Target intelligence / Profile preview

Oxysterol-binding protein 1 (OSBP)

Target
OSBP
Molecular classification
Lipid transporter, Lipid-binding protein, Non-vesicular lipid transfer protein, Other
01

Overview

Oxysterol-binding protein 1 (OSBP) is a cytosolic lipid-transfer protein that acts as a key mediator of non-vesicular lipid transport, primarily moving cholesterol and oxysterols between the endoplasmic reticulum and Golgi membranes[9][3][6]. OSBP contains a central oxysterol-binding protein-related domain (ORD), which harbors a hydrophobic cavity suited for binding oxysterols, cholesterol, and specific phospholipids, as well as the ability to bind certain phosphoinositides[3][1]. OSBP regulates cellular sterol and sphingolipid metabolism, impacting membrane composition and signaling at membrane contact sites[6][9]. Dysregulation of OSBP function is linked to diseases such as cancer and cardiovascular disease, though OSBP itself is not a classical receptor but rather functions as a key lipid transporter and sensor[4][7]. Experimental OSBP inhibitors, while promising as research tools and in early-stage drug discovery, present challenges due to their potential to disrupt fundamental lipid regulatory networks essential for cellular physiology.

Other names
Oxysterol binding proteinOSBPOSBP1oxysterol-binding protein 1
02

Mechanism of action

Inhibitors of OSBP block non-vesicular lipid/sterol trafficking between endoplasmic reticulum (ER) and Golgi, disrupting lipid homeostasis, leading to altered signaling and cellular function[8].

03

Biological functions

Lipid transport (especially sterols and phospholipids)Regulation of lipid/cholesterol homeostasisModulation of membrane contact sitesCeramide and sphingomyelin metabolismSignal transductionOther
04

Disease associations

CancerCardiovascular diseaseOther (e.g., roles in lipid-associated metabolic disorders)
05

Safety considerations

Broad inhibition of OSBP may perturb essential sterol/lipid signaling and membrane traffickingPotential toxicity from disruption of cholesterol and phospholipid homeostasisTargeting OSBP may affect multiple organs due to its ubiquitous expression and crucial cellular roles
06

Interacting drugs

Itraconazole (identified as an inhibitor of OSBP)

3 more in the full profile.

07

Biomarkers

OSBP expression (in tissue, context-dependent, sometimes used as a research biomarker for cell or tissue lipid status)Changes in specific lipid species downstream of OSBP activity (e.g. changes in phosphatidylinositol-4-phosphate or sphingomyelin)

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