TGFBR Pathway

TGFB a small secreted polypeptide signals through the type II serine/threonine kinase dimeric receptor (TGFBR2) that recruits and phosphorylates the type I dimeric receptor (TGFBR1). TGFBR1 phosphorylates and activates SMADs which are transcription factors regulating genes involved in cell proliferation, differentiation, apoptosis and growth. Many advanced stage cancers are known to over-express both the TGFB and TGFBR promoting aggressive tumor formation. Inhibiting the TGFB signaling pathway is a key therapeutic strategy in treating cancer.

Enable your therapeutic programs  by discovering small molecule inhibitors/ antibodies to TGFBR by using a robust, yet simple PathHunter® TGFBR1/TGFBR2 Dimerization Assay. These pre-validated assays offer ready-to-use cells and a simple screen-friendly protocol  to obtain sensitive and HTS data.


—Features and Benefits

  • Novel cell-based assay to uncover inhibitors of ligand induced receptor dimerization
  • Whole cell, chemiluminescent assay
  • Minimize false positives and toxicity with shorter compound incubation times

—Applications

  • Assay enables the study of:  small molecule receptor dimerization inhibitors, antibodies
  • Study compound toxicity profiles

Assay Principle

PathHunter® U2OS TGFBR1/TGFBR2 cell line feature novel in vivo applications of Enzyme Fragment Complementation (EFC) technology in which the β-galactosidase (β-gal) enzyme has been split into two inactive fragments. A small complementing fragment of β-gal, ProLink™ (PK) tag has been fused recombinantly to the TGFBR1. The larger portion of β-gal, termed EA for ‘enzyme acceptor’, is fused to the TGFBR2. Agonist binding to the TBFBR2 induces its heterodimerization with TGFBR1 forcing the complementation of PK with EA resulting in a fully complemented β-gal enzyme. Signal is measured quantitatively using the chemiluminescent substrate in the PathHunter® Detection Kit.

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