Page last updated: 2024-10-24

positive regulation of lipoprotein lipase activity

Definition

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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Proteins (2)

ProteinDefinitionTaxonomy
Oxysterols receptor LXR-alphaAn oxysterols receptor LXR-alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13133]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 (37)

CompoundDefinitionClassesRoles
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
25-hydroxycholesterol25-hydroxy steroid;
oxysterol
human metabolite
bexarotenebenzoic acids;
naphthalenes;
retinoid
antineoplastic agent
3 beta-hydroxy-delta 5-cholenic acidsteroid
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
(20s)-20-hydroxycholesterol20-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-hydroxycholesterolbiomarker;
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-hydroxycholesterolapoptosis inducer;
human metabolite;
mouse metabolite;
neuroprotective agent
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
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-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
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
piericidin apiericidin 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-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
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
bms 687453
way 2526232-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole: a partial LXR agonist
cholenic acid dimethylamidecholenic acid dimethylamide: binds LXRalpha receptor; structure in first source
incb-018424nitrile;
pyrazoles;
pyrrolopyrimidine
antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
glucopiericidin aglucopiericidin A: from Streptomyces pactum S48727 as co-metabolite of piericidin A(1); structure given in first source; glycoside antibiotic
gsk4112GSK4112: a Rev-erbalpha agonist; structure in first source
sr9009
sr9011SR9011: a REV-ERB agonist; structure in first source
sr9238SR9238: liver-selective LXR inverse agonist that suppresses hepatic steatosis; structure in first source