Studies of 2,5'-anhydro-3'-azido-3'-deoxythymidine (Meeting abstract). NLM AIDSLINE Important note: Information in this article was accurate in 1993. The state of the art may have changed since the publication date.

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Studies of 2,5'-anhydro-3'-azido-3'-deoxythymidine (Meeting abstract).

Proc Annu Meet Am Assoc Cancer Res; 34:A87 1993. Unique Identifier : AIDSLINE ICDB/93691070
Sun AS; Prusoff WH; Dept. of Pharmacology, Yale Univ. Sch. of Medicine, New Haven, CT; 06510

Abstract: 2,5'-Anhydro-3'-azido-3'-deoxythymidine (anAZT) has been reported to have antiviral activity against HIV-1 in cell culture and is converted to AZT and then thymine (thy) by a human liver homogenate (LH). The properties and purification of the factors involved in the degradation of anAZT are under study. Incubation of [2-14C]anAZT with a LH (in 0.1% Triton X-100) resulted in cleavage of the anhydro-linkage with identification of AZT and thy by HPLC. 88% of the activity was recovered in the 100,000 x g supernatant (S) with a 2-fold purification. Incubation of S with proteinase K, but not with DNase II, enhanced the reaction. Incubation with RNase A or lysozyme reduced the reaction slightly, and 0.1 N HCL or NaOH inactivated the reaction completely. Fractionation of S with 90% ethanol enhanced the activity in the supernatant, with more than 99% recovery and a 130-fold purification. Negligible activity was found in the precipitate. Pilot studies with Sephadex G50, G100 or G200 showed that about 100%, 45% or 10% of the activity was in the void vol, respectively. The factors, which catalyze the reaction, seem to be a macromolecule(s) with a mol wt larger than 100,000.
Keywords: Deoxyribonucleases/PHARMACOLOGY Ribonucleases/PHARMACOLOGY Serine Proteinases/PHARMACOLOGY Zidovudine/ISOLATION & PURIF/*METABOLISM ABSTRACTKWDdeoxyribonucleases/pharmacologyribonucleases/pharmacologyserineproteinases/pharmacologyzidovudine/isolation&purif/KWDmetabolismabstract
930730
M9371001

Copyright © 1993 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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