Drug intelligence / Profile preview

PEA-15-DD

Development stage
Preclinical
Lead developer
University of Texas MD Anderson Cancer Center
Modality
Recombinant Proteins and Enzymes
Administration
Intraperitoneal
01

Overview

PEA-15-DD is a phosphomimetic mutant of the 15-kDa phosphoprotein PEA-15 (Phosphoprotein Enriched in Astrocytes-15). In this variant, the two primary serine phosphorylation sites, Serine 104 and Serine 116, are substituted with aspartic acid (D) to simulate a constitutively double-phosphorylated state. Research conducted at the UT MD Anderson Cancer Center has utilized PEA-15-DD as a comparative tool to investigate the role of PEA-15 phosphorylation in cancer progression. While the unphosphorylated mutant (PEA-15-AA) exhibits potent antitumor activity by sequestering phospho-ERK in the cytoplasm and inhibiting beta-catenin signaling, the PEA-15-DD form is associated with pro-tumorigenic phenotypes and is the predominant form found in high-grade ovarian tumor tissues. In preclinical models, PEA-15-DD failed to inhibit tumor formation, contrasting with the therapeutic potential observed in the unphosphorylated PEA-15-AA variant.

Other names
double-phosphorylated PEA-15 mutantPEA-15 S104D/S116Dphosphomimetic PEA-15
02

Targets

RPS6KA3 (RSK2)Fas-associated death domain protein/Caspase-8 complexMAPK3 (Mitogen-activated protein kinase 1)

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