Page last updated: 2024-10-24

apolipoprotein A-I receptor binding

Definition

Target type: molecularfunction

Binding to an apolipoprotein A-I receptor. [GOC:BHF, GOC:rl]

Apolipoprotein A-I receptor (AI-receptor) binding is a crucial step in the reverse cholesterol transport (RCT) pathway, a process that removes excess cholesterol from peripheral tissues and delivers it to the liver for excretion. The AI-receptor, a member of the scavenger receptor superfamily, is expressed primarily on the surface of hepatocytes, the main cells of the liver. It plays a pivotal role in the uptake of high-density lipoprotein (HDL), the major cholesterol carrier in the blood.

HDL particles, rich in apolipoprotein A-I (apoA-I), bind to the AI-receptor on hepatocytes. This binding event triggers a series of intracellular signaling events that ultimately lead to the internalization of the HDL particle into the hepatocyte. Once inside the cell, HDL is broken down, and its cholesterol cargo is either excreted into bile or used for other cellular processes.

The binding of apoA-I to the AI-receptor is highly specific and is mediated by a series of interactions between amino acid residues on both the receptor and the apolipoprotein. These interactions are influenced by the conformation of apoA-I, which can change depending on the lipid content of the HDL particle. For instance, apoA-I adopts a distinct conformation when bound to lipid, which enhances its affinity for the AI-receptor.

The interaction between apoA-I and the AI-receptor is essential for maintaining cholesterol homeostasis and protecting against cardiovascular disease. Defects in this process can lead to the accumulation of cholesterol in the blood, increasing the risk of atherosclerosis, heart attacks, and strokes. Therefore, understanding the molecular mechanisms of AI-receptor binding is crucial for developing novel therapies targeting cholesterol metabolism and cardiovascular health.'
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Proteins (2)

ProteinDefinitionTaxonomy
Cell division control protein 42 homologA cell division control protein 42 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P60953]Homo sapiens (human)
Oxysterols receptor LXR-betaAn oxysterols receptor LXR-beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P55055]Homo sapiens (human)

Compounds (32)

CompoundDefinitionClassesRoles
fasudilfasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia.

fasudil: intracellular calcium antagonist; structure in first source
isoquinolines;
N-sulfonyldiazepane
antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent
ketorolac5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively.

ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.

Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)
amino acid;
aromatic ketone;
monocarboxylic acid;
pyrrolizines;
racemate
analgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
4-chlorophenol4-chlorophenol : A monochlorophenol substituted at the pare position by a chlorine atom.

4-chlorophenol: used as a root canal irrigant
monochlorophenol
butylparabenorganic molecular entity
3-chlorophenol3-chlorophenol : A monochlorophenol carrying the chloro substituent at position 3.monochlorophenol
4-phenoxyphenolphenoxyphenol
bis(4-oxyphenyl)sulfide4,4'-thiodiphenol: structure in first sourcephenols
1-deoxynojirimycin1-deoxy-nojirimycin: structure in first source

duvoglustat : An optically active form of 2-(hydroxymethyl)piperidine-3,4,5-triol having 2R,3R,4R,5S-configuration.
2-(hydroxymethyl)piperidine-3,4,5-triol;
piperidine alkaloid
anti-HIV agent;
anti-obesity agent;
bacterial metabolite;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
hepatoprotective agent;
hypoglycemic agent;
plant metabolite
betulinic acidhydroxy monocarboxylic acid;
pentacyclic triterpenoid
anti-HIV agent;
anti-inflammatory agent;
antimalarial;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
plant metabolite
sanguinarine chloride
chelerythrine chloride
bexarotenebenzoic acids;
naphthalenes;
retinoid
antineoplastic agent
podocarpic acidpodocarpic acid : An abietane diterpenoid lacking the isopropyl substituent with an aromatic C-ring and a hydroxy group at the 12-position.

podocarpic acid: structure
abietane diterpenoid
cyanidincyanidin cation : An anthocyanidin cation that is flavylium substituted at positions 3, 3', 4', 5 and 7 by hydroxy groups.

cyanidin: RN given refers to parent cpd; structure
5-hydroxyanthocyanidinantioxidant;
metabolite;
neuroprotective agent
(22r)-22-hydroxycholesterol(22R)-22-hydroxycholesterol : An oxysterol that is the 22R-hydroxy derivative of cholesterol.22-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid;
oxysterol
2-chloro-1,4-dimethoxybenzenedimethoxybenzene
gw 3965GW 3965: a liver X receptor liganddiarylmethane
t0901317T0901317: an LXRalpha and LXRbeta agonist
alitretinoinAlitretinoin: A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA.retinoic acidantineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist
2-[[benzamido(sulfanylidene)methyl]amino]-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acidCID1067700: a pan-GTPase inhibitor; structure in first sourcethienopyran
24,25-epoxycholesterol24,25-epoxycholesterol: Rn given refers to (3alpha,5beta)-isomer; structure given in first source

24(S),25-epoxycholesterol : A 3beta-hydroxy-Delta(5)-steroid that is desmosterol in which the double bond at position 24-25 has been oxidised to the corresponding epoxide (the 24S diastereoisomer). It is an oxysterol agonist of the liver X receptor.
3beta-hydroxy-Delta(5)-steroid;
cholestanoid;
epoxy steroid
liver X receptor agonist
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
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
acanthoic acidacanthoic acid: from root bark of Acanthopanax koreanum; structure given in first source
y 27632, dihydrochloride, (4(r)-trans)-isomer
3-chloro-4-(3-(7-propyl-3-trifluoromethyl-6-benzisoxazolyl)propylthio)phenylacetic acid
riccardin criccardin C: isolated from liverworts; functions as a liver X receptor (LXR)alpha agonist and an LXRbeta antagonist; structure in first source
secramine asecramine A: inhibits VSVG transport from the Golgi to the plasma membrane; also inhibits Cdc42-dependent cell functions; structure in first source
bms 687453
way 2526232-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole: a partial LXR agonist
incb-018424nitrile;
pyrazoles;
pyrrolopyrimidine
antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
sr9238SR9238: liver-selective LXR inverse agonist that suppresses hepatic steatosis; structure in first source