Palbociclib: Difference between revisions
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<StructureSection load='' size='340' side='right' caption=' | <StructureSection load='' size='340' side='right' caption='Palbociclib' scene='10/1001138/Cv/1'> | ||
Palbociclib, sold under the brand name Ibrance among others, is a medication developed by Pfizer for the treatment of HR-positive and HER2-negative breast cancer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. <ref name="a2">PMID:19874578</ref><ref name="a3">PMID:24369047</ref> | Palbociclib, sold under the brand name Ibrance among others, is a medication developed by Pfizer for the treatment of HR-positive and HER2-negative breast cancer. See also [https://en.wikipedia.org/wiki/Palbociclib Palbociclib]. It is a selective inhibitor of the [[cyclin-dependent kinases]] CDK4 and CDK6 (see also [[CDK4]]).<ref name="a2">PMID:19874578</ref><ref name="a3">PMID:24369047</ref> | ||
In the G1 phase of the cell cycle, mammalian cells must pass a checkpoint, known as the restriction point "R", in order to complete the cell cycle and divide. CDK4 and CDK6 complex with cyclin D drive the phosphorylation of the retinoblastoma protein, Rb, which allows the cell to pass R and commit to division. Regulation of one or more proteins involved in this checkpoint is lost in many cancers. However, by inhibiting CDK4/6, palbociclib ensures that the cyclin D-CDK4/6 complex cannot aid in phosphorylating Rb. This prevents the cell from passing R and exiting G1, and in turn from proceeding through the cell cycle.<ref name="a5">PMID:28438180</ref> | |||
<scene name='10/1001138/Overall/3'>The X-ray co-crystal structure of human CDK6 and Palbociclib</scene> ([[5l2i]]). | |||
<scene name='10/1001138/Binding_site/1'>Palbociclib binding site</scene>. | |||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||