trifluoromethyl)benzenes; benzamides; fluorenes; piperidines | anticholesteremic drug; MTP inhibitor |
| sch 60663 | SCH 60663: structure in first source | ||
| dirlotapide | dirlotapide: structure in first source | ||
| ssr180575 | SSR180575: structure in first source | ||
| amg 3 | AMG 3: structure in first source | ||
| km-233 | KM-233: used for the treatment of high-grade glioma; structure in first source | ||
| daa 1106 | |||
| mk 0354 | |||
| naluzotan | naluzotan: an antidepressant and anti-anxiety agent; structure in first source | ||
| anacetrapib | |||
| dpa-713 | |||
| a 803467 | A 803467: an Nav1.8 sodium channel blocker; structure in first source | ||
| gdc 0941 | pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring. | indazoles; morpholines; piperazines; sulfonamide; thienopyrimidine | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| jnj-31020028 | |||
| n-fluoroacetyl-n-(2,5-dimethoxybenzyl)-2-phenoxyaniline | N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline: a peripheral benzodiazepine receptor PET ligand; structure in first source | ||
| skepinone-l | skepinone-L: a dibenzosuberone-type p38 MAPK inhibitor; structure in first source | ||
| evacetrapib | benzazepine | ||
| MS-417 | MS-417 : A member of the class of thienotriazolodiazepines that is the methyl ester of [(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid. A bromodomain and extra-terminal domain (BET)-specific inhibitor that belongs to a group of thienodiazepine-based compounds | methyl ester; monochlorobenzenes; thienotriazolodiazepine |