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pharmacology chemotherapy

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Question:

Mercaptopurine (6-MP) and Thioguanine (6-TG) inhibition of purine synthesis

Author: Suzuki



Answer:

A number of metabolic processes involving purine biosynthesis and interconversions are affected by the nucleotide analog, TIMP. Like adenosine monophosphate (AMP), guanosine monophosphate (GMP), and inosine monophosphate (IMP), TIMP can inhibit the first step of de novo purine-ring biosynthesis (catalyzed by glutamine phosphoribosyl pyrophosphate amidotransferase). TIMP also blocks the formation of AMP and xanthinuric acid from inosinic acid. Incorporation into nucleic acids: TIMP is converted to thioguanine monophosphate (TGMP), which after phosphorylation to di- and triphosphates can be incorporated into RNA. The deoxyribonucleotide analogs that are also formed are incorporated into DNA. This results in nonfunctional RNA and DNA.


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Suzuki
Suzuki