Target intelligence / Profile preview

Intestinal endothelium receptors

Molecular classification
Receptor, Cell adhesion molecule, G protein-coupled receptor, Enzyme
01

Overview

Intestinal endothelium receptors refer to a diverse group of cell surface proteins expressed on the vascular lining of the gastrointestinal tract that mediate critical physiological processes such as leukocyte homing, vascular permeability, and vasomotor control. In the upper gastrointestinal tract (esophagus and stomach), the endothelial receptor profile is distinct from the lower tract; for instance, the mucosal addressin cell adhesion molecule 1 (MAdCAM-1) is predominantly expressed in the small and large intestine, while vascular cell adhesion molecule 1 (VCAM-1) and intercellular adhesion molecule 1 (ICAM-1) serve as the primary mediators of inflammation-induced leukocyte recruitment in the upper GI. Additionally, the endothelin system (ET-A and ET-B receptors) and somatostatin receptors (notably SSTR2) play significant roles in regulating blood flow and smooth muscle motility throughout the upper GI tract. These receptors are major therapeutic targets in inflammatory conditions like Crohn's disease and eosinophilic esophagitis, as well as in vascular disorders like portal hypertension and gastrointestinal bleeding. Drugs targeting these receptors, such as integrin inhibitors, endothelin antagonists, and somatostatin analogs, aim to modulate the immune response or improve regional hemodynamics.

Other names
Gut vascular receptorsGastrointestinal endothelial receptorsMucosal addressin cell adhesion molecule 1 (MAdCAM-1)Vascular cell adhesion molecule 1 (VCAM-1)Intercellular adhesion molecule 1 (ICAM-1)Endothelin receptors (ETA and ETB)Somatostatin receptor 2 (SSTR2)Angiotensin-converting enzyme 2 (ACE2)
02

Mechanism of action

Blockade of leukocyte-endothelial interactions (e.g., α4β7-MAdCAM-1 binding) to reduce inflammation; Antagonism of endothelin receptors to modulate vascular resistance; Activation of somatostatin receptors to induce splanchnic vasoconstriction; Viral spike protein binding to ACE2 for cellular entry.

03

Biological functions

Leukocyte traffickingVascular permeabilityVasomotor tone regulationImmune cell recruitmentViral entry
04

Disease associations

Inflammatory bowel diseaseCrohn's diseaseEosinophilic esophagitisGastritisPortal hypertensionCOVID-19
05

Safety considerations

Increased risk of opportunistic infectionsPotential for progressive multifocal leukoencephalopathy (PML)HepatotoxicityFluid retentionBradycardia
06

Interacting drugs

Vedolizumab

7 more in the full profile.

07

Biomarkers

Soluble MAdCAM-1Soluble VCAM-1Endothelin-1 levelsFecal calprotectin

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