Multikinase Degraders
The present invention discloses the synthesis of compounds that can degrade multiple kinases. The compounds have a promiscuous kinase binder warhead, which is linked to E3 ligase recruiting moiety. Such compounds can be tested in any cellular assays, and if there is an effect on the assay it is possible to identify kinases degradation of which causes the observed effect. For example such compounds can be tested in drug-resistant cells from cancer patients, and if any of the compounds is toxic it is highly likely that the observed toxicity is due to the degradation of protein kinases. Quantitative mass-spectrometry can be used to then discover degradation of which kinase is toxic to the drug resistant cells. Subsequently, selective degraders of that kinase can be designed for drug discovery purposes. As such the developed compounds are useful tools to identify kinases as drug targets, but compounds themselves can also be used as drugs, if the degradation of multiple kinases is desired to achieve the desired pharmacological effect. In addition, compounds can be used to quickly test if a particular kinase can be degraded by E3 ligase such as Cereblon, VHL or any other E3 ligase.
App Type | Case No. | Country | Patent/Publication No. | |
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Inquire | National Phase | 2019-053 | Canada | CN115246821A |