A triple action CDK4/6-PI3K-BET inhibitor with augmented cancer cell cytotoxicity
| Autor: | Dhananjaya Pal, Guillermo A. Morales, Alok R. Singh, Tatiana G. Kutateladze, Adam M. Burgoyne, Kendra R. Vann, Donald L. Durden, Francisco M. Vega, Shweta Joshi, Aran B. Merati |
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| Přispěvatelé: | National Institutes of Health (US), Tower Cancer Research Foundation, Universidad de Sevilla. Departamento de Biología Celular |
| Rok vydání: | 2020 |
| Předmět: | |
| Zdroj: | Cell Discovery Cell Discovery, Vol 6, Iss 1, Pp 1-4 (2020) Digital.CSIC. Repositorio Institucional del CSIC instname idUS: Depósito de Investigación de la Universidad de Sevilla Universidad de Sevilla (US) idUS. Depósito de Investigación de la Universidad de Sevilla |
| Popis: | The PI3K-AKT-mTOR pathway has been at the center of anti-cancer drug development1,2, but targeted inhibition of PI3K kinase activity is proven to provide a limited therapeutic effect and is often followed by the development of resistance to the drug3. This limitation could in part be alleviated through concurrently inhibiting multiple pathological pathways characterized by synthetic lethality relationship. For example, beneficial effects in metastatic breast cancer are observed when inhibition of PI3K is combined with BET proteins inhibition4. While the need for combinations of single agent targeted therapies has become clear, this approach commonly requires dose reduction of the individual agents due to additive toxicity that may compromise efficacy5. This work was supported by the NIH grants CA192656 (D.L.D.), FD005113 (D.L.D., A.M.B.), GM135671 (T.G.K.), GM125195 (T.G.K.) and the Tower Cancer Research Foundation grant (A.M.B.). K.R.V. is a CFReT Fellow. |
| Databáze: | OpenAIRE |
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