6-Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed)Nucleotides: The monomeric units from which DNA or RNA polymers are constructed. They consist of a purine or pyrimidine base, a pentose sugar, and a phosphate group. (From King & Stansfield, A Dictionary of Genetics, 4th ed)Guanine NucleotidesMethylthioinosine: 6-(Methylthio)-9-beta-D-ribofuranosylpurine. An analog of inosine with a methylthio group replacing the hydroxyl group in the 6-position.Precursor Cell Lymphoblastic Leukemia-Lymphoma: A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.Methyltransferases: A subclass of enzymes of the transferase class that catalyze the transfer of a methyl group from one compound to another. (Dorland, 28th ed) EC 2.1.1.Antimetabolites: Drugs that are chemically similar to naturally occurring metabolites, but differ enough to interfere with normal metabolic pathways. (From AMA Drug Evaluations Annual, 1994, p2033)Antimetabolites, Antineoplastic: Antimetabolites that are useful in cancer chemotherapy.Purine Nucleotides: Purines attached to a RIBOSE and a phosphate that can polymerize to form DNA and RNA.Methotrexate: An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.Hypoxanthines: Purine bases related to hypoxanthine, an intermediate product of uric acid synthesis and a breakdown product of adenine catabolism.Thionucleotides: Nucleotides in which the base moiety is substituted with one or more sulfur atoms.Adenine NucleotidesInflammatory Bowel Diseases: Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.Thionucleosides: Nucleosides in which the base moiety is substituted with one or more sulfur atoms.Immunosuppressive Agents: Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging.Asparaginase: A hydrolase enzyme that converts L-asparagine and water to L-aspartate and NH3. EC 3.5.1.1.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Purines: A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.Inosine Monophosphate: Inosine 5'-Monophosphate. A purine nucleotide which has hypoxanthine as the base and one phosphate group esterified to the sugar moiety.Thioinosine: Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503)Polymorphism, Single Nucleotide: A single nucleotide variation in a genetic sequence that occurs at appreciable frequency in the population.Phosphoribosyl Pyrophosphate: The key substance in the biosynthesis of histidine, tryptophan, and purine and pyrimidine nucleotides.Pharmacology: The study of the origin, nature, properties, and actions of drugs and their effects on living organisms.Aminosalicylic Acids: A group of 2-hydroxybenzoic acids that can be substituted by amino groups at any of the 3-, 4-, 5-, or 6-positions.Xanthine Oxidase: An iron-molybdenum flavoprotein containing FLAVIN-ADENINE DINUCLEOTIDE that oxidizes hypoxanthine, some other purines and pterins, and aldehydes. Deficiency of the enzyme, an autosomal recessive trait, causes xanthinuria.Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed)Crohn Disease: A chronic transmural inflammation that may involve any part of the DIGESTIVE TRACT from MOUTH to ANUS, mostly found in the ILEUM, the CECUM, and the COLON. In Crohn disease, the inflammation, extending through the intestinal wall from the MUCOSA to the serosa, is characteristically asymmetric and segmental. Epithelioid GRANULOMAS may be seen in some patients.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.Aldehyde Oxidase: An aldehyde oxidoreductase expressed predominantly in the LIVER; LUNGS; and KIDNEY. It catalyzes the oxidation of a variety of organic aldehydes and N-heterocyclic compounds to CARBOXYLIC ACIDS, and also oxidizes quinoline and pyridine derivatives. The enzyme utilizes molybdenum cofactor and FAD as cofactors.Prodrugs: A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.Leukemia L1210Inosine: A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)Ion Exchange Resins: High molecular weight, insoluble polymers which contain functional groups that are capable of undergoing exchange reactions (ION EXCHANGE) with either cations or anions.Azauridine: A triazine nucleoside used as an antineoplastic antimetabolite. It interferes with pyrimidine biosynthesis thereby preventing formation of cellular nucleic acids. As the triacetate, it is also effective as an antipsoriatic.Azaguanine: One of the early purine analogs showing antineoplastic activity. It functions as an antimetabolite and is easily incorporated into ribonucleic acids.Cytarabine: A pyrimidine nucleoside analog that is used mainly in the treatment of leukemia, especially acute non-lymphoblastic leukemia. