By P. Roy-Burman Ph. D. (auth.), P. Roy-Burman Ph. D. (eds.)
The intent for the layout of structural analogues of a regular metabolite is that such compounds may perhaps intervene within the usage or functionality of the metabolite. A compound that's potent during this admire will be referred to as an antimetabolite. to achieve success in chemotherapy of bacterial, viral, or tumor progress, an antimetabolite should still adversely impact a few very important metabolic reactions within the parasite or parasitic tissue with out heavily endangering the host tissue. If a metabolic technique of the offending development isn't the same as that of the host, it really is most probably that the metabolism or job of a compound, structurally on the topic of a metabolite excited by that procedure, can be assorted in those cells. Such alterations are beneficial for devising powerful medications with selective activities. Sulfanilamide, a structural analogue of para aminobenzoic acid, interferes with the usage of this metabolite within the synthesis of folic acid, an important issue for progress. micro organism synthesize their very own folic acid and are incapable of using exogenously on hand folic acid. besides the fact that, the location is strictly contrary within the animal host. that's, animal tissues can't synthesize folic acid and are totally based upon exogenous resources. those changes in metabolism make attainable using sulfanilamide as a selective inhibitor of development. different antibacterial or antiparasitic medicinal drugs, similar to penicillin (BURCHALL, FERONE and HITCHINGS, 1965) and inhibitors of dihydrofolate reductase (HITCHINGS and BURCHALL, 1965; HITCHINGS, 1964; BURCHALL and HITCHINGS, 1965) have analogous fascinating selective toxicity effects.
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Extra info for Analogues of Nucleic Acid Components: Mechanisms of Action
However, certain mutants of Salmonella typhimurium resistant to aza-G exhibit loss of guanine and not of hypoxanthine phosphoribosyltransferase activity (KALLE and GOTS, 1961). If a single enzyme is also responsible for the conversions in these mutants, it is attractive to speculate that enzyme may be modified Purines 32 during exposure to the inhibitor so as to escape its inhibitory effects. In other words it may be possible that the new enzyme formed in the resistant cells accepts only hypoxanthine as substrate and does not accept guanine or its congener (aza-G).
14. Catabolic pathways of thio-G. Broken lines represent possible routes of conversion not definitely established (ELI ON, 1967) differences in these catabolic reactions in man and mouse. , 1962), while deamination and subsequent oxidation to thiouric acid occurs to only a small extent in man, but is the main pathway in the mouse (ELlON, 1967). Similar to the catabolism of 6-mercaptopurine, sulfate is a major end product in the degradative reactions of thio-G. The exact route of sulfate formation is not known.
Resistance: Studies with microorganisms, mouse neoplasms in vivo, and mammalian cells in culture have shown that cellular resistance to aza-G is associated with decreased conversion of the analogue to the ribonucleotide due to partial or complete loss of guanine-hypoxanthine phosphoribosyltransferase activity. Since the catalyzing activity is believed to be due to a single enzyme acting on both guanine and hypoxanthine, its loss blocks the formation of GMP and its analogue as well as IMP in the salvage pathway.