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Original Article

Clinical Science Review: Update on Trimetrexate, a Folate Antagonist with Antineoplastic and Antiprotozoal Properties

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Pages 159-172 | Published online: 11 Jun 2009

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Kenneth D Bagshawe, Philip J Burke, Richard J Knox, Roger G Melton & Surinder K Sharma. (1999) Targeting enzymes to cancers - new developments. Expert Opinion on Investigational Drugs 8:2, pages 161-172.
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Albert Kheradpour, Ellin Berman, Erdem Göker, James T. Lin, William P. Tong & Joseph R. Bertino. (1995) A Phase II Study of Continuous Infusion of Trimetrexate in Patients with Refractory Acute Leukemia. Cancer Investigation 13:1, pages 36-40.
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Safoura Hariri, Behnam Rasti, Farhad Shirini & Jahan B. Ghasemi. (2021) A combined structure-based pharmacophore modeling and 3D-QSAR study on a series of N-heterocyclic scaffolds to screen novel antagonists as human DHFR inhibitors. Structural Chemistry 32:4, pages 1571-1588.
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Gerrit Jansen, Joost van der Heijden, Ruud Oerlemans, Willem F. Lems, Ilan Ifergan, Rik J. Scheper, Yehuda G. Assaraf & Ben A. C. Dijkmans. (2004) Sulfasalazine is a potent inhibitor of the reduced folate carrier: Implications for combination therapies with methotrexate in rheumatoid arthritis. Arthritis & Rheumatism 50:7, pages 2130-2139.
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M. R. Machiavelli, G. Salum, J. E. P??rez, E. H. Ortiz, A. O. Romero, F. Bologna, C. T. Vallejo, J. A. Lacava, M. E. Dominguez & B. A. Leone. (2004) Double Modulation of 5-Fluorouracil by Trimetrexate and Leucovorin in Patients With Advanced Colorectal Carcinoma. American Journal of Clinical Oncology 27:2, pages 149-154.
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R.G. Amado, L.S. Rosen, J.R. Hecht, L.-S. Lin & P.J. Rosen. (2002) Low-dose trimetrexate glucuronate and protracted5-fluorouracil infusion in previously untreated patients with advanced pancreatic cancer. Annals of Oncology 13:4, pages 582-588.
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John Roboz. 2002. Mass Spectrometry in Cancer Research. Mass Spectrometry in Cancer Research 201 360 .
Harriet O. Smith, John A. Blessing & Luis Vaccarello. (2002) Trimetrexate in the Treatment of Recurrent or Advanced Leiomyosarcoma of the Uterus: A Phase II Study of the Gynecologic Oncology Group. Gynecologic Oncology 84:1, pages 140-144.
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Stavit Drori, Gerrit Jansen, Robert Mauritz, Godefridus J. Peters & Yehuda G. Assaraf. (2000) Clustering of Mutations in the First Transmembrane Domain of the Human Reduced Folate Carrier in GW1843U89-resistant Leukemia Cells with Impaired Antifolate Transport and Augmented Folate Uptake. Journal of Biological Chemistry 275:40, pages 30855-30863.
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Kenneth D Bagshawe, Surinder K Sharma, Philip J Burke, Roger G Melton & Richard J Knox. (1999) Developments with targeted enzymes in cancer therapy. Current Opinion in Immunology 11:5, pages 579-583.
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Vladimir I. Polshakov, Berry Birdsall, Thomas A. Frenkiel, Angelo R. Gargaro & James Feeney. (2008) Structure and dynamics in solution of the complex of lactobacillus casei dihydrofolate reductase with the new lipophilic antifolate drug trimetrexate . Protein Science 8:3, pages 467-481.
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Gerrit Jansen, Robert Mauritz, Stavit Drori, Hannah Sprecher, Ietje Kathmann, Marlene Bunni, David G. Priest, Paul Noordhuis, Jan H. Schornagel, Herbert M. Pinedo, Godefridus J. Peters & Yehuda G. Assaraf. (1998) A Structurally Altered Human Reduced Folate Carrier with Increased Folic Acid Transport Mediates a Novel Mechanism of Antifolate Resistance. Journal of Biological Chemistry 273:46, pages 30189-30198.
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Claire Robson, KarenA Wright, PeterR Twentyman, PeterA Lambert & RogerJ Griffin. (1998) Chemical synthesis and biological properties of novel fluorescent antifolates in pgp- and mrp-overexpressing tumour cell lines. Biochemical Pharmacology 56:7, pages 807-816.
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A. O. Romero, J. E. Perez, M. A. Cuevas, J. A. Lacava, C. L. Sabatini, M. E. Dominguez, R. Rodriguez, M. R. Barbieri, E. H. Ortiz, M. A. Salvadori, L. A. Romero Acuña, J. M. Romero Acuña, M. J. Langhi, S. Amato, M. R. Machiavelli, B. A. Leone, C. T. Vallejo, V. Lorusso & M. DeLena. (1998) Double Modulation of 5-Fluorouracil by Methotrexate and High-Dose L-Leucovorin in Advanced Colorectal Cancer. American Journal of Clinical Oncology 21:1, pages 94-98.
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Andre Rosowsky, Clara E. Mota & Sherry E. Queener. (2009) Brominated trimetrexate analogues as inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase . Journal of Heterocyclic Chemistry 33:6, pages 1959-1966.
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