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阿西维辛 Acivicin(GGT特异性抑制剂)  

2006-12-30 17:35:58|  分类: 化学试剂及生化 |  标签: |举报 |字号 订阅

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Acivicin
阿西维辛 Acivicin(GGT特异性抑制剂) - Solomon - 标准品生化试剂毒素酶试剂盒A specific inhibitor of gamma-glutamyl transpeptidase and transmembrane glutathione transport. It is a potent antitumor and antileishmania agent, and it induces apoptosis in human lymphoblastoid cells.
Cas No. 42228-92-2
Formula Wt.     178.57
Melting Point     209oC-211oC
Chemical Name     (2S)-2-amino-2-[(5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl]acetic acid
Purity             ≥98%                                 
Solubility     Soluble in water. Slightly soluble in methanol, ethanol or chloroform.
电话:13788991907   E-mail:电话@163.com提供                  Acivicin      10mg ,25mg ,100mg
Synonym          a-Amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid; ACIA
上海惠诚生物科技有限公司       TEL:021- 60498804 ,38920908,58374317
Acivicin is a heterocyclic analog of L-glutamate which was originally isolated from the fermentation products of Streptomyces sviceus.  Problems with byproducts in the large scale fermentation of acivicin led to a four year period where acivicin was not available to purchase.  LKT Labs has successfully synthesized a supply of acivicin and is currently the only supplier of this potent cancer chemotherapeutic.
Acivicin is a potent anti-cancer agent which demonstrated anti-tumor activity first in 1973 against L1210 and P388 mouse leukemia and human lung xenographs implanted in mice.  Originally acivicin was used to block DNA synthesis by inhibiting the transfer of the amido group from L-glutamine.  When it was tested in Phase I and II clinical trials patients suffered from multiple side effects which resulted in acivicin not being used in the clinic.
Rapidly proliferating tumor cells have elevated activities of γ-Glutamyl-transpeptidase (γ-GT), due to its involvement in the de novo biosynthesis of purine and pyrimidine nucleotides.  These elevated  levels help supplement the rapidly dividing cells with essential amino acid precursors for glutathione biosynthesis.  Several studies indicate that acivicin inhibits γ-GT and thereby reduces the glutathione levels in tumor cells.  Reduction of the glutathione levels would essentially starve the tumor cells of essential building blocks and result in cancer cell death.
In order to supply these essential building blocks γ-GT must first undergo a transformation from its inactive precursor to the active enzyme through an intramolecular autoprocessing event which is facilitated by threonine 308.  Acivicin acts as an irreversible inhibitor of this critical threonine residue in the active site of γ-GT and prevents γ-GT from converting to its active form.  Mechanistically, threonine 308 nucleophilically replaces the chlorine atom in acivicin through a tetrahedral intermediate which subsequently collapses to the inactive threonine-acivicin complex.  Extensive modeling studies have shown that this attack is facilitated by the backbone amides of Gly 472 and Gly 473, which would stabilize the developing negative charge on the nitrogen.
1.  Gamma Glutamyl Transpeptidase Activity and the Maintenance of Elevated Cysteine Levels in Cellular Carcinoma.  Patricia Ruoso, 2001. University of Toronto Masters Thesis.
2.  Crystal Structure of Acivicin-Inhibited γ-Glutamyltranspeptidase Reveals Critical Roles for Its C-Terminus in Autoprocessing and Catalysis.  Biochemistry, 2009, 48, 2459 – 2467.
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