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CAAI

總結: Covalent-allosteric AKT inhibitors: high affinity inhibitors with A new mode of binding for cancer therapy.

技術優勢: AKT inhibitors with a new mode of action
The inhibitors bind AKT irreversibly and specifically with highest affinity

技術應用: AKT is a serine/threonine kinase and oncogene that has already been identified and addressed as a target in cancer therapy by several pharma companies. The invented substances are of high interest for any pharma company with an oncology pipeline and are of special advantage for those who seek to improve, broaden or supplement their kinase inhibitor portfolio.

詳細技術說明: To survive, cancer cells cluster extra centrosomes to achieve pseudo-bipolar division. The invention aims to prevent clustering of extra centrosomes by prematurely activating centrosomes to induce microtubule nucleation before mitotic onset. Tubulin, by interacting with the centrosomal Protein CPAP, negatively regulates CPAP-dependent peri-centriolar material recruitment and concurrently microtubule nucleation. Screening for compounds that perturb CPAP-tubulin interaction led to the identification of novel compounds, which selectively bind at the CPAP binding site of tubulin. These compounds prematurely activate extra centrosomes to nucleate microtubules causing cancer cells to undergo centrosome declustering, multipolar mitosis, prolonged mitotic arrest and cell death.

分類: - international:
C07D471/04
- cooperative:
A61P35/00; C07D471/04; G01N33/57484

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