Abiraterone acetate
From Proteopedia
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Abiraterone, the active metabolite of abiraterone acetate, inhibits Cytochrome P450 17A1 (CYP17A1), which manifests as two enzymes, 17α-hydroxylase (IC50 = 2.5 nM) and 17,20-lyase (IC50 = 15 nM) (approximately 6-fold more selective for inhibition of 17α-hydroxylase over 17,20-lyase)<ref name="a23">Neidle S (30 September 2013). Cancer Drug Design and Discovery. Academic Press. pp. 341–342. ISBN 978-0-12-397228-6.</ref><ref name="a24">PMID:29710837</ref> that are expressed in testicular, adrenal, and prostatic tumor tissues. See also [[Cytochrome P450]]. | Abiraterone, the active metabolite of abiraterone acetate, inhibits Cytochrome P450 17A1 (CYP17A1), which manifests as two enzymes, 17α-hydroxylase (IC50 = 2.5 nM) and 17,20-lyase (IC50 = 15 nM) (approximately 6-fold more selective for inhibition of 17α-hydroxylase over 17,20-lyase)<ref name="a23">Neidle S (30 September 2013). Cancer Drug Design and Discovery. Academic Press. pp. 341–342. ISBN 978-0-12-397228-6.</ref><ref name="a24">PMID:29710837</ref> that are expressed in testicular, adrenal, and prostatic tumor tissues. See also [[Cytochrome P450]]. | ||
| - | <scene name='97/978895/Cv/2'>Human steroidogenic cytochrome P450 17A1 mutant N52Y with inhibitor abiraterone</scene> ([[6wr1]]). | + | <scene name='97/978895/Cv/2'>Human steroidogenic cytochrome P450 17A1 mutant N52Y with inhibitor abiraterone</scene> ([[6wr1]]). |
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| + | <scene name='97/978895/Binding_site/1'>Abiraterone binding site</scene>. Water molecules are shown as red spheres. | ||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 13:53, 1 August 2023
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References
- ↑ "Abiraterone Acetate Monograph for Professionals". Drugs.com. Archived from the original on 6 May 2012. Retrieved 15 November 2019.
- ↑ "Zytiga- abiraterone acetate tablet, film coated". DailyMed. 13 June 2019. Archived from the original on 13 November 2014. Retrieved 15 November 2019.
- ↑ "Yonsa- abiraterone acetate tablet". DailyMed. 5 June 2018. Archived from the original on 13 August 2020. Retrieved 15 November 2019.
- ↑ Neidle S (30 September 2013). Cancer Drug Design and Discovery. Academic Press. pp. 341–342. ISBN 978-0-12-397228-6.
- ↑ Fernández-Cancio M, Camats N, Flück CE, Zalewski A, Dick B, Frey BM, Monné R, Torán N, Audí L, Pandey AV. Mechanism of the Dual Activities of Human CYP17A1 and Binding to Anti-Prostate Cancer Drug Abiraterone Revealed by a Novel V366M Mutation Causing 17,20 Lyase Deficiency. Pharmaceuticals (Basel). 2018 Apr 29;11(2):37. PMID:29710837 doi:10.3390/ph11020037
