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Chemical compound
Aminopterin (or 4-aminopteroic acid), the 4–amino derivative of folic acid, is an antineoplastic drug with immunosuppressive properties often used in chemotherapy. Aminopterin is a synthetic derivative of pterin. Aminopterin works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase. Its binding affinity for dihydrofolate reductase effectively blocks tetrahydrofolate synthesis. This results in the depletion of nucleotide precursors and inhibition of DNA, RNA, and protein synthesis.
It is classified as an extremely hazardous substance in the United States as defined in Section 302 of the U.S. Emergency Planning and Community Right-to-Know Act (42 U.S.C. 11002), and is subject to strict reporting requirements by facilities which produce, store, or use it in significant quantities.[1]
^"40 C.F.R.: Appendix A to Part 355—The List of Extremely Hazardous Substances and Their Threshold Planning Quantities" (PDF) (July 1, 2008 ed.). Government Printing Office. Archived from the original (PDF) on February 25, 2012. Retrieved October 29, 2011. {{cite journal}}: Cite journal requires |journal= (help)
Aminopterin (or 4-aminopteroic acid), the 4–amino derivative of folic acid, is an antineoplastic drug with immunosuppressive properties often used in...
(hypoxanthine-aminopterin-thymidine medium) is a selection medium for mammalian cell culture, which relies on the combination of aminopterin, a drug that...
therapeutic index of methotrexate was better than that of aminopterin, and clinical use of aminopterin was thus abandoned in favor of methotrexate.[citation...
Network. On 23 March, the New York State Food Laboratory reported that aminopterin was found in samples sent to them by Cornell. Michigan State University...
leukemias. Realizing this, he attempted to use a folate antagonist, aminopterin, to block the function of folic acid in patients with leukemia in hopes...
are incubated in HAT medium (hypoxanthine-aminopterin-thymidine medium) for roughly 10 to 14 days. Aminopterin blocks the pathway that allows for nucleotide...
is supplemented with hypoxanthine, aminopterin and thymidine, hence the name HAT medium. Antimetabolite aminopterin blocks the cellular biosynthesis of...
de novo purine synthesis pathway is also disrupted. Exposing cells to aminopterin (a folic acid analogue which inhibits dihydrofolate reductase) makes...
Yellapragada Subbarow of Lederle Laboratories. These analogues — first aminopterin and then amethopterin (now methotrexate) were antagonistic to folic acid...
Subbarow, known for the synthesis of the first ever chemotherapeutic drug aminopterin, and subsequently methotrexate. He is also known for the synthesis of...
Guelph in Ontario, identified contaminants in some of the recalled food: aminopterin, melamine, and cyanuric acid. If consumed by themselves, isolated doses...
and children with acute lymphoblastic leukemia a folic acid inhibitor, aminopterin—10 showed improvement by clinical and hematologic parameters after three...
recommended when pregnancy is discovered during or before chemotherapy. Aminopterin, a cytostatic drug with antifolate effect, was used during the 1950s...
children produced by folic acid antagonist, 4-aminopteroyl-glutamic acid (aminopterin)". N. Engl. J. Med. 238 (23): 787–93. doi:10.1056/NEJM194806032382301...
Boston pathologist Sidney Farber believed from past experiments that aminopterin, a folic acid mimic, could potentially cure leukemia in children. The...
went on to make other major discoveries; including the synthesis of aminopterin (later developed into methotrexate), the first cancer chemotherapy. 1923:...
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