Target type: biologicalprocess
Any process that activates or increases the activity of the enzyme lipoprotein lipase. [GOC:ai]
Positive regulation of lipoprotein lipase (LPL) activity is a complex biological process involving multiple steps and regulatory mechanisms. LPL is an enzyme that hydrolyzes triglycerides in lipoproteins, releasing free fatty acids that can be taken up by tissues. This process is crucial for lipid metabolism and energy homeostasis.
**Regulation of LPL activity occurs at several levels:**
**1. Transcriptional Regulation:**
* **Insulin:** Insulin stimulates LPL transcription and expression in various tissues, particularly adipose tissue.
* **Peroxisome proliferator-activated receptor (PPAR) alpha:** PPARalpha agonists, such as fibrates, enhance LPL expression and activity.
* **Hormone sensitive lipase (HSL):** HSL, an enzyme involved in triglyceride breakdown, regulates LPL expression in adipose tissue.
**2. Post-translational Modification:**
* **Phosphorylation:** LPL activity can be regulated by phosphorylation at specific residues. Insulin promotes LPL phosphorylation, leading to increased activity.
* **Glycosylation:** Glycosylation modifications can influence LPL stability and activity.
**3. Cellular Localization and Transport:**
* **LPL is synthesized in the liver and secreted into the blood.**
* **It binds to heparan sulfate proteoglycans (HSPG) on the surface of endothelial cells in capillaries.** This binding is essential for LPL activity and allows it to interact with lipoproteins.
* **Lipoprotein lipase can be internalized and degraded by endothelial cells.** This process regulates LPL activity and prevents excessive accumulation of LPL on the endothelial surface.
**4. Interaction with Lipoproteins:**
* **LPL hydrolyzes triglycerides in chylomicrons and very low-density lipoproteins (VLDL).** This process generates free fatty acids and glycerol.
* **The activity of LPL is influenced by the composition and structure of lipoproteins.** For instance, high levels of apolipoprotein C-III can inhibit LPL activity.
**5. Feedback Mechanisms:**
* **Free fatty acids released by LPL activity can feedback and regulate LPL expression and activity.** This feedback loop helps to maintain lipid homeostasis.
In summary, positive regulation of lipoprotein lipase activity is a multifaceted process involving transcriptional, post-translational, and cellular mechanisms. This regulation is critical for maintaining proper lipid metabolism and energy balance in the body.'
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Protein | Definition | Taxonomy |
---|---|---|
Oxysterols receptor LXR-alpha | An oxysterols receptor LXR-alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13133] | Homo sapiens (human) |
Oxysterols receptor LXR-beta | An oxysterols receptor LXR-beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P55055] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
4-chlorophenol | 4-chlorophenol : A monochlorophenol substituted at the pare position by a chlorine atom. 4-chlorophenol: used as a root canal irrigant | monochlorophenol | |
butylparaben | organic molecular entity | ||
3-chlorophenol | 3-chlorophenol : A monochlorophenol carrying the chloro substituent at position 3. | monochlorophenol | |
4-phenoxyphenol | phenoxyphenol | ||
bis(4-oxyphenyl)sulfide | 4,4'-thiodiphenol: structure in first source | phenols | |
1-deoxynojirimycin | 1-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 acid | hydroxy 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 | |
25-hydroxycholesterol | 25-hydroxy steroid; oxysterol | human metabolite | |
bexarotene | benzoic acids; naphthalenes; retinoid | antineoplastic agent | |
3 beta-hydroxy-delta 5-cholenic acid | steroid | ||
podocarpic acid | podocarpic 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 | |
(20s)-20-hydroxycholesterol | 20-hydroxycholesterol : An oxysterol that is cholesterol substituted by a hydroxy group at position 20. 20-hydroxycholesterol: RN given refers to (20S)-isomer | 20-hydroxy steroid; 3beta-hydroxy-Delta(5)-steroid; oxysterol | human metabolite; mouse metabolite |
24-hydroxycholesterol | (24S)-24-hydroxycholesterol : A 24-hydroxycholesterol that has S configuration at position 24. It is the major metabolic breakdown product of cholesterol in the brain. | 24-hydroxycholesterol | biomarker; human blood serum metabolite; mouse metabolite |
27-hydroxycholesterol | (25R)-cholest-5-ene-3beta,26-diol : A 26-hydroxycholesterol in which the 25-position has R-configuration. | 26-hydroxycholesterol | apoptosis inducer; human metabolite; mouse metabolite; neuroprotective agent |
cyanidin | cyanidin 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-hydroxyanthocyanidin | antioxidant; 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 | |
22s-hydroxycholesterol | (22S)-22-hydroxycholesterol : An oxysterol that is the 22S-hydroxy derivative of cholesterol. | 22-hydroxy steroid; 3beta-hydroxy-Delta(5)-steroid; oxysterol | |
2-chloro-1,4-dimethoxybenzene | dimethoxybenzene | ||
gw 3965 | GW 3965: a liver X receptor ligand | diarylmethane | |
t0901317 | T0901317: an LXRalpha and LXRbeta agonist | ||
alitretinoin | Alitretinoin: 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 acid | antineoplastic agent; keratolytic drug; metabolite; retinoid X receptor agonist |
24,25-epoxycholesterol | 24,25-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 |
genistein | 7-hydroxyisoflavones | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; geroprotector; human urinary metabolite; phytoestrogen; plant metabolite; tyrosine kinase inhibitor | |
piericidin a | piericidin A : A member of the class of monohydroxypyridines that acts as an irreversible mitochondrial Complex I inhibitor that strongly associates with ubiquinone binding sites in both mitochondrial and bacterial forms of NADH:ubiquinone oxidoreductase piericidin A: pyridine-substituted fatty alcohol antibiotic; minor descriptor (75-85); on-line & Index Medicus search ANTIBIOTICS (75-85); RN given refers to (S-(R*,R*-(all-E)))-isomer | aromatic ether; methylpyridines; monohydroxypyridine; secondary allylic alcohol | antimicrobial agent; bacterial metabolite; EC 1.6.5.3 [NADH:ubiquinone reductase (H(+)-translocating)] inhibitor; mitochondrial respiratory-chain inhibitor |
pregna-4,17-diene-3,16-dione | pregna-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 receptor | 3-hydroxy steroid | androgen |
acanthoic acid | acanthoic acid: from root bark of Acanthopanax koreanum; structure given in first source | ||
3-chloro-4-(3-(7-propyl-3-trifluoromethyl-6-benzisoxazolyl)propylthio)phenylacetic acid | |||
riccardin c | riccardin C: isolated from liverworts; functions as a liver X receptor (LXR)alpha agonist and an LXRbeta antagonist; structure in first source | ||
bms 687453 | |||
way 252623 | 2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole: a partial LXR agonist | ||
cholenic acid dimethylamide | cholenic acid dimethylamide: binds LXRalpha receptor; structure in first source | ||
incb-018424 | nitrile; pyrazoles; pyrrolopyrimidine | antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | |
glucopiericidin a | glucopiericidin A: from Streptomyces pactum S48727 as co-metabolite of piericidin A(1); structure given in first source; glycoside antibiotic | ||
gsk4112 | GSK4112: a Rev-erbalpha agonist; structure in first source | ||
sr9009 | |||
sr9011 | SR9011: a REV-ERB agonist; structure in first source | ||
sr9238 | SR9238: liver-selective LXR inverse agonist that suppresses hepatic steatosis; structure in first source |