Aug 28, 2024 · Introducing a novel PI3K PROTAC that effectively overcomes resistance to HER2-targeted therapy. Demonstrating the capability of the PI3K PROTAC to significantly enhance the sensitivity of lapatinib in HER2-positive breast cancer.

Aug 28, 2024 · In this study, we introduce a novel PI3K-p110α Proteolysis TAargeting Chimera (PROTAC) that effectively inhibits the proliferation of breast cancer cells by degrading PI3K-p110α.

Nov 1, 2024 · In brief, a selective and efficient PROTAC molecule was developed to induce the degradation of p110α and concurrent reduction of p85 proteins, providing a tool compound for the biological study of PI3K-α by blocking its enzymatic and non-enzymatic functions.

May 1, 2022 · PI3K kinase plays an important role in regulating key processes in cells, such as cell growth, metabolism, proliferation, and apoptosis. The overexpression of PI3K kinase exists in many cancers. The proteolytic target chimera (PROTAC) technology is a new technology that uses the ubiquitin-proteasome …

May 1, 2022 · PI3K kinase plays an important role in regulating key processes in cells, such as cell growth, metabolism, proliferation, and apoptosis. The overexpression of PI3K kinase exists in many cancers. The proteolytic target chimera (PROTAC) technology is a new technology that uses the ubiquitin–proteasome system to degrade a given target protein.

May 30, 2024 · To address this concern, we developed a proteolysis-targeting chimera (PROTAC) heterobifunctional molecule that specifically degrades PIK3CG and potently suppresses AML progression alone and in...

The PI3K pathway is a key regulatory hub for cell growth, survival, and metabolism. Activation of PI3K is a frequent hallmark of cancer, highlighted by the prevalence of somatic mutations in genes encoding key components of this pathway.

Jan 1, 2024 · We present here evidence that a high affinity binding module with the capacity to target all class I PI3K isoforms can facilitate selective degradation of the most frequently mutated class I isoform, PI3Kα, when incorporated into a cereblon-targeted (CRBN) degrader.

Proteolysis targeting chimera (PROTAC) is a novel technology that could be used to induce PI3K kinase degradation with cancer therapeutic potential. With extensive expertise and comprehensive platform, we provide PI3K-based PROTAC design services for drug development.

Recently, a PI3K-targeted phosphor-PROTAC (ErbB2 PP PI3K) has been successfully fabricated to degrade PI3K in breast cancer cell lines MDA-MB-175 and MDA-MB-231 through the inherent affinity of peptide targeting warheads with SH2 domain of PI3K 65, as the first reported p-PROTAC with confirmed in vivo activity and no acquired drug-resistant ...