Target intelligence / Profile preview

Hormone-Sensitive Lipase (HSL)

Target
HSL
Molecular classification
Enzyme, Hydrolase
01

Overview

Hormone-sensitive lipase (HSL) is a key intracellular enzyme involved in lipid metabolism. It primarily catalyzes the hydrolysis of stored triglycerides, diglycerides, and monoglycerides within adipocytes and other tissues, releasing free fatty acids and glycerol. HSL also acts on cholesteryl esters and retinyl esters, contributing to cholesterol mobilization and vitamin A metabolism. HSL activity is tightly regulated by hormonal signals like catecholamines (activation) and insulin (inhibition), and its dysregulation is implicated in metabolic disorders such as obesity and type 2 diabetes.

Other names
LIPEtriacylglycerol lipasediacylglycerol lipasecholesteryl ester hydrolase
02

Mechanism of action

Drugs inhibit HSL activity to reduce free fatty acid release and improve insulin sensitivity.

03

Biological functions

LipolysisHydrolysis of triglyceridesHydrolysis of diglyceridesHydrolysis of monoglyceridesCholesteryl ester hydrolysisRetinyl ester hydrolysisCholesterol mobilizationFatty acid mobilization
04

Disease associations

ObesityType 2 diabetes mellitus (T2DM)Insulin resistanceMetabolic syndromeCardiovascular diseaseAbnormal fat accumulation
05

Safety considerations

Potential for dysregulation of normal fat mobilizationSide effects related to altering lipid metabolism
06

Biomarkers

Plasma-free fatty acid levels

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