Target intelligence / Profile preview

Transforming Growth Factor Beta Receptor Type I (TGFBR1)

Target
TGFBR1
Molecular classification
Receptor, Transmembrane serine/threonine kinase
01

Overview

TGFBR1 is a transmembrane serine/threonine kinase receptor that plays a central role in the transforming growth factor-beta (TGF-β) signaling pathway. Upon ligand binding and activation by TGFBR2, TGFBR1 phosphorylates SMAD proteins, propagating signals into the cell to regulate cellular processes like proliferation, differentiation, and apoptosis. It has dual roles as tumor suppressor/promoter, and is implicated in various diseases, including Loeys-Dietz syndrome and cancer. Several small-molecule inhibitors target TGFBR1 kinase activity.

Other names
ALK5Activin A receptor type II-like kinase
02

Mechanism of action

Small-molecule inhibitors that target TGFBR1's kinase activity, preventing phosphorylation and activation of downstream signaling molecules such as SMADs.

03

Biological functions

Signal transductionCell proliferationDifferentiationApoptosisMotilityImmune homeostasisStem-cell self-renewalCell cycle arrest
04

Disease associations

Loeys-Dietz Syndrome Type IAortic Aneurysm SyndromeMultiple Self-Healing Squamous EpitheliomaCancerFibrotic diseases
05

Safety considerations

Context-dependent tumor suppressor/promoter roles requiring careful consideration in cancer therapy.Potential for off-target effects due to broad expression across various tissues.
06

Interacting drugs

GW788388

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