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CAAI

总结

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

技术优势

AKT inhibitors with a new mode of action
The inhibitors bind AKT irreversibly and specifically with highest affinity

技术应用

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.

详细技术说明

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.

合作类型

Licensing

申请日期

03/05/2016 00:00:00

申请号码

EP20160720132 20160503

分类

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

其他

Patent application

ID号码

4410

国家/地区

德国