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. Its actions are specific for the S phase of the cell cycle. It also has antiviral and immunosuppressant properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p472)Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Purine Nucleosides: Purines with a RIBOSE attached that can be phosphorylated to PURINE NUCLEOTIDES.Cloning, Molecular: The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.Hypoxanthine Phosphoribosyltransferase: An enzyme that catalyzes the conversion of 5-phosphoribosyl-1-pyrophosphate and hypoxanthine, guanine, or 6-mercaptopurine to the corresponding 5'-mononucleotides and pyrophosphate. The enzyme is important in purine biosynthesis as well as central nervous system functions. Complete lack of enzyme activity is associated with the LESCH-NYHAN SYNDROME, while partial deficiency results in overproduction of uric acid. EC 2.4.2.8.Erythrocytes: Red blood cells. Mature erythrocytes are non-nucleated, biconcave disks containing HEMOGLOBIN whose function is to transport OXYGEN.Leukemia, Lymphoid: Leukemia associated with HYPERPLASIA of the lymphoid tissues and increased numbers of circulating malignant LYMPHOCYTES and lymphoblasts.Kinetics: The rate dynamics in chemical or physical systems.Remission Induction: Therapeutic act or process that initiates a response to a complete or partial remission level.Adenine: A purine base and a fundamental unit of ADENINE NUCLEOTIDES.Pregnancy: The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.Hepatitis, Autoimmune: A chronic self-perpetuating hepatocellular INFLAMMATION of unknown cause, usually with HYPERGAMMAGLOBULINEMIA and serum AUTOANTIBODIES.Pregnancy Outcome: Results of conception and ensuing pregnancy, including LIVE BIRTH; STILLBIRTH; SPONTANEOUS ABORTION; INDUCED ABORTION. The outcome may follow natural or artificial insemination or any of the various ASSISTED REPRODUCTIVE TECHNIQUES, such as EMBRYO TRANSFER or FERTILIZATION IN VITRO.DenmarkPregnancy Complications: Conditions or pathological processes associated with pregnancy. They can occur during or after pregnancy, and range from minor discomforts to serious diseases that require medical interventions. They include diseases in pregnant females, and pregnancies in females with diseases.
Kornberg, A., Lieberman, I. and Simms, E.S. (1955). "Enzymatic synthesis of purine nucleotides". J. Biol. Chem. 215: 417-427. ... B enzm: 1.1/2/3/4/5/6/7/8/10/11/13/14/15-18, 2.1/2/3/4/5/6/7/8, 2.7.10, 2.7.11-12, 3.1/2/3/4/5/6/7, 3.1.3.48, 3.4.21/22/23/24, ... Flaks, J.G. (1963). "Nucleotide synthesis from 5-phosphoribosylpyrophosphate". Methods Enzymol. 6: 136-158. ... Guanin i 6-merkaptopurin mogu da zamene hipoksantin. Reference[uredi - уреди , uredi izvor]. *↑ ...
nucleotide analogues - nucleotides alternatives that contain a nucleic acid, a sugar, and 1-3 phosphates. This means these ... mercaptopurine) or a pyrimidine, chemicals that become the building-blocks of DNA. They prevent these substances from becoming ... However, because they are analogues and therefore slightly different than regular nucleotides, causing the cell's growth to be ... Antimetabolites generally impair DNA replication machinery, either by incorporation of chemically altered nucleotides or by ...
The nucleotides are incorporated into newly synthesized (but non-functional) DNA, halting replication. The nucleotides act to ... A 2003 population-based study in Denmark showed that the use of azathioprine and related mercaptopurine resulted in a seven- ... and then phosphorylated to form the nucleotides thioinosinic acid and thioguanylic acid respectively. These nucleotides ... A portion of the nucleotides is additionally phosphorylated to the triphosphate forms. These bind to GTP-binding protein Rac1, ...
Some mercaptopurine is converted to nucleotide derivatives of 6-thioguanine (6-TG) by the sequential actions of inosinate (IMP ... This alters the synthesis and function of RNA and DNA.[citation needed] Mercaptopurine interferes with nucleotide ... Mercaptopurine is in the thiopurine and antimetabolite family of medications. Mercaptopurine was approved for medical use in ... "Label: Mercaptopurine - mercaptopurine tablet". Archived from the original on 6 October 2015. Retrieved 11 March 2015. Wang L, ...
On the other hand, some cases of IBD that are resistant to mercaptopurine (or its pro-drug azathioprine) may be responsive to ... However, the intra-cellular thio-nucleotide metabolites of thioguanine (6-TGN) have longer half-lives and can therefore be ... Sigel, Astrid; Sigel, Helmut (1996). Metal Ions in Biological Systems: Volume 32: Interactions of Metal Ions with Nucleotides: ... Cancers that do not respond to treatment with mercaptopurine do not respond to thioguanine. ...
1996). "Thiopurine S-methyltransferase deficiency: two nucleotide transitions define the most prevalent mutant allele ... 1997). "Molecular diagnosis of thiopurine S-methyltransferase deficiency: genetic basis for azathioprine and mercaptopurine ... Weinshilboum RM, Sladek SL (1980). "Mercaptopurine pharmacogenetics: Monogenic inheritance of erythrocyte thiopurine ... Nucleosides Nucleotides Nucleic Acids. 23 (8-9): 1385-91. doi:10.1081/NCN-200027637. PMID 15571264. Lee W, Lockhart AC, Kim RB ...
