Page last updated: 2024-10-24

bioactive lipid receptor activity

Definition

Target type: molecularfunction

Combining with a bioactive lipid and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. A bioactive lipid is a lipid for which changes in lipid levels result in functional consequences in a variety of cellular processes. [GOC:bf, GOC:mah, PMID:12215548, PMID:18216770]

Bioactive lipid receptor activity encompasses the ability of a protein to bind and respond to specific bioactive lipids, such as fatty acids, steroids, and eicosanoids. These lipids act as signaling molecules, triggering a cascade of downstream events that regulate various cellular processes.

The molecular function of bioactive lipid receptor activity involves several key steps:

1. **Lipid Binding:** The receptor protein possesses a specific binding site that recognizes and interacts with the bioactive lipid. This binding event is highly specific, ensuring that only the intended lipid molecule can activate the receptor.

2. **Conformational Change:** Upon binding, the receptor undergoes a conformational change, altering its shape and structure. This change is crucial for the receptor to initiate downstream signaling pathways.

3. **Signal Transduction:** The conformational change in the receptor activates intracellular signaling pathways. This can involve the recruitment of adaptor proteins, activation of kinases or phosphatases, or the generation of second messengers, such as cyclic AMP or calcium ions.

4. **Cellular Response:** The activated signaling pathways ultimately lead to specific cellular responses. These responses can include changes in gene expression, protein synthesis, cell proliferation, differentiation, migration, or apoptosis.

Bioactive lipid receptors play critical roles in numerous physiological processes, including:

- **Metabolism:** Regulating lipid metabolism, glucose homeostasis, and energy balance.
- **Inflammation:** Mediating inflammatory responses and immune system activation.
- **Growth and Development:** Controlling cell growth, differentiation, and development.
- **Neurotransmission:** Regulating synaptic transmission and neuronal signaling.
- **Cardiovascular function:** Influencing blood pressure, heart rate, and vascular tone.

Examples of bioactive lipid receptors include:

- **G protein-coupled receptors (GPCRs):** These receptors activate G proteins, leading to the production of second messengers. Examples include the receptors for prostaglandins, leukotrienes, and thromboxanes.
- **Nuclear receptors:** These receptors bind to DNA and regulate gene expression. Examples include the receptors for estrogens, androgens, and thyroid hormones.
- **Lipid kinases:** These enzymes phosphorylate lipids, altering their signaling properties. Examples include phosphatidylinositol 3-kinase (PI3K) and phospholipase C (PLC).

Understanding the molecular function of bioactive lipid receptor activity is crucial for developing novel therapies targeting lipid signaling pathways in various diseases.'
"

Proteins (2)

ProteinDefinitionTaxonomy
Probable G-protein coupled receptor 174A probable G-protein coupled receptor 174 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9BXC1]Homo sapiens (human)
Free fatty acid receptor 1A free fatty acid receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O14842]Homo sapiens (human)

Compounds (19)

CompoundDefinitionClassesRoles
lauric aciddodecanoic acid : A straight-chain, twelve-carbon medium-chain saturated fatty acid with strong bactericidal properties; the main fatty acid in coconut oil and palm kernel oil.medium-chain fatty acid;
straight-chain saturated fatty acid
algal metabolite;
antibacterial agent;
plant metabolite
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
16-hydroxypalmitic acid16-hydroxyhexadecanoic acid : An omega-hydroxy-long-chain fatty acid that is hexadecanoic acid (also known as palmitic acid) which is substituted at position 16 by a hydroxy group. It is a key monomer of cutin in the plant cuticle.hydroxypalmitic acid;
omega-hydroxy-long-chain fatty acid
plant metabolite
thiophenoxyacetic acidthiophenoxyacetic acid: structure
rosiglitazoneaminopyridine;
thiazolidinediones
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
12-hydroxydodecanoic acid12-hydroxylauric acid : A medium-chain fatty acid that is the 12-hydroxylated derivative of lauric acid.omega-hydroxy-medium-chain fatty acidhuman metabolite
3-hydroxydodecanoic acid3-hydroxydodecanoic acid: RN given refers to cpd without isomeric designation

3-hydroxylauric acid : A medium-chain fatty acid that is the 3-hydroxylated derivative of lauric acid; associated with fatty acid metabolic disorders.
3-hydroxy fatty acid;
medium-chain fatty acid
docosahexaenoateall-cis-docosa-4,7,10,13,16,19-hexaenoic acid : A docosahexaenoic acid having six cis-double bonds at positions 4, 7, 10, 13, 16 and 19.

docosahexaenoate : A polyunsaturated fatty acid anion that is the conjugate base of docosahexaenoic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.

docosahexaenoic acid : Any C22 polyunsaturated fatty acid containing six double bonds.

efalex: a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement
docosahexaenoic acid;
omega-3 fatty acid
algal metabolite;
antineoplastic agent;
Daphnia tenebrosa metabolite;
human metabolite;
mouse metabolite;
nutraceutical
ricinoleic acidricinoleic acid : A (9Z)-12-hydroxyoctadec-9-enoic acid in which the 12-hydroxy group has R-configuration..

ricinoleic acid: RN given refers to (R-(Z))-isomer; structure in Merck Index, 9th ed, #8005
(9Z)-12-hydroxyoctadec-9-enoic acid
linoleic acidlinoleic acid : An octadecadienoic acid in which the two double bonds are at positions 9 and 12 and have Z (cis) stereochemistry.

Linoleic Acid: A doubly unsaturated fatty acid, occurring widely in plant glycosides. It is an essential fatty acid in mammalian nutrition and is used in the biosynthesis of prostaglandins and cell membranes. (From Stedman, 26th ed)
octadecadienoic acid;
omega-6 fatty acid
algal metabolite;
Daphnia galeata metabolite;
plant metabolite
gamma-linolenic acidgamma-linolenic acid : A C18, omega-6 acid fatty acid comprising a linolenic acid having cis- double bonds at positions 6, 9 and 12.

gamma-Linolenic Acid: An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed)
linolenic acid;
omega-6 fatty acid
human metabolite;
mouse metabolite;
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
1-O-oleoyl-sn-glycero-3-phosphoserine1-O-oleoyl-sn-glycero-3-phosphoserine : A 1-acyl-sn-glycerophosphoserine compound having an oleoyl substituent at the 1-hydroxy position.1-acyl-sn-glycero-3-phosphoserine
gw9508GW9508: structure in first sourcearomatic amine
tak-875biphenyls
amg-837AMG-837: GPR40 agonist
tug-469TUG-469: a GPR40 agonist with antidiabetic activity; structure in first source
tug-891GPU-028: structure in first source
am 1638