Ibrutinib
From Proteopedia
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<scene name='99/997914/Overall/1'>Tyrosine-protein kinase BTK with Ibrutinib</scene> ([[5p9j]]). | <scene name='99/997914/Overall/1'>Tyrosine-protein kinase BTK with Ibrutinib</scene> ([[5p9j]]). | ||
| - | <scene name='99/997914/Binding_site/3'>Ibrutinib binding site</scene>. Water molecules are shown as red spheres. brutinib is a potent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK). The acrylamide group of ibrutinib forms a covalent bond with the cysteine residue C481 in the BTK active site, leading to sustained inhibition of BTK enzymatic activity. BTK is an important signalling molecule of the B-cell antigen receptor (BCR) pathway, which is plays a role in the pathogenesis of several B-cell malignancies including mantle cell lymphoma (MCL), diffuse large B-cell lymphoma (DLBCL), follicular lymphoma, and chronic lymphocytic leukemia (CLL). Preclinical studies have shown that ibrutinib effectively inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.</ref><ref name="a6">[https://www.ema.europa.eu/en/medicines/human/EPAR/imbruvica "Imbruvica EPAR".] European Medicines Agency (EMA). 8 July 2021. Retrieved 14 July 2021.</ref> | + | <scene name='99/997914/Binding_site/3'>Ibrutinib binding site</scene>. Water molecules are shown as red spheres. brutinib is a potent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK). The <scene name='99/997914/Covalent/1'>acrylamide group of ibrutinib forms a covalent bond with the cysteine residue C481 in the BTK active site</scene>, leading to sustained inhibition of BTK enzymatic activity. BTK is an important signalling molecule of the B-cell antigen receptor (BCR) pathway, which is plays a role in the pathogenesis of several B-cell malignancies including mantle cell lymphoma (MCL), diffuse large B-cell lymphoma (DLBCL), follicular lymphoma, and chronic lymphocytic leukemia (CLL). Preclinical studies have shown that ibrutinib effectively inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.</ref><ref name="a6">[https://www.ema.europa.eu/en/medicines/human/EPAR/imbruvica "Imbruvica EPAR".] European Medicines Agency (EMA). 8 July 2021. Retrieved 14 July 2021.</ref> |
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 13:20, 8 October 2023
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References
- ↑ "Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated". DailyMed. 8 April 2020. Retrieved 21 April 2020.
- ↑ 2.0 2.1 "Imbruvica EPAR". European Medicines Agency (EMA). 8 July 2021. Retrieved 14 July 2021.
