Target intelligence / Profile preview

Transforming Growth Factor Beta Receptor I (TGFBR1)

Target
TGFBR1
Molecular classification
Receptor, Serine/Threonine Kinase, Protein Kinase, Transmembrane protein
01

Overview

Transforming growth factor beta receptor I (TGFBR1), also known as activin A receptor type II-like kinase 5 (ALK-5), is a membrane-bound serine/threonine protein kinase and a key component of the TGF-beta receptor family. It plays a central role in mediating cellular responses to members of the transforming growth factor beta (TGF-β) superfamily, which are multifunctional cytokines involved in regulating cell proliferation, differentiation, apoptosis, and other critical processes. Upon ligand binding, TGFBR1 propagates intracellular signaling by phosphorylating downstream effectors such as R-Smad proteins. Dysregulation can contribute to diseases such as cancer progression or fibrotic disorders. Mutations in TGFBR1 are associated with Loeys–Dietz syndrome.

Other names
ALK-5Activin A Receptor Type II-Like Kinase 5Activin A Receptor Type II-Like Kinase
02

Mechanism of action

Small-molecule inhibitors targeting TGFBR1 kinase activity, blocking downstream signaling.

03

Biological functions

Signal transductionCell proliferationCell differentiationApoptosisImmune system regulationWound healingTranscriptional regulation
04

Disease associations

CancerLoeys-Dietz syndromeFibrotic disordersAortic aneurysm
05

Interacting drugs

GW788388

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