Target intelligence / Profile preview

Lipid droplet (LD)

Target
LD
Molecular classification
Organelle, Lipid-protein complex, Subcellular compartment
01

Overview

Lipid droplets are ubiquitous, dynamic organelles that serve as the primary storage site for neutral lipids, such as triacylglycerols and sterol esters, within eukaryotic cells. Once considered inert fat storage sacs, they are now recognized as metabolic hubs that interact with other organelles, including the endoplasmic reticulum and mitochondria, to regulate energy homeostasis and lipid signaling. They consist of a hydrophobic core surrounded by a phospholipid monolayer decorated with various proteins, most notably the perilipin family. Dysregulation of lipid droplet dynamics is a hallmark of several metabolic disorders, including obesity, non-alcoholic fatty liver disease (NAFLD/MASLD), and atherosclerosis, as well as certain cancers where they support rapid proliferation and stress resistance. Pharmacological targeting of lipid droplets often involves modulating the enzymes responsible for lipid synthesis (such as DGAT) or breakdown (such as ATGL), aiming to resolve pathological lipid accumulation or mobilize energy reserves in metabolic and oncological contexts.

Other names
AdiposomeOil bodySpherosomeFat bodyLipid body
02

Mechanism of action

Inhibition of triacylglycerol synthesis (e.g., DGAT1/2 inhibitors), modulation of lipolysis (e.g., ATGL or HSL inhibition), stimulation of lipophagy, and disruption of lipid droplet-associated protein function (e.g., Perilipin modulation).

03

Biological functions

Lipid storageEnergy homeostasisLipid metabolismProtein sequestrationMembrane traffickingCellular stress responseLipotoxicity protection
04

Disease associations

ObesityNon-alcoholic fatty liver disease (NAFLD)Metabolic-associated steatotic liver disease (MASLD)Type 2 diabetesAtherosclerosisCancerNeurodegenerative diseaseHepatitis C infection
05

Safety considerations

Systemic lipid dysregulationLipotoxicity in non-adipose tissuesGastrointestinal distress (common with DGAT inhibitors)Potential disruption of steroid hormone synthesisImpact on lipid-soluble vitamin absorption
06

Interacting drugs

Pradigastat

5 more in the full profile.

07

Biomarkers

Perilipin 2 (PLIN2/Adipophilin) expressionIntracellular triacylglycerol levelsLipid droplet diameter/number (via microscopy)Perilipin 1 (PLIN1) levelsCIDE family proteins

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