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Amorpha-4,11-diene
Amorpha-4,11-diene is a precursor to artemisinin Artemisinin () and its semisynthetic derivatives are a group of drugs used in the treatment of malaria due to '' Plasmodium falciparum''. It was discovered in 1972 by Tu Youyou, who shared the 2015 Nobel Prize in Physiology or Medicine for her .... See also * Amorpha-4,11-diene synthase References Sesquiterpenes ...
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Amorpha-4,11-diene Synthase
The enzyme amorpha-4,11-diene synthase (EC 4.2.3.24) (ADS) catalyzes the chemical reaction :(2''E'',6''E'')-farnesyl diphosphate ⇌ amorpha-4,11-diene + diphosphate This enzyme belongs to the family of lyases, specifically those carbon-oxygen lyases acting on phosphates. The systematic name of this enzyme class is (2''E'',6''E'')-farnesyl-diphosphate diphosphate-lyase (amorpha-4,11-diene-forming). This enzyme is also called amorphadiene synthase. This enzyme is mainly found in ''Artemisia annua'', a temperate Asian native flowering plant, and ADS catalyzes the first committed step in the antimalarial drug artemisinin synthesis. Enzyme Properties Physical Properties Amorpha-4,11-diene synthase is a 533 amino acid long protein with a molecular weight of 62.2 kDa and isoelectric point of 5.25. ADS shows a pH optimum at pH 6.5 and a minimum at pH 7.5. With Mg2+, Mn2+ and Co2+ as cofactors, large enzyme activity observed, with Ni2+, low activity observed, and with Cu2+ and ...
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Artemisinin
Artemisinin () and its semisynthetic derivatives are a group of drugs used in the treatment of malaria due to ''Plasmodium falciparum''. It was discovered in 1972 by Tu Youyou, who shared the 2015 Nobel Prize in Physiology or Medicine for her discovery. Artemisinin-based combination therapies (ACTs) are now standard treatment worldwide for ''P. falciparum'' malaria as well as malaria due to other species of ''Plasmodium''. Artemisinin is extracted from the plant ''Artemisia annua'', sweet wormwood, a herb employed in Chinese traditional medicine. A precursor compound can be produced using a genetically engineered yeast, which is much more efficient than using the plant. Artemisinin and its derivatives are all sesquiterpene lactones containing an unusual peroxide bridge. This endoperoxide 1,2,4-trioxane ring is responsible for their antimalarial properties. Few other natural compounds with such a peroxide bridge are known. Artemisinin and its derivatives have been used for the t ...
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