Abemaciclib: Difference between revisions
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<StructureSection load='' size='340' side='right' caption=' | <StructureSection load='' size='340' side='right' caption='Abemaciclib' scene='10/1002442/Cv/1'> | ||
Abemaciclib, sold under the brand name Verzenio among others, is a medication for the treatment of advanced or metastatic breast cancers. It was developed by Eli Lilly and it acts as a CDK inhibitor selective for [[cyclin-dependent kinases]] CDK4 and CDK6.<ref name="a3">PMID:26264704</ref> See also [https://en.wikipedia.org/wiki/Abemaciclib Abemaciclib] and [[CDK4]]. | Abemaciclib, sold under the brand name Verzenio among others, is a medication for the treatment of advanced or metastatic breast cancers. It was developed by Eli Lilly and it acts as a CDK inhibitor selective for [[cyclin-dependent kinases]] CDK4 and CDK6.<ref name="a3">PMID:26264704</ref> See also [https://en.wikipedia.org/wiki/Abemaciclib Abemaciclib] and [[CDK4]]. | ||
Like the related drugs [[palbociclib]] and ribociclib, abemaciclib inhibits the enzymes [[cyclin-dependent kinase 4]] (CDK4) and cyclin-dependent kinase 6 (CDK6).<ref name="a7">"Highlights of Prescribing Information for Verzenio" (PDF). September 2017. Archived (PDF) from the original on 5 September 2021. Retrieved 22 November 2017</ref> These enzymes are responsible for phosphorylating and thus deactivating the retinoblastoma protein, which plays a role in cell cycle progression from the G1 (first gap) to the S (synthesis) phase.<ref name="a8">PMID:1655277</ref> Blocking this pathway prevents cells from progressing to the S phase, thereby inducing apoptosis (cell death).<ref name="a7">"Highlights of Prescribing Information for Verzenio" (PDF). September 2017. Archived (PDF) from the original on 5 September 2021. Retrieved 22 November 2017</ref> In vitro analysis using cancer cell lines, it is reported that abemaciclib induces non‐apoptotic cell death characterized by formation of cytoplasmic vacuoles derived from lysosomes. This result suggests that there may be a mechanism of action other than inhibition of a cyclin-dependent kinase.<ref name="a9">PMID:32304130</ref> | Like the related drugs [[palbociclib]] and [[ribociclib]], abemaciclib inhibits the enzymes [[Cyclin Dependent Kinase-4|cyclin-dependent kinase 4]] (CDK4) and cyclin-dependent kinase 6 (CDK6).<ref name="a7">"Highlights of Prescribing Information for Verzenio" (PDF). September 2017. Archived (PDF) from the original on 5 September 2021. Retrieved 22 November 2017</ref> These enzymes are responsible for phosphorylating and thus deactivating the retinoblastoma protein, which plays a role in cell cycle progression from the G1 (first gap) to the S (synthesis) phase.<ref name="a8">PMID:1655277</ref> Blocking this pathway prevents cells from progressing to the S phase, thereby inducing apoptosis (cell death).<ref name="a7">"Highlights of Prescribing Information for Verzenio" (PDF). September 2017. Archived (PDF) from the original on 5 September 2021. Retrieved 22 November 2017</ref> In vitro analysis using cancer cell lines, it is reported that abemaciclib induces non‐apoptotic cell death characterized by formation of cytoplasmic vacuoles derived from lysosomes. This result suggests that there may be a mechanism of action other than inhibition of a cyclin-dependent kinase.<ref name="a9">PMID:32304130</ref> | ||
<scene name='10/1002442/Overall/2'>The X-ray co-crystal structure of human CDK6 and Abemaciclib</scene> ([[5l2s]]). | <scene name='10/1002442/Overall/2'>The X-ray co-crystal structure of human CDK6 and Abemaciclib</scene> ([[5l2s]]). | ||
<scene name='10/1002442/Binding_site/1'>Abemaciclib binding site</scene>. Water molecule is shown as red sphere. | |||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||