Drug intelligence / Profile preview

ΔRAF1-ERT

Development stage
Preclinical
Lead developer
Université de Montréal
Modality
Recombinant Proteins and Enzymes
Administration
Intratumoral
01

Overview

ΔRAF1-ERT is a tamoxifen-inducible, constitutively active fusion protein used as a research tool to study the MAPK/ERK signaling pathway. It comprises a truncated, constitutively active version of the RAF1 kinase (ΔRAF1) fused to a modified ligand-binding domain of the estrogen receptor (ERT). In the presence of tamoxifen or its metabolite 4-hydroxytamoxifen, the fusion protein becomes active, leading to the hyperactivation of downstream MEK and ERK kinases. In the context of pancreatic ductal adenocarcinoma (PDAC) research, ΔRAF1-ERT has been utilized to demonstrate that high levels of ERK signaling can induce cellular senescence and suppress tumor progression, suggesting a potential therapeutic strategy of restoring ERK-mediated tumor suppression in early-stage lesions.

Other names
deltaRAF1-ERTdeltaRAF-1-ERTdeltaRAF 1-ERTRAF1-ERTRAF-1-ERTRAF 1-ERT
02

Targets

RAF1 (c-Raf-1 (Y340D/Y341D))ESR1 (ERα)

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