Amastatin Explained

Amastatin, also known as 3-amino-2-hydroxy-5-methylhexanoyl-L-valyl-L-valyl-L-aspartic acid, is a naturally occurring, competitive and reversible aminopeptidase inhibitor that was isolated from Streptomyces sp. ME 98-M3.^[1] It specifically inhibits leucyl aminopeptidase, alanyl aminopeptidase (aminopeptidase M/N), bacterial leucyl aminopeptidase (Aeromonas proteolytica aminopeptidase), leucyl/cystinyl aminopeptidase (oxytocinase/vasopressinase),^[2] and, to a lesser extent, glutamyl aminopeptidase (aminopeptidase A),^[3] as well as other aminopeptidases.^[4] It does not inhibit arginyl aminopeptidase (aminopeptidase B).^{[5] [6]} Amastatin has been found to potentiate the central nervous system effects of oxytocin and vasopressin in vivo.^[7] It also inhibits the degradation of met-enkephalin, dynorphin A, and other endogenous peptides.^[8]

See also

• Bestatin
• Pepstatin

Notes and References

1. Book: Buckingham J . Amastatins . Dictionary of Natural Products. https://books.google.com/books?id=1W0NUD42fA4C&pg=PA197. 2 December 1993. CRC Press. 978-0-412-46620-5. 197–.
2. Nakanishi Y, Nomura S, Okada M, Ito T, Katsumata Y, Kikkawa F, Hattori A, Tsujimoto M, Mizutani S . 6 . Immunoaffinity purification and characterization of native placental leucine aminopeptidase/oxytocinase from human placenta . Placenta . 21 . 7 . 628–634 . September 2000 . 10985965 . 10.1053/plac.2000.0564 .
3. Book: Schloss JV . Modern Aspects of Enzyme Inhibition with Particular Emphasis on Reaction-Intermediate Analogs and Other Potent, Reversible Inhibitors . Boger P, Sandmann G . Target Sites of Herbicide Action. https://books.google.com/books?id=eRGpF10Yj10C&pg=PA203 . 31 July 1989. CRC Press. 978-0-8493-4985-0. 203–.
4. Book: Scott T, Mercer EI . Concise Encyclopedia Biochemistry and Molecular Biology . registration . 1997 . Walter de Gruyter. 978-3-11-014535-9. 35–.
5. Book: Umezawa H . Small Molecular Immunomodifiers of Microbial Origin: Fundamental and Clinical Studies of Bestatin . 9 May 2014. Elsevier Science. 978-1-4831-9033-4. 10–.
6. Book: Drey CN . Beta and Higher Homologous Amino Acids. Barrett G . Chemistry and Biochemistry of the Amino Acids . https://books.google.com/books?id=gjLsCAAAQBAJ&pg=PA28 . 6 December 2012. Springer Science & Business Media. 978-94-009-4832-7. 28– . 10.1007/978-94-009-4832-7_3 .
7. Meisenberg G, Simmons WH . Amastatin potentiates the behavioral effects of vasopressin and oxytocin in mice . Peptides . 5 . 3 . 535–539 . 1984 . 6540873 . 10.1016/0196-9781(84)90083-4 . 3881661 .
8. Oka T, Hiranuma T, Liu XF, Ohgiya N, Iwao K, Matsumiya T . [Enkephalin-inactivating enzymes] . ja . Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica . 101 . 4 . 197–207 . April 1993 . 8390390 . 10.1254/fpj.101.4_197 . free .