Target intelligence / Profile preview

BMP-binding endothelial regulator protein (BMPER)

Target
BMPER
Molecular classification
Secreted glycoprotein (extracellular matrix protein), Extracellular modulator of signaling, BMP antagonist/agonist (depending on context), Other (does not fit into classical receptor/transporter/enzyme families)
01

Overview

BMP-binding endothelial regulator protein (BMPER) is a secreted extracellular matrix glycoprotein expressed by endothelial cell precursors and mature endothelial cells. It contains five cysteine-rich domains, a von Willebrand D domain, and a trypsin inhibitor domain, and is orthologous to Drosophila crossveinless-2. BMPER directly binds BMP2, BMP4, and BMP6, and finely tunes their signaling in a highly context-dependent manner, acting as either an antagonist or agonist of BMP-mediated Smad1/5 activation. It plays a vital role in blood vessel formation, endothelial cell migration, embryonic vascular development, and also interacts with metabolic and insulin signaling pathways. BMPER modulates angiogenesis by dose-dependent regulation of BMP activity and is considered a potential therapeutic target for vascular diseases and metabolic disorders[1][2][3][4][5].

Other names
BMPERKIAA1965hCV2Cv2CRIM3Bone morphogenetic protein-binding endothelial cell precursor-derived regulatorProtein crossveinless-2crossveinless-2CV-2CV2BMP-binding endothelial regulator precursor protein
02

Mechanism of action

Not applicable, as no direct drugs targeting BMPER are reported or approved. Existing research focuses on BMPER modulation of BMP ligands and their receptors.

03

Biological functions

Angiogenesis (promotes endothelial sprouting and migration in a dose-dependent manner)Embryonic vascular development (essential for developmental patterning and endothelial cell precursor differentiation)Regulation of BMP signaling (modulates BMP2, BMP4, BMP6 function, can antagonize or promote BMP signaling depending on context)Regulation of insulin signaling (direct activation, related to metabolic tissue function)
04

Disease associations

Cardiovascular disease (implicated in vascular development and homeostasis, dysregulation may affect vascular integrity and remodeling)Metabolic disease (participates in insulin signaling and metabolic tissue function)Developmental disorders (mutations can lead to abnormal vascular/organ development)Other (role in cancer, but primarily based on regulation of endothelial function and angiogenesis)
05

Safety considerations

Therapeutic challenges likely include dose-dependent effects (can be both agonist and antagonist of BMP signaling), complexity of vascular/developmental outcomes, and potential for off-target effects in multiple organ systems
06

Interacting drugs

None currently approved or in clinical use as direct BMPER modulators
07

Biomarkers

BMPER expression/activity has been studied as a marker for vascular precursor cell status and angiogenic activity in research settings

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