Page last updated: 2024-10-24

cholesterol transport

Definition

Target type: biologicalprocess

The directed movement of cholesterol, cholest-5-en-3-beta-ol, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:mah, ISBN:0198506732]

Cholesterol transport is a complex and essential process that involves the movement of cholesterol between different cells and tissues throughout the body. It is crucial for maintaining cellular integrity, hormone production, and overall health. Here's a detailed breakdown of the process:

1. **Dietary Cholesterol Absorption:**
- Cholesterol consumed in food is absorbed in the small intestine.
- Bile salts, produced by the liver, emulsify dietary fats and cholesterol, facilitating their digestion and absorption.
- Cholesterol is then incorporated into micelles, small spherical structures that allow its transport across the intestinal lining.

2. **Cholesterol Transport from Intestine to Liver:**
- Absorbed cholesterol is packaged into chylomicrons, large lipoprotein particles that carry triglycerides and cholesterol.
- Chylomicrons enter the lymphatic system and eventually reach the bloodstream.
- Lipoprotein lipase, an enzyme present in blood vessel walls, breaks down triglycerides in chylomicrons, releasing fatty acids.
- Remnant chylomicrons, now enriched with cholesterol, are taken up by the liver.

3. **Cholesterol Synthesis in the Liver:**
- The liver also synthesizes cholesterol, which is crucial for various bodily functions.
- The liver uses cholesterol for producing bile acids, steroid hormones, and cell membranes.

4. **Cholesterol Transport from Liver to Other Tissues:**
- The liver packages cholesterol into low-density lipoproteins (LDL), also known as "bad cholesterol."
- LDL particles transport cholesterol to tissues throughout the body.
- Cells take up LDL cholesterol through receptor-mediated endocytosis, a process that involves specific receptors on cell surfaces.

5. **Cholesterol Transport Back to the Liver:**
- High-density lipoproteins (HDL), known as "good cholesterol," are responsible for transporting excess cholesterol back to the liver.
- HDL scavenges cholesterol from peripheral tissues and delivers it to the liver, where it can be excreted in bile.

6. **Regulation of Cholesterol Transport:**
- The liver plays a central role in regulating cholesterol levels.
- Factors like diet, genetics, and hormones influence cholesterol synthesis and transport.
- When cholesterol levels are high, the liver reduces cholesterol synthesis and increases LDL receptor expression, leading to more LDL uptake.
- Conversely, when cholesterol levels are low, the liver increases cholesterol synthesis and decreases LDL receptor expression.

7. **Role of Cholesterol in Maintaining Cell Structure and Function:**
- Cholesterol is an essential component of cell membranes, providing structural integrity and regulating membrane fluidity.
- It also serves as a precursor for the synthesis of various steroid hormones, including cortisol, testosterone, and estrogen.

8. **Consequences of Abnormal Cholesterol Transport:**
- High levels of LDL cholesterol can accumulate in blood vessels, leading to atherosclerosis, a condition characterized by plaque buildup in arteries, which can increase the risk of heart disease and stroke.
- Low levels of HDL cholesterol can contribute to an increased risk of heart disease.
- Proper regulation of cholesterol transport is vital for maintaining overall health and reducing cardiovascular risk.

In summary, cholesterol transport is a complex and tightly regulated process that ensures adequate cholesterol supply to tissues while maintaining safe levels in the bloodstream. Understanding this process is crucial for preventing and managing cardiovascular disease.'
"

Proteins (5)

ProteinDefinitionTaxonomy
NPC1-like intracellular cholesterol transporter 1An NPC1-like intracellular cholesterol transporter 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UHC9]Homo sapiens (human)
Cystic fibrosis transmembrane conductance regulatorA cystic fibrosis transmembrane conductance regulator that is encoded in the genome of human. [PRO:CNA, UniProtKB:P13569]Homo sapiens (human)
Cholesteryl ester transfer proteinA cholesteryl ester transfer protein that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11597]Homo sapiens (human)
Phosphatidylcholine-sterol acyltransferaseA phosphatidylcholine-sterol acyltransferase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P04180]Homo sapiens (human)
Low-density lipoprotein receptorA low-density lipoprotein receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P01130]Homo sapiens (human)

Compounds (44)

CompoundDefinitionClassesRoles
niacinNiacin: 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
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
dehydroepiandrosteronedehydroepiandrosterone : An androstanoid that is androst-5-ene substituted by a beta-hydroxy group at position 3 and an oxo group at position 17. It is a naturally occurring steroid hormone produced by the adrenal glands.