Essayan DM (November 2001). "Cyclic nucleotide phosphodiesterases". J. Allergy Clin. Immunol. 108 (5): 671-80. doi:10.1067/mai. ... and/or mercaptopurine. TNF inhibitors put patients at increased risk of certain opportunistic infections. The FDA has warned ... 12 (6-7): 445-52. doi:10.1016/j.phymed.2003.12.011. PMID 16008121. Raduner S, Majewska A, Chen JZ, Xie XQ, Hamon J, Faller B, ... 9 (6): 299-301. doi:10.1124/mi.9.6.5. PMC 2861806 . PMID 20048135. Keffer J, Probert L, Cazlaris H, Georgopoulos S, Kaslaris E ...
Similarly, hypersensitivity to the antiretroviral drug abacavir is strongly associated with a single-nucleotide polymorphism ... thereby regulating the balance between cytotoxic thioguanine nucleotide and inactive metabolites in hematopoietic cells. TPMT ... 37 (2): 232-6. doi:10.1111/j.1365-2710.2011.01262.x. PMID 21507031. U.S. Food and Drug Administration (FDA). "Table of ... 10 (6): 961-9. doi:10.2217/pgs.09.37. PMID 19530963. Hauser, Alexander S.; Chavali, Sreenivas; Masuho, Ikuo; Jahn, Leonie J.; ...
Mercaptopurine itself can also be administered directly. By preventing the clonal expansion of lymphocytes in the induction ... which is a key enzyme in the de novo guanosine nucleotide synthesis. In contrast to other human cell types, lymphocytes B and T ... It is nonenzymatically cleaved to mercaptopurine, that acts as a purine analogue and an inhibitor of DNA synthesis. ... These include: folic acid analogues, such as methotrexate purine analogues, such as azathioprine and mercaptopurine pyrimidine ...
In oncology, pharmacogenetics historically is the study of germline mutations (e.g., single-nucleotide polymorphisms affecting ... mercaptopurine/azathioprine, gemcitabine/capecitabine/AraC and tamoxifen, respectively. The decision to use pharmacogenetic ... 348 (6): 538-49. doi:10.1056/NEJMra020526. PMID 12571262. Phillips KA, Veenstra DL, Oren E, Lee JK, Sadee W (November 2001). " ... One in 300 people have two variant alleles and lack TPMT activity; these people need only 6-10% of the standard dose of the ...
Nucleoside/Nucleotide reverse transcriptase inhibitors Entecavir Tenofovir disoproxil fumarate (TDF) Nucleotide polymerase ... α Filgrastimα Fludarabineα Fluorouracilα Gemcitabineα Hydroxycarbamideα Ifosfamideα Imatinibα Irinotecanα Mercaptopurineα Mesna ... Retrieved 6 March 2017. Beall, Reed (2016). "Patents and the WHO Model List of Essential Medicines (18th Edition): Clarifying ...
Azathioprine and mercaptopurine[edit]. Azathioprine (Prometheus' Imuran), is the main immunosuppressive cytotoxic substance. It ... which is a key enzyme in the de novo guanosine nucleotide synthesis. In contrast to other human cell types, lymphocytes B and T ... Mercaptopurine itself can also be administered directly. By preventing the clonal expansion of lymphocytes in the induction ... It is nonenzymatically cleaved to mercaptopurine, that acts as a purine analogue and an inhibitor of DNA synthesis. ...
The building blocks are nucleotides; a molecule comprising a nucleobase, a sugar and a phosphate group. The nucleobases are ... The thiopurines include thioguanine and mercaptopurine. Anti-microtubule agents are plant-derived chemicals that block cell ... a nucleotide without the phosphate group), but have altered chemical groups. These drugs exert their effect by either blocking ... mercaptopurine, and 5-fluorouracil. Female infertility by chemotherapy appears to be secondary to premature ovarian failure by ...
... mercaptopurine riboside] and dilazep for the human equilibrative nucleoside transporter, hENT1". Biochem. J. 380 (Pt 1): 131-7 ... Nucleoside transporters are required for nucleotide synthesis in cells that lack de novo nucleoside synthesis pathways, and are ... 279 (6): 4490-7. doi:10.1074/jbc.M307938200. PMID 14607828. Lehner B, Semple JI, Brown SE, et al. (2004). "Analysis of a high- ... 6 (9): 791-806. doi:10.1101/gr.6.9.791. PMID 8889548. Griffiths M, Yao SY, Abidi F, et al. (1998). "Molecular cloning and ...
... poisons the transcription-coupled nucleotide excision repair (TCR) complex, promotes degradation of RNA polymerase II, and ... 1'R,6R,6aR,7R,13S,14S,16R)-6',8,14-trihydroxy-7',9-dimethoxy-4,10,23-trimethyl-19-oxo-3',4',6,7,12,13,14,16-octahydrospiro[6,16 ... His group developed such a method and published it in 1996.[6] This was later followed by a simpler and more tractable method ... The total synthesis by E.J. Corey [6] used this proposed biosynthesis to guide their synthetic strategy. The synthesis uses ...
