Abiraterone acetate: Difference between revisions
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<scene name='97/978895/Binding_site/1'>Abiraterone binding site</scene>. Water molecules are shown as red spheres. | <scene name='97/978895/Binding_site/1'>Abiraterone binding site</scene>. Water molecules are shown as red spheres. | ||
CYP17A1 catalyzes two sequential reactions: (a) the conversion of <scene name='97/978895/Pregnenolone/1'>pregnenolone</scene> and <scene name='89/895670/Cv/7'>progesterone</scene> (see also [[progesterone]]) to their 17α-hydroxy derivatives by its 17α-hydroxylase activity, and (b) the subsequent formation of <scene name='97/978895/Dehydroepiandrosterone/1'>dehydroepiandrosterone</scene> (DHEA) and androstenedione, respectively, by its 17,20-lyase activity.<ref name="a25">PMID:16287438</ref> DHEA and androstenedione are androgens and precursors of testosterone. Inhibition of CYP17A1 activity by abiraterone acetate thus decreases circulating levels of androgens such as DHEA, testosterone, and dihydrotestosterone (DHT). Abiraterone acetate, via abiraterone, has the capacity to lower circulating testosterone levels to less than 1 ng/dL (''i.e.'', undetectable) when added to castration.<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="a26">PMID:25311216</ref> | CYP17A1 catalyzes two sequential reactions: (a) the conversion of <scene name='97/978895/Pregnenolone/1'>pregnenolone</scene> and <scene name='89/895670/Cv/7'>progesterone</scene> (see also [[progesterone]]) to their 17α-hydroxy derivatives by its 17α-hydroxylase activity, and (b) the subsequent formation of <scene name='97/978895/Dehydroepiandrosterone/1'>dehydroepiandrosterone</scene> (DHEA) and <scene name='97/978895/Androstenedione/1'>androstenedione</scene>, respectively, by its 17,20-lyase activity.<ref name="a25">PMID:16287438</ref> DHEA and androstenedione are androgens and precursors of testosterone. Inhibition of CYP17A1 activity by abiraterone acetate thus decreases circulating levels of androgens such as DHEA, testosterone, and dihydrotestosterone (DHT). Abiraterone acetate, via abiraterone, has the capacity to lower circulating testosterone levels to less than 1 ng/dL (''i.e.'', undetectable) when added to castration.<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="a26">PMID:25311216</ref> | ||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||