Acivicin
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Names | |
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IUPAC name
(2S)-Amino[(5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl]ethanoic acid
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Other names
Antibiotic AT 125
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Identifiers | |
42228-92-2 | |
ChEBI | CHEBI:74545 |
ChEMBL | ChEMBL1231101 |
ChemSpider | 259938 |
Jmol 3D model | Interactive image |
PubChem | 294641 |
UNII | O0X60K76I6 |
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Properties | |
C5H7ClN2O3 | |
Molar mass | 178.574 |
Vapor pressure | {{{value}}} |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references | |
Acivicin is an inhibitor of gamma-glutamyl transferase. It is fermented product of Streptomyces sviceus and has promise as an antineoplastic agent.[1] It interferes with glutamate metabolism and inhibits glutamate dependent synthesis of enzymes, and is thereby potentially helpful in treatment of solid tumors.[2]
Research
An in vitro study showed that Acivicin at a concentration of 5 µM Acivicin inhibited by 78% the growth of human pancreatic carcinoma cells (MIA PaCa-2) after 72 hours in continuous culture. It was also found that acivicin at a concentration of 450 µM irreversibly inactivated MIA PaCa-2 γ-glutamyl transpeptidase (10 nmol/min/106 cells) with an inactivation half-life of 80 minutes.[1]
Phase I studies
Phase I dose escalating studies conducted in 23 cancer patients administered acivicin with a concomitant 96-h i.v. infusion of a mixture of 16 amino acids showed reversible, dose-limiting CNS toxicity, characterized by lethargy, confusion and decreased mental status.
References
External links
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- Experimental cancer drugs
- Amino acid derivatives
- Oxazolidines
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- Antineoplastic and immunomodulating drug stubs