Target intelligence / Profile preview

Endothelial cell-specific molecule 1 (ESM1)

Target
ESM1
Molecular classification
Proteoglycan, Secreted glycoprotein, Other
01

Overview

Endothelial cell-specific molecule 1 (ESM1), also known as endocan, is a secreted, cysteine-rich dermatan sulfate proteoglycan highly expressed by endothelial cells, especially in the lung and kidney[4]. ESM1 is encoded by the *ESM1* gene on chromosome 5q11.2 and is regulated by cytokines and growth factors. It consists of a 20 kDa protein core (mature: 165 amino acids) and a dermatan sulfate glycosaminoglycan chain[1][2]. ESM1 plays a key role in the regulation of cell adhesion, migration, promoting angiogenesis, modulating inflammation, and influencing neutrophil and leukocyte trafficking via interaction with integrins and VE-cadherin. Overexpression and secretion of ESM1 are frequently observed in a variety of cancers, where it contributes to tumor growth, angiogenesis, enhanced metastasis, and therapy resistance by activating several signaling pathways (notably PI3K-Akt, NF-κB, VEGF-A/VEGFR-2, Wnt/β-catenin, and EMT). ESM1 is being studied as both a prognostic biomarker and a potential therapeutic target in oncology, inflammation, cardiovascular, and renal diseases[2][3][4][1].

Other names
EndocanESM-1endothelial cell specific molecule 1endothelial cell-specific molecule 1ESM 1
02

Mechanism of action

Anti-ESM1 antibodies may inhibit cancer cell proliferation, migration, angiogenesis, and metastasis via blocking PI3K/Akt, NF-κB, EMT, and VEGF/VEGFR-2 pathways[2][3]. Antisense oligonucleotides or other knockdown strategies reduce ESM1 expression, leading to inhibition of tumor progression and improved apoptosis[3].

03

Biological functions

Angiogenesis regulationCell adhesionCell migration and invasionEpithelial-mesenchymal transition (EMT)Regulation of cell proliferationModulation of inflammationImmune response modulation
04

Disease associations

Cancer (including cervical, lung, colorectal, gastric, breast, prostate, glioma, adrenocortical carcinoma, bladder)Cardiovascular diseaseInflammationRenal (kidney) diseaseHypertensionChronic renal failure
05

Safety considerations

Potential for disrupting normal endothelial and immune functions, given ESM1’s physiological roles in angiogenesis and inflammation[1][2][3].Targeting ESM1 may risk impairing wound healing, normal tissue angiogenesis, or immune cell trafficking.
06

Interacting drugs

None established in clinical use as of now; ESM1-targeting antibodies and antisense oligonucleotides are in experimental stages[1][2][3].
07

Biomarkers

Elevated ESM1 (endocan) levels are biomarkers for cancer progression (especially poor prognosis in cervical, colorectal, lung, gastric, breast, and other cancers)[3][4].Used as a prognostic marker for hypertension, transplant rejection, chronic renal failure, and some inflammatory or cardiovascular diseases[1][4].

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