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Chelsea L Dieck et al.
Cancer cell, 34(1), 136-147 (2018-07-11)
Activating mutations in the cytosolic 5'-nucleotidase II gene NT5C2 drive resistance to 6-mercaptopurine in acute lymphoblastic leukemia. Here we demonstrate that constitutively active NT5C2 mutations K359Q and L375F reconfigure the catalytic center for substrate access and catalysis in the absence
Michael E Rytting et al.
Cancer, 120(23), 3660-3668 (2014-07-22)
Various trials have reported improved outcomes for adolescents and young adults (AYAs) with acute lymphoblastic leukemia (ALL) who received treatment with pediatric-based regimens. Those reports prompted the current investigation of the pediatric augmented Berlin-Frankfurt-Münster (ABFM) regimen in AYA patients. The
Phuong Thu Vu Hoang et al.
Journal of pediatric hematology/oncology, 36(7), 534-540 (2013-12-11)
To compare the relapse-free survival (RFS) in Vietnamese (n=141) and white (n=94) children living in Vietnam and Belgium, respectively, and treated in their own country for acute lymphoblastic leukemia according to the same FRALLE 2000 protocol. RFS was significantly worse
Nathalie K Zgheib et al.
Pharmacogenetics and genomics, 24(8), 387-396 (2014-07-10)
The aim of this study is to analyze polymorphisms in genes involved in 6-mercaptopurine detoxification (TPMT); methotrexate (MTX) metabolism including ABCB1 (or MDR1), ABCC2, SLC19A1 (or RFC1), and SLCO1B1; and the MTX effect mainly MTHFR and TYMS, and to assess
Kim K B Clemmensen et al.
Pediatric blood & cancer, 61(4), 653-658 (2013-11-23)
The event-free survival of childhood acute lymphoblastic leukemia (ALL) has been reported to be superior when oral methotrexate (MTX) and 6-mercaptopurine (6MP) maintenance therapy (MT) is administered in the evening compared to the morning. In the ALL92 MT study we
Ido Laish et al.
Harefuah, 151(12), 692-695 (2013-01-22)
Thiopurine drugs, azathioprine (Imuran) and 6-mercaptopurine (6-MP), are immunomodulators that have been shown to be effective at inducing and maintaining remission in inflammatory bowel disease. Although usually well-tolerated, the occurrence of side effects, typically myelotoxicity and hepatotoxicity, is a major
Heeseon An et al.
Nature, 583(7815), 303-309 (2020-07-03)
Mammalian cells reorganize their proteomes in response to nutrient stress through translational suppression and degradative mechanisms using the proteasome and autophagy systems1,2. Ribosomes are central targets of this response, as they are responsible for translation and subject to lysosomal turnover
Julienne Brackett et al.
Pediatric blood & cancer, 61(6), 1114-1117 (2014-01-01)
Mercaptopurine (6-MP), a critical component of acute lymphoblastic leukemia (ALL) therapy, is metabolized to 6-thioguanine (6-TGN) which is responsible for its anti-leukemic effect, and to 6-methylmercaptopurine nucleotides (6-MMPN/6-MMP) which can be hepatotoxic. Some patients preferentially metabolize 6-MP to 6-MMPN which
Ajay Vora et al.
The Lancet. Oncology, 15(8), 809-818 (2014-06-14)
No randomised study has shown whether stratification of treatment by minimal residual disease (MRD) response improves outcome in children and young people with acute lymphoblastic leukaemia (ALL). We assessed whether children and young people with clinical standard and intermediate-risk ALL
Jaszianne Tolbert et al.
Archives of disease in childhood, 100(1), 101-105 (2014-10-23)
In the last two decades, tremendous advances have been made in the treatment of acute lymphocytic leukaemia (ALL) in children with 5 year 'cure' rates in excess of 90%. The maintenance of remission is due, in part, to individualisation of therapy
Salma Melaouhia et al.
Therapie, 68(5), 313-320 (2013-11-15)
The objective of our work is to search if there is a relation between azathioprine's metabolites (6-thioguanines nucleotides and 6-methyl mercaptopurines) and clinical efficacy and adverse effects of azathioprine in inflammatory bowel disease population. We included patients with Crohn's disease
Resistance revealed in acute lymphoblastic leukemia.
Jon C Aster et al.
Nature medicine, 19(3), 264-265 (2013-03-08)
Florencia Alvarez et al.
ACS applied materials & interfaces, 5(2), 249-255 (2012-12-21)
The copper intrauterine device (IUD) based its contraceptive action on the release of cupric ions from a copper wire. Immediately after the insertion, a burst release of copper ions occurs, which may be associated to a variety of side effects.
Mette Levinsen et al.
Cancer chemotherapy and pharmacology, 75(1), 59-66 (2014-10-29)
Through enhancement of 6-mercaptopurine (6MP) bioavailability and inhibition of purine de novo synthesis, high-dose methotrexate (HD-MTX) may increase incorporation into DNA of 6-thioguanine nucleotides, the cytotoxic metabolites of 6MP. Patients with intermediate activity of thiopurine methyltransferase (TPMT(IA)) have higher cytosol
Irreversible myelopathy associated with nelaribine in T-cell acute lymphoblastic leukemia.
Russell P Gollard et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 31(19), e327-e331 (2013-05-30)
Y S de Boer et al.
Alimentary pharmacology & therapeutics, 37(6), 640-646 (2013-01-26)
Ten percent of patients with autoimmune hepatitis (AIH) are nonresponsive or intolerant to thiopurine therapy. A skewed metabolism, leading to the preferential generation of (hepato)toxic thiopurine metabolites (6-MMPs) instead of the metabolic active 6-tioguanine (thioguanine) nucleotides (6-TGNs), may explain this
Letter: allopurinol co-therapy is safe and effective in autoimmune hepatitis.
S Al-Shamma et al.
Alimentary pharmacology & therapeutics, 37(9), 919-919 (2013-04-05)
F Fichel et al.
Annales de dermatologie et de venereologie, 140(3), 209-214 (2013-03-08)
Herein, we report the first case of kaposiform haemangioendothelioma (KHE) associated with acute B-lymphoblastic leukemia (B-ALL). A five-month-old infant presented a plaque of angiomatous appearance on the forearm that had increased in volume since birth, as well as pallor and
Kevin A Hommel et al.
European journal of gastroenterology & hepatology, 25(4), 469-473 (2013-01-18)
To evaluate an individually tailored multicomponent nonadherence treatment protocol using a telehealth delivery approach in adolescents with inflammatory bowel disease. Nine participants, age 13.71±1.35 years, completed a brief treatment online through Skype. Medication nonadherence, severity of disease, and feasibility/acceptability data
Non-cirrhotic portal hypertension due to 6-mercaptopurine use for Crohn's disease.
Suresh Pola et al.
Digestive diseases and sciences, 59(7), 1642-1644 (2014-02-19)
Nilesh Chande et al.
The Cochrane database of systematic reviews, 8(8), CD006618-CD006618 (2014-08-28)
Ulcerative colitis (UC) is a chronic inflammatory bowel disease. Corticosteroids and 5-aminosalicylates are the most commonly used therapies. However, many patients require immunosuppressive therapy for steroid-refractory and steroid-dependent disease. Methotrexate is a medication that is effective for treating a variety
Sarah A Buckley et al.
American journal of hematology, 89(4), 423-428 (2014-01-03)
Intensive chemotherapy for newly diagnosed acute myeloid leukemia (AML) or myelodysplastic syndromes (MDS) is associated with significant treatment-related morbidity and mortality. Herein, we investigate how pretreatment characteristics relate to early adverse outcomes in such patients, studying 205 consecutive individuals receiving
Comparative structural and spectrum analyses of 6-mercaptopurine monohydrate and 6-mercaptopurine hydrochloride
Perez-Ruiz E, et al.
Canadian Journal of Analytical Sciences and Spectroscopy, 43(3), 59-67 (1998)
Gannie Tzoneva et al.
Nature medicine, 19(3), 368-371 (2013-02-05)
Acute lymphoblastic leukemia (ALL) is an aggressive hematological tumor resulting from the malignant transformation of lymphoid progenitors. Despite intensive chemotherapy, 20% of pediatric patients and over 50% of adult patients with ALL do not achieve a complete remission or relapse
American Gastroenterological Association Institute technical review on the use of thiopurines, methotrexate, and anti-TNF-α biologic drugs for the induction and maintenance of remission in inflammatory Crohn's disease.
Themistocles Dassopoulos et al.
Gastroenterology, 145(6), 1464-1478 (2013-11-26)
Goran Marinković et al.
Journal of immunology (Baltimore, Md. : 1950), 192(9), 4370-4378 (2014-03-29)
Azathioprine and its metabolite 6-mercaptopurine (6-MP) are well established immunosuppressive drugs. Common understanding of their immunosuppressive properties is largely limited to immune cells. However, in this study, the mechanism underlying the protective role of 6-MP in endothelial cell activation is
John W D McDonald et al.
The Cochrane database of systematic reviews, 8(8), CD003459-CD003459 (2014-08-08)
Although corticosteroids are effective for induction of remission of Crohn's disease, many patients relapse when steroids are withdrawn or become steroid dependent. Furthermore, corticosteroids exhibit significant adverse effects. The success of methotrexate as a treatment for rheumatoid arthritis led to
Jiaqi Han et al.
Current pharmaceutical design, 26(46), 6013-6020 (2020-09-02)
6-Mercaptopurine (6-MP) is widely used to treat pediatric acute lymphoblastic leukemia (ALL). Mini-tablets of 5 mg per tablet were developed for precision individual therapy for children and individuals with poor thiopurine S-methyltransferase (TPMT) or nucleoside diphophate-linked moiety X-type motif 15
Kenji Taki et al.
The Journal of toxicological sciences, 38(1), 159-167 (2013-01-30)
MicroRNAs (miRNAs) are small single-stranded RNAs of 19-25 nucleotides and are important in posttranscriptional regulation of genes. Recently, the role of miRNAs in toxicity incidence is reported to be a regulator of key-stopper of gene expression, however the detailed mechanism
Lidwien M Hanff et al.
International journal of clinical pharmacology and therapeutics, 52(8), 653-662 (2014-05-08)
Pediatric patients with acute lymphoblastic leukemia (ALL) are treated with oral 6-mercaptopurine (6MP) for nearly 2 years, but no pediatric formulation has been available. In this study, an oral 6MP liquid suitable for pediatric use was developed and tested in
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