Dehydroepiandrosterone: A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
17-oxo steroid;
3beta-hydroxy-Delta(5)-steroid;
androstanoid
androgen;
human metabolite;
mouse metabolite
methyl anthranilatemethyl anthranilate : A benzoate ester that is the methyl ester of anthranilic acid.benzoate esterflavouring agent;
metabolite
ursolic acidhydroxy monocarboxylic acid;
pentacyclic triterpenoid
geroprotector;
plant metabolite
25-hydroxycholesterol25-hydroxy steroid;
oxysterol
human metabolite
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
7-ketocholesterol7-ketocholesterol : A cholestanoid that consists of cholesterol bearing an oxo substituent at position 7.

7-ketocholesterol: inhibits uptake of cholesterol in rabbit aorta
3beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
7-oxo steroid;
cholestanoid
neuroprotective agent
cholestane-3,5,6-triol, (3beta, 5alpha, 6beta)-isomer3beta-hydroxy steroid;
5alpha-hydroxy steroid;
6beta-hydroxy steroid
6-ketocholestanol
tadalafilbenzodioxoles;
pyrazinopyridoindole
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
ezetimibeezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).

Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.
azetidines;
beta-lactam;
organofluorine compound
anticholesteremic drug;
antilipemic drug;
antimetabolite
torcetrapib(trifluoromethyl)benzenes;
carbamate ester;
quinolines
anticholesteremic drug;
CETP inhibitor
ys 64cholestan-6-oxo-3,5-diol: metabolite of 5,6-epoxycholesterol; structure in first sourcecholestanoid
22s-hydroxycholesterol(22S)-22-hydroxycholesterol : An oxysterol that is the 22S-hydroxy derivative of cholesterol.22-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid;
oxysterol
sb 203580imidazoles;
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-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine
cholest-5-en-3 beta,7 alpha-diol, (3beta,7beta)-isomer7beta-hydroxy steroid;
oxysterol
delta-8-tetrahydrocannabinol1-benzopyran
s 1033(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone: a cystic fibrosis transmembrane conductance regulator inhibitor; structure in first source
uccf-029organic heterotricyclic compound;
organooxygen compound
quercetin7-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
apigeninChamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.trihydroxyflavoneantineoplastic agent;
metabolite
rutinHydroxyethylrutoside: Monohydroxyethyl derivative of rutin. Peripheral circulation stimulant used in treatment of venous disorders.disaccharide derivative;
quercetin O-glucoside;
rutinoside;
tetrahydroxyflavone
antioxidant;
metabolite
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
17-(dimethylaminoethylamino)-17-demethoxygeldanamycin17-(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
tanespimycinCP 127374: analog of herbimycin A1,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound;
secondary amino compound
antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor
dalcetrapibdalcetrapib: 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-ol3-((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
sch 60663SCH 60663: structure in first source
amg 3AMG 3: structure in first source
km-233KM-233: used for the treatment of high-grade glioma; structure in first source
mk 0354
anacetrapib
humaninhumanin: suppresses neuronal cell death induced by the Swedish mutant of amyloid precursor protein; suppresses neuronal cell death induced by three different types of FAD genes and amyloid beta; amino acid sequence in first source
vx-770ivacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with the amino group of 5-amino-2,4-di-tert-butylphenol. Used for the treatment of cystic fibrosis.

ivacaftor: a CFTR potentiator; structure in first source
aromatic amide;
monocarboxylic acid amide;
phenols;
quinolone
CFTR potentiator;
orphan drug
lumacaftorlumacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropane-1-carboxylic acid with the aromatic amino group of 3-(6-amino-3-methylpyridin-2-yl)benzoic acid. Used for the treatment of cystic fibrosis.

lumacaftor: a corrector of CF transmembrane conductance regulator (CTFR); structure in first source
aromatic amide;
benzodioxoles;
benzoic acids;
cyclopropanes;
organofluorine compound;
pyridines
CFTR potentiator;
orphan drug
gdc 0941pictrelisib : 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
cholenic acid dimethylamidecholenic acid dimethylamide: binds LXRalpha receptor; structure in first source
skepinone-lskepinone-L: a dibenzosuberone-type p38 MAPK inhibitor; structure in first source
evacetrapibbenzazepine