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Mercaptopurine - FDA prescribing information, side …

The effect of 6-mercaptopurine (6-MP) and its nucleoside and nucleotide derivatives on the rate of RNA synthesis with reticulocyte RNA-dependent RNA polymerase has been examined. Of the 6-MP derivatives tested only 6-mercaptopurine ribo-5′-monophosphate (6-MPR-P) significantly stimulates the rate of RNA synthesis with hemoglobin mRNA as a template while 6-MP and 6-MPR have little or no effect. Kinetic studies have demonstrated that 6-MPR-P activates the RNA-dependent RNA polymerase by increasing the Vmax of the enzyme rather than by decreasing the Km values for the substrates. It is suggested that the stimulation of RNA-dependent RNA synthesis by 6-MPR-P may explain the transient development of megaloblastic anemia following 6-MP therapy.

T1 - The effect of 6-mercaptopurine and its derivatives on mammalian RNA-dependent RNA synthesis

6-MP is very similar to the purine bases in . When used in DNA (copying), it prevents cell division. This also leads to inhibition of DNA synthesis and function, as 6-MP incorporates thiopurine nucleotides. 6-mercaptopurine (6-MP) causes remissions in childhood cases without severely harming normal cells.

Mercaptopurine 50 mg tablets - - (eMC) - Home - …

Title:Synthesis and In Vivo Antimalarial Activity of Novel Derivatives of 6- Mercaptopurine

Mohammed MH and Taher MA. Synthesis of new two derivatives of 6-mercaptopurine (6mp) 6-[5-pyridine-4-yl- 1, 2, 3, 4-oxadiazole-2-yl)dithiol]-9h-purine (38) and 9h-purine-6-yl-benyldithiocarbamate (45) with cytotoxicity results from the national cancer institute's anticancer drug screen. Int J Pharm Sci Res 2012; Vol. 3(8): 2613-2622

Mercaptopurine recipients may manifest decreased cellular hypersensitivities and decreased allograft rejection. Induction of immunity to infectious agents or vaccines will be subnormal in these patients; the degree of immunosuppression will depend on antigen dose and temporal relationship to drug. This immunosuppressive effect should be carefully considered with regard to intercurrent infections and risk of subsequent neoplasia.

Xaluprine 20 mg/ml oral suspension - - (eMC) - …

inhibition of nucleotide synthesis mercaptopurine, fluorouracil, methotrexate

What is known about the risks? ANSWER Azathioprine (AZA) is a cytotoxic antimetabolite that is used to inhibit purine synthesis, which is especially important for leukocytes and lymphocytes. After nonenzymatic reduction to 6-mercaptopurine, further metabolism occurs before thioguanine nucleotides are formed. Thioguanine nucleotides are responsible for inhibiting DNA synthesis, thus causing cytotoxicity to cells. Although anomalies occurred in rodents exposed to the drug in utero, AZA has not been identified as a human teratogen.

SYNTHESIS OF NEW TWO DERIVATIVES OF 6-MERCAPTOPURINE (6MP) 6-[5-PYRIDINE-4-YL- 1, 2, 3, 4-OXADIAZOLE-2-YL)DITHIOL]-9H-PURINE (38) AND 9H-PURINE-6-YL-BENYLDITHIOCARBAMATE (45) WITH CYTOTOXICITY RESULTS FROM THE NATIONAL CANCER INSTITUTE'S ANTICANCER DRUG SCREEN

What major difference is there between purine and pyrimidine synthesis in terms ..
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Xaluprine 20 mg/ml oral suspension - by Nova Laboratories Ltd

Mercaptopurine (6-MP) competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to thioinosinic acid (TIMP). This intracellular nucleotide inhibits several reactions involving inosinic acid (IMP), including the conversion of IMP to xanthylic acid (XMP) and the conversion of IMP to adenylic acid (AMP) via adenylosuccinate (SAMP). In addition, 6-methylthioinosinate (MTIMP) is formed by the methylation of TIMP. Both TIMP and MTIMP have been reported to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway for purine ribonucleotide synthesis. Experiments indicate that radiolabeled mercaptopurine may be recovered from the DNA in the form of deoxythioguanosine. Some mercaptopurine is converted to nucleotide derivatives of 6-thioguanine (6-TG) by the sequential actions of inosinate (IMP) dehydrogenase and xanthylate (XMP) aminase, converting TIMP to thioguanylic acid (TGMP).

Amino Acid Synthesis and Metabolism

Intercalating agents wedge between bases along the DNA. The intercalated drug molecules affect the structure of the DNA, preventing polymerase and other DNA binding proteins from functioning properly. The result is prevention of DNA synthesis, inhibition of transcription and induction of mutations.

Practice Questions | Biochemistry for Medics – Lecture …

Examples include: Carboplatin and Cisplatin:
These related drugs covalently bind to DNA with preferential binding to the N-7 position of guanine and adenine. They are able to bind to two different sites on DNA producing cross-links, either intrastrand (within the same DNA molecule which results in inhibition of DNA synthesis and transcription.

Ketorolac Tromethamine Tablets Drug Information

N2 - The effect of 6-mercaptopurine (6-MP) and its nucleoside and nucleotide derivatives on the rate of RNA synthesis with reticulocyte RNA-dependent RNA polymerase has been examined. Of the 6-MP derivatives tested only 6-mercaptopurine ribo-5′-monophosphate (6-MPR-P) significantly stimulates the rate of RNA synthesis with hemoglobin mRNA as a template while 6-MP and 6-MPR have little or no effect. Kinetic studies have demonstrated that 6-MPR-P activates the RNA-dependent RNA polymerase by increasing the Vmax of the enzyme rather than by decreasing the Km values for the substrates. It is suggested that the stimulation of RNA-dependent RNA synthesis by 6-MPR-P may explain the transient development of megaloblastic anemia following 6-MP therapy.

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