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Transforming Growth Factor Beta Receptor II (Dominant Negative) (DN-TGFβRII)

Target: DN-TGFβRII
Molecular classification: Receptor, Transmembrane serine/threonine kinase

Overview

Transforming growth factor beta receptor II (TGFβRII) is a transmembrane serine/threonine kinase that forms part of the TGF-β receptor complex. The dominant negative form, DN-TGFβRII, lacks the intracellular kinase domain, acting as a competitive inhibitor of endogenous TGF-β signaling. By sequestering ligand or forming non-functional complexes with type I receptors, DN-TGFβRII blocks endogenous receptor-mediated signaling in cells expressing it. It has been explored for overcoming immunosuppression in tumors and dissecting TGFB pathway roles.

Other names: ΔTGFβRIIDN-TGFB-RII

Mechanism of action

Competitive inhibition/blockade of endogenous TGFB signaling by sequestering ligand or forming non-functional complexes with type I receptors.

Biological functions

Competitive inhibition of TGF-β signalingBlocks immunosuppressionEnhances anti-tumor immunityRegulates cell proliferationRegulates cell differentiationRegulates apoptosisImmune responseTissue remodelingHomeostasis

Disease associations

CancerImmune disordersFibrosis

Safety considerations

Systemic blockade can cause side effects due to loss of homeostatic regulation across multiple tissuesTargeted delivery/expression is critical for safety/efficacy

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