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PROTACs suppression of CDK4/6, crucial kinases for cell cycle regulation in cancer

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Abstract

PROTACs based on two selective, FDA approved, CDK4/6 inhibitors were formed. One of them, based on palbociclib, potently initiates degradation of these CDK proteins, and suppresses phosphorylation of retinoblastoma protein (Rb) leading to cell cycle arrest. These PROTACs are active at nanomolar concentrations, and appear to be the first for CDK4/6.

Graphical abstract: PROTACs suppression of CDK4/6, crucial kinases for cell cycle regulation in cancer

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Publication details

The article was received on 07 Jan 2019, accepted on 06 Feb 2019 and first published on 13 Feb 2019


Article type: Communication
DOI: 10.1039/C9CC00163H
Citation: Chem. Commun., 2019, Advance Article

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    PROTACs suppression of CDK4/6, crucial kinases for cell cycle regulation in cancer

    B. Zhao and K. Burgess, Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9CC00163H

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