Inheriting abnormal thiopurine S-methyltransferase may affect the metabolism of the thiopurine drugs mercaptopurine and ... Bose KS, Sarma RH (October 1975). "Delineation of the intimate details of the backbone conformation of pyridine nucleotide ... 348 (6): 553-6. doi:10.1056/NEJMe020173. PMID 12571264.. *^ a b "Drug-Interactions.com". Archived from the original on 30 ... 348 (6): 529-37. doi:10.1056/NEJMra020021. PMID 12571261.. *^ a b Evans WE, McLeod HL (February 2003). "Pharmacogenomics--drug ...
The building blocks are nucleotides; a molecule comprising a nucleobase, a sugar and a phosphate group. The nucleobases are ... mercaptopurine, and 5-fluorouracil.[90] ... a nucleotide without the phosphate group), but have altered ... 18 (7): 853-6.. *^ a b Gurney H (Apr 2002). "How to calculate the dose of chemotherapy". British Journal of Cancer. 86 (8): ... 305 (6): 549-551. PMID 21304073. doi:10.1001/jama.2011.92.. *^ Mir LM, Gehl J, Sersa G, Collins CG, Garbay JR, Billard V, ...
Guanine is one of the four nucleotides that makes up DNA. The methylated DNA strands stick together such that cell division ... 23 (6): 488-96. PMC 2737459. PMID 19544689.. *^ Rueda Domínguez, A; Márquez, A; Gumá, J; Llanos, M; Herrero, J; de Las Nieves, ... As of mid-2006, dacarbazine is commonly used as a single agent in the treatment of metastatic melanoma,[5][6] and as part of ... 28 (23): 3680-6. doi:10.1200/jco.2009.26.9381. PMID 20625128. Archived from the original on 16 July 2016.. ...
... chemically alters the DNA nucleotide guanine through alkylation, and causes linkages between strands of DNA. This ... InChI=1S/C13H18Cl2N2O2/c14-5-7-17(8-6-15)11-3-1-10(2-4-11)9-12(16)13(18)19/h1-4,12H,5-9,16H2,(H,18,19)/t12-/m0/s1 Y ... This page was last edited on 6 August 2018, at 18:06 (UTC). ... Mercaptopurine#). Pyrimidine. *Thymidylate synthase inhibitor ( ...
Induction of mispairing of the nucleotides leading to mutations.. The precise mechanisms by which chlorambucil acts to kill ... InChI=1S/C14H19Cl2NO2/c15-8-10-17(11-9-16)13-6-4-12(5-7-13)2-1-3-14(18)19/h4-7H,1-3,8-11H2,(H,18,19) Y ... 6] It can be used for treating some types of non-Hodgkin lymphoma, Waldenström macroglobulinemia, polycythemia vera, ...
In genetics, crosslinking of DNA occurs when various exogenous or endogenous agents react with two nucleotides of DNA, forming ... Mitomycin C can only act as a crosslinker when a DNA nucleotide has had a reduction to its quinone ring. When two dG's have ... Crosslinked DNA is repaired in cells by a combination of enzymes and other factors from the nucleotide excision repair (NER) ... These cross-linking agents have the ability to act as single-agent therapies by targeting and destroying specific nucleotides ...
Nucleoside and nucleotide reverse-transcriptase inhibitors. *PDE5 inhibitors. *Proton pump inhibitors. *Statins ... 6 (18): 2252-7. doi:10.4161/cc.6.18.4751. PMID 17700065.. *^ Lipton JO, Sahin M (October 2014). "The neurology of mTOR". Neuron ... doi:10.1007/s11523-011-0177-6. PMID 21533544.. *^ Nowak, Pawel; Cole, Derek C.; Brooijmans, Natasja; Bursavich, Matthew G.; ... Computational modelling studies helped the synthesise of the compound.[6] Adverse events[edit]. Treatment with mTOR inhibitors ...
Nucleoside/Nucleotide reverse transcriptase inhibitors[edit]. *Entecavir. *Tenofovir disoproxil fumarate (TDF). Medicines for ... Mercaptopurineα. *Methotrexateα. *Oxaliplatinα. *Paclitaxelα. *Pegaspargaseα[note 60] ... Retrieved 6 March 2017.. *^ Beall, Reed (2016). "Patents and the WHO Model List of Essential Medicines (18th Edition): ... 97 (6): 394-404C. doi:10.2471/BLT.18.222448. hdl:10665/325509. ISSN 0042-9686. PMC 6560372. PMID 31210677.. ...
nucleotide analogues - nucleotides alternatives that contain a nucleic acid, a sugar, and 1-3 phosphates. This means these ... Anti-metabolites masquerade as a purine (azathioprine, mercaptopurine) or a pyrimidine, chemicals that become the building- ... However, because they are analogues and therefore slightly different than regular nucleotides, causing the cell's growth to be ... Antimetabolites generally impair DNA replication machinery, either by incorporation of chemically altered nucleotides or by ...
Now, 6 months later because remicade isnt working on its own he has prescribed me imuran and I am concerned. How can something ... Now, 6 months later because remicade isnt working on its own he has prescribed me imuran and I am concerned. How can something ... I was tested (for 6-MP). My doctor has been pretty serious about monitoring my bloodwork and ordering all sorts of fancy tests ... Thiopurines [azathioprine (AZA), 6-mercaptopurine (6-MP) and thioguanine (6-TG)] have a well-established role as ...
The nucleotides were hydrolyzed to their own bases by heating the sample for 45 min at 100 degrees C. During acid hydrolysis ... 6-thioguanine (6-TGN) and methyl 6-mercaptopurine nucleotides (Me6-MPNs) are the two major metabolites found in erythrocytes ... With this procedure, mean recoveries of 73.1% and 84.0% for 6-TGN and Me6-MPN derivatives, respectively, were found. ... we have developed a HPLC method for the simultaneous determination of 6-TGNs and Me6-MPNs in erythrocytes. A simple and rapid ...
... and cyclophosphamide on nucleotide metabolism of human erythrocytes. / Kay, N. E.; Oski, F. A. ... and cyclophosphamide on nucleotide metabolism of human erythrocytes. In: Clinical Research. 1973 ; Vol. 21, No. 3. ... and cyclophosphamide on nucleotide metabolism of human erythrocytes, Clinical Research, vol. 21, no. 3. ... and cyclophosphamide on nucleotide metabolism of human erythrocytes. Clinical Research. 1973 Jan 1;21(3). ...
... and may enhance the activation of 6-mercaptopurine (6-MP) to 6-thioguanine nucleotides... ... Methotrexate Methotrexate polyglutamates Mercaptopurine Leukemia Thioguanine nucleotides This is a preview of subscription ... Dervieux T, Hancock M, Evans W, Pui CH, Relling MV (2002) Effect of methotrexate polyglutamates on thioguanine nucleotide ... Rostami-Hodjegan A, Lennard L, Lilleyman JS (1995) The accumulation of mercaptopurine metabolites in age fractionated red blood ...
6-Thiohypoxanthine; Linear Formula: C5H4N4S · H2O; Empirical Formula: C5H4N4S · H2O; find related products, papers, technical ... Nucleotide Synthesis in Cancer Cells Neoplastic cells are highly dependent on the de novo synthesis of nucleotides to maintain ... 6-Mercaptopurine is a widely used antileukemic agent that inhibits de novo purine synthesis through incorporation of thiopurine ... 6-Mercaptopurine monohydrate is an antimetabolite and antineoplastic drug. Its cocrystallization with 4-hydroxybenzoic acid and ...
nucleotide diphosphatase (NUDT15) deficiency. * recently received or scheduled to receive a vaccine ... Mercaptopurine, 6-MP oral suspension. What is this medicine?. MERCAPTOPURINE, 6-MP (mer kap toe PYOOR een) is a chemotherapy ... an unusual or allergic reaction to mercaptopurine, other medicines, foods, dyes, or preservatives ...
Chen, Z. S., Lee, K., and Kruh, G. D. (2001). Transport of cyclic nucleotides and estradiol 17-beta-D-glucuronide by multidrug ... MRP4 shows the remarkable capacity to transport cyclic nucleotides and MRP4 has been established as an independent regulator of ... Resistance to 6-mercaptopurine and 6-thioguanine. J. Biol. Chem. 276, 33747-33754. doi: 10.1074/jbc.M104833200 ...
Mercaptopurine is an antimetabolite chemotherapy medication used in combination with other medications in the treatment of ... Mercaptopurine is a "purine antagonist," meaning that it inhibits purine nucleotide synthesis and metabolism. ... How to Take Mercaptopurine. Mercaptopurine is taken by mouth (in the form of a tablet or a liquid), once a day. Ideally it ... Possible Side Effects of Mercaptopurine. There are a number of things you can do to manage the side effects of Mercaptopurine. ...
Inhibits de novo purine nucleotide synthesis, activated by HGPRT, cell cycle specific ; For acute leukemia (AML, ALL), CML ... Inhibits dihydrofolate reductase, decreases synthesis of thymidylate, amino acids, purine nucleotides; cell cycle specific ...
... further metabolism occurs before thioguanine nucleotides are formed.2 Thioguanine nucleotides are responsible for inhibiting ... Azathioprine, mercaptopurine and birth outcome: a population-based cohort study. Aliment Pharmacol Ther 2003;17(6):827-34. ... Differing contribution of thiopurine methyltransferase to mercaptopurine versus thioguanine effects in human leukemic cells. ... Am J Med Genet A 2003;116A(1):31-6. Medline. *Schardein JL. Chemically induced birth defects. 3rd ed. New York, NY: Marcel ...
Kornberg, A., Lieberman, I. and Simms, E.S. (1955). "Enzymatic synthesis of purine nucleotides". J. Biol. Chem. 215: 417-427. ... B enzm: 1.1/2/3/4/5/6/7/8/10/11/13/14/15-18, 2.1/2/3/4/5/6/7/8, 2.7.10, 2.7.11-12, 3.1/2/3/4/5/6/7, 3.1.3.48, 3.4.21/22/23/24, ... Flaks, J.G. (1963). "Nucleotide synthesis from 5-phosphoribosylpyrophosphate". Methods Enzymol. 6: 136-158. ... Guanin i 6-merkaptopurin mogu da zamene hipoksantin. Reference[uredi - уреди , uredi izvor]. *↑ ...
Chen ZS, Lee K, and Kruh GD. Transport of cyclic nucleotides and estradiol 17-β-d-glucuronide by multidrug resistance protein 4 ... The multidrug resistance protein 5 functions as an ATP-dependent export pump for cyclic nucleotides. J Biol Chem 275: 30069- ... is a cyclic nucleotide efflux pump and a resistance factor for fluoropyrimidines 2′,3′-dideoxycytidine and 9′-(2′- ... and MRP5-mediated transport of cyclic nucleotides from intact cells. J Biol Chem 278: 17664-17671, 2003. ...
Azathioprine 1.5-2.5 mg/kg/day or mercaptopurine 0.75-1.5 mg/kg/day may be used in active CD as adjunctive therapy and as a ... Azathioprine 1.5-2.5 mg/kg/day, or mercaptopurine 0.75-1.25 mg/kg/day are the first line agents of choice for steroid dependent ... Azathioprine 1.5-2.5 mg/kg/day or mercaptopurine 0.75-1.5 mg/kg are effective, but reserved as second line therapy because of ... Azathioprine 1.5-2.5 mg/kg/day or mercaptopurine 0.75-1.5 mg/kg/day may be used for preventing postoperative recurrence and may ...
... nucleotide sequence, and products of two Pseudomonas denitrificans cob genes encoding nicotinate-nucleotide: ... 2. Kornberg, A., Lieberman, I. and Simms, E.S. Enzymatic synthesis of purine nucleotides. J. Biol. Chem. 215 (1955) 417-427.. 3 ... 2. Kornberg, A., Lieberman, I. and Simms, E.S. Enzymatic synthesis of purine nucleotides. J. Biol. Chem. 215 (1955) 417-427.. 3 ... Enzyme studies on the formation of the α-glycosidic nucleotide precursor. J. Biol. Chem. 244 (1969) 1659-1666. [PMID: 4238408] ...
... it can be assumed that formation of TGN occurs via the nucleotide interconversion pathway TIMP → 6-thioxanthosine monophosphate ... 6-MP, 6-thioxanthine (6-TX), 6-thioguanine (6-TG), TUA, and 8-hydroxy-6-MP (8-OH-6-MP) were extracted from the organs, whereas ... This indicates rapid cellular uptake of 6-MP and an accumulation of 6-MP derivatives that can be explained by formation of the ... The highest concentrations of 6-TG derivatives were found in the spleen and bone marrow. This correlates with the clinical and ...
6 [4.3-8.4], p = 0.01) and smoking currently or in the past (4.3 [2.9-5] vs. 6.7 [5-0.3]). Interestingly, only those treated ... 6% higher levels of VCAM-1 (1178.3 [815.2-1600.1] vs. 893.8 [635.4-959.8] ng/ml, p = 0.02) and 41% higher thrombomodulin levels ... Patients with GPA showed a 15.9% increase in serum levels of VCAM-1 (p = 0.01), 66% of IL-6 (p , 0.001) and 50.9% of ... Interleukin-6 (IL-6), VCAM-1, and soluble thrombomodulin were measured using standardized ELISA method (all, R&D Systems, ...
Single Nucleotide Polymorphisms at a Distance from Aryl Hydrocarbon Receptor Binding Sites Influence AHR Ligand-Dependent Gene ... 2001) Transport of cyclic nucleotides and estradiol 17-β-d-glucuronide by multidrug resistance protein 4. Resistance to 6- ... mercaptopurine and 6-thioguanine. J Biol Chem 276:33747-33754.. OpenUrlAbstract/FREE Full Text ... 6,7-3H(N)]Estradiol 17-β-d-glucuronide (41.8 Ci/mmol) was purchased from PerkinElmer Life and Analytical Sciences (Groningen, ...
Some mercaptopurine is converted to nucleotide derivatives of 6-thioguanine (6-TG) by the sequential actions of inosinate (IMP ... Mercaptopurine may decrease the anticoagulant activities of Tioclomarol.. Experimental. Tofacitinib. Mercaptopurine may ... Deslanoside may decrease the cardiotoxic activities of Mercaptopurine.. Approved. Dicoumarol. Mercaptopurine may decrease the ... Peruvoside may decrease the cardiotoxic activities of Mercaptopurine.. Experimental. Phenindione. Mercaptopurine may decrease ...
Purine nucleotides. Sub Class. Cyclic purine nucleotides. Direct Parent. 3,5-cyclic purine nucleotides. Alternative Parents. ... This compound belongs to the class of organic compounds known as 3,5-cyclic purine nucleotides. These are purine nucleotides ... Nucleotide binding. Specific Function. Not Available. Gene Name. cyaB2. Uniprot ID. P94182. Uniprot Name. Adenylate cyclase. ... Cyclic nucleotide-regulated potassium channel activated by cAMP.. Gene Name. Not Available. Uniprot ID. Q98GN8. Uniprot Name. ...
... and they inhibit main steps in the formation of purine and pyrimidine bases as well as nucleotides (Parker, 2009). This class ... Another class of drugs directly damages DNA by adding methyl or other alkyl groups onto nucleotide bases (Izbicka and Tolcher, ... As such, paclitaxel metabolism into 6α-hydroxypaclitaxel is reduced upon hypoxic conditions compared to normoxic conditions in ... and 6-(4-chlorophenyl)imidazo[2,1-b] [1,3]thiazole-5-carbaldehydeO-(3,4-dichlorobenzyl)oxime (CITCO) is an imidazothiazole ...
At the start of azathioprine or mercaptopurine therapy, measurement of TPMT activity has a role in identifying the 1 in 300 ... These drugs require conversion to thioguanine nucleotides to exert their therapeutic (cytotoxic) effect; however, that ... mercaptopurine accumulates, and a larger proportion of 6-mercaptopurine is converted to the cytotoxic 6-thioguanine nucleotide ...
Differences in nucleotide hydrolysis contribute to the differences between erythrocyte 6-thioguanine nucleotide concentrations ... Liquid chromatography-tandem mass spectrometry analysis of erythrocyte thiopurine nucleotides and effect of thiopurine ... Simultaneous determination of 6-thioguanine and methyl 6-mercaptopurine nucleotides of azathioprine in red blood cells by HPLC ... denoting a compound containing the radical C6H5Hg-, forming various antiseptic, antibacterial, and fungicidal salts; compounds ...
... which inhibits purine nucleotide synthesis and blocks RNA formation and metabolism. Azathioprine has been implicated to be ... rheumatoid arthritis and transplant recipients treated with this mercaptopurine [5,9]. Azathioprine treatment aims at inducing ... 6], and one patient with Crohn`s disease [5]. It appears reasonable to assume that impaired immunosurveillance iatrogenically ... Increased risk of lymphoma among inflammmatory bowel disease patients treated with azathioprine and 6-mercaptopurine. Gut 54: ...
Scheit, Karl Heinz, "Nucleotides with Modified Phosphate Groups", in Nucleotide Analogs John Wiley & Sons, 1980, Chapter Four ... For example, if a nucleotide unit at a certain position of an oligonucleotide is capable of hydrogen bonding with a nucleotide ... A Nucleotide Analog That Is a substrate, Competitive Inhibitor, or Regulator of Some Enzymes That Interact with Adenosine 5- ... Such HPLC-isolated nucleotide diastereomers can be further characterized by analytical HPLC comparisons with commercial samples ...
NUCLEOTIDE ANALOGS. Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide ... PREPARATION AND USE OF 7A-HETEROCYCLE SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES AS PAR-1.... The present ... TREATMENT OF CROHNS DISEASE WITH DELAYED-RELEASE 6-MERCAPTOPURINE. Methods of treating patients suffering from Crohns disease ...
  • Further developments in research may lead to the discovery of rare, but functionally relevant single nucleotide polymorphisms and a better understanding of multiple genomic, epigenomic as well as phenotypic factors, contributing to drug response in malignancies. (cancerindex.org)
  • Further, numerous single-nucleotide polymorphisms (SNPs) have been identified in human AOX1. (aspetjournals.org)
  • Eleven single nucleotide polymorphisms (SNPs) were detected in a mutation scan of 24 unrelated animals of three different cattle breeds, including one SNP that affects the amino acid sequence of GART. (embl-heidelberg.de)
  • Mercaptopurine is one of a large series of purine analogues which interfere with nucleic acid biosynthesis and has been found active against human leukemias. (drugbank.ca)
  • Mercaptopurine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to thioinosinic acid (TIMP). (drugbank.ca)
  • 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). (drugbank.ca)
  • Each scored tablet contains 50 mg mercaptopurine and the inactive ingredients corn and potato starch, lactose, magnesium stearate, and stearic acid. (drugs.com)
  • Common non-synonymous nucleotide and amino-acid change are bolded. (intechopen.com)
  • Azathioprine is stable in solution at neutral or acid pH but hydrolysis to mercaptopurine occurs in excess sodium hydroxide (0.1N), especially on warming. (nih.gov)
  • In the second instance a larger percentage of 6-MP was excreted unchanged and the fraction converted to 6-thiouric acid was drastically reduced. (docme.ru)
  • The sodium salt of azathioprine is sufficiently soluble to make a 10 mg/mL water solution which is stable for 24 hours at 59° to 77°F (15° to 25°C). Azathioprine is stable in solution at neutral or acid pH but hydrolysis to mercaptopurine occurs in excess sodium hydroxide (0.1N), especially on warming. (rxlist.com)
  • MRP5 could confer resistance to several anticancer drugs, including cisplatin, purine analogues (such as 6-mercaptopurine and 6-thioguanine), pyrimidine analogues (such as gemcitabine, cytosine arabinoside (Ara-C) and 5-fluorouracil (5-FU)) , the natural product doxorubicin and to anti-folate drugs (such as MTX), but not to Vinca alkaloids (such as vincristine) [ PMID: 21740521 ]. (ebi.ac.uk)
  • PURIXAN ® (mercaptopurine) is a nucleoside metabolic inhibitor indicated for the treatment of patients with acute lymphoblastic leukemia (ALL) as a component of a combination maintenance therapy regimen. (purixan-us.com)
  • Symptoms of allergic reaction to mercaptopurine include rash , itching , swelling , dizziness , trouble breathing , and inflammation of the pancreas . (wikipedia.org)
  • While autoimmune diseases themselves tend to be associated with a more frequent occurrence of malignancies there appears to be a higher incidence of lymphomas in patients with inflammatory bowel disease, rheumatoid arthritis and transplant recipients treated with this mercaptopurine [5, (upmc.edu)
  • A total of 61.4% of the patients achieved remission and only 32.6% of these children had 6-TGN values within the target range proposed for inflammatory bowel disease (250-450 pmol/8 x 10(8) red blood cells). (biomedsearch.com)
  • 6-mercaptopurine was used sparingly in the Oxford Inflammatory Bowel Disease clinic. (brainstrom.org)
  • MERCAPTOPURINE, 6-MP (mer kap toe PYOOR een) is a chemotherapy drug. (ahealthyme.com)
  • Thus, relapse associated activating mutations in NT5C2 confer resistance to 6-MP and 6-TG chemotherapy. (lightsources.org)
  • Recent evidence (( 3 )-( 6 )) suggests that genes that regulate apoptotic cell death may play an important role in determining the sensitivity of tumor cells to chemotherapy. (rupress.org)
  • Premalignant lesions are clinically treated with an array of therapies, including chemotherapy, topical immunomodulatory and anti-inflammatory agents, cryotherapy, surgical excision, and photodynamic therapy ( 5, 6 ). (aacrjournals.org)
  • The AICAR transformylase inhibitors BW1540 and BW2315 are sulfamido-bridged 5,8-dideazafolate analogs with remarkably potent K(i) values of 8 and 6 nm, respectively, compared with most other antifolates. (embl-heidelberg.de)
  • Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs. (ebi.ac.uk)
  • It is not generally appreciated that erythrocytes do not express the enzyme IMP dehydrogenase and cannot convert mercaptopurine to TGN, which explains some of the confusion in interpretation of erythrocyte TGN measurements. (nih.gov)
  • Animal tumors that are resistant to mercaptopurine often have lost the ability to convert mercaptopurine to TIMP. (drugs.com)
  • More information about allele, protein, nucleotide changes, trivial name and effect of the gene of polymorphism on enzyme activity may be found in http://www.cypalleles.ki.se/index.htm and http://www.snpedia.com/index.php/SNPedia.Common alleles, substrates and clinical evidences of some CYPs. (intechopen.com)
  • 6. Kinetic and spectrophotometric investigation of the interaction of the enzyme with inhibitors and p-nitrophenyl acetate. (docphin.com)
  • Although these side effects may be dose related, the genotype of the 6-thiopurinemethyltransferase enzyme is probably a more important determinant of developing leucopenia. (brainstrom.org)
  • Current routine assays measure the nucleotides after hydrolysation to nucleic bases and are therefore unable to distinguish between mono-, di-, and triphosphates. (diva-portal.org)
  • To clarify the pharmacokinetic interactions between these two antimetabolites, we serially measured RBC 6-TGN and MTX polyglutamates (MTXPG) levels following repeated courses of HDMTX (5 g/m² over 24 h) with daily oral 6-MP (25 mg/m²) during interval therapy in 20 children with ALL. (springer.com)
  • Plasma protein binding averages 19% over the concentration range 10 to 50 µg/mL (a concentration only achieved by intravenous administration of mercaptopurine at doses exceeding 5 to 10 mg/kg). (drugbank.ca)