Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development
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Maria Paola Costi | Giuseppe Paglietti | Francisco Gamarro | Stefania Ferrari | Karen McLuskey | Mario Loriga | W. Hunter | F. Gamarro | S. Piras | P. Corona | F. Gibellini | William N Hunter | Federica Gibellini | S. Ferrari | Sandra Piras | Antonio Cavazzuti | Sergio Allecca | Paola Corona | Lindsay Tulloch | L. Tulloch | A. Cavazzuti | M. Loriga | G. Paglietti | K. McLuskey | Sergio Allecca | Federica Gibellini
[1] T. Mosmann. Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. , 1983, Journal of immunological methods.
[2] S. Castanys,et al. Characterization of an ABCA‐like transporter involved in vesicular trafficking in the protozoan parasite Trypanosoma cruzi , 2004, Molecular microbiology.
[3] W. Hunter,et al. Inhibition of Leishmania major pteridine reductase by 2,4,6-triaminoquinazoline: structure of the NADPH ternary complex. , 2004, Acta crystallographica. Section D, Biological crystallography.
[4] Gordon A. Leonard,et al. Pteridine reductase mechanism correlates pