thioguanine sentence in Hindi
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- Thioguanine is catabolized ( broken down ) via two pathways.
- The thiopurines include thioguanine and mercaptopurine.
- Thioguanine is excreted primarily through the kidneys in urine, but mainly as a metabolite, 2-amino-6-methylthiopurine.
- Thioguanine cannot be demonstrated in cerebrospinal fluid, similar to the closely related compound 6-mercaptopurine which also cannot penetrate to the brain.
- TPMT is best known for its role in the metabolism of the thiopurine drugs such as azathioprine, 6-mercaptopurine and 6-thioguanine.
- Thioguanine is incorporated into human bone marrow cells, but like other thiopurines, it is not known to cross the blood-brain barrier.
- Thiopurine methyltransferase ( TPMT ) catalyzes the S-methylation of thiopurines, thereby regulating the balance between cytotoxic thioguanine nucleotide and inactive metabolites in hematopoietic cells.
- An additional effect may be derived from the incorporation of 6-thioguanine into RNA . This yields a modified RNA strand which cannot be read by the ribosomes.
- It is inhibited by Mycophenolic acid, ribavirin, and 6TGMP ( 6-thioguanine monophosphate ) . 6TGMP inhibition prevents purine interconversion and thus the synthesis of purine nucleotides.
- Thioguanine, like other thiopurines, is cytotoxic to white cells; as a result it is immunosuppressive at lower doses and anti-leukemic / anti-neoplastic at higher doses.
- The second pathway is the methylation of thioguanine to 2-amino-6-methylthiopurine, which is minimally effective as an anti-neoplastic and significantly less toxic than thioguanine.
- The second pathway is the methylation of thioguanine to 2-amino-6-methylthiopurine, which is minimally effective as an anti-neoplastic and significantly less toxic than thioguanine.
- Studies show that this protein provides resistance to thiopurine anticancer drugs, 6-mercatopurine and thioguanine, and the anti-HIV drug 9-( 2-phosphonylmethoxyethyl ) adenine.
- TPMT catalyzes the methylation of 6-mercaptopurine into the inactive metabolite 6-methylmercaptopurine-this methylation prevents mercaptopurine from further conversion into active, cytotoxic thioguanine nucleotide ( TGN ) metabolites.
- Thus, a cell lacking TK is resistant to bromodeoxyuridine ( BrdU ) and a cell lacking HGPRT is resistant to 6-thioguanine ( 6-TG ) and 8-azaguanine.
- However, the intra-cellular thio-nucleotide metabolites of thioguanine ( 6-TGN ) have longer half-lives and can therefore be measured after thioguanine is eliminated from the plasma.
- However, the intra-cellular thio-nucleotide metabolites of thioguanine ( 6-TGN ) have longer half-lives and can therefore be measured after thioguanine is eliminated from the plasma.
- Among these, albendazole, amoxicillin, amoxicillin-clavulanate, allopurinol, mercaptopurine, mupriocin, pyrimethamine, ranitidine, thioguanine, trimethoprim and zidovudine are listed on the World Health Organization's list of essential medications.
- The TPMT enzyme is responsible, in part, for the methylation of 6-MP into the inactive metabolite 6-methylmercaptopurine-this methylation prevents 6-MP from further conversion into active, cytotoxic thioguanine nucleotide ( TGN ) metabolites.
- The plasma half-life of thioguanine is short, due to the rapid uptake into liver and blood cells and conversion to 6-TGN . The median plasma half-life of 80-minutes with a range of 25 240 minutes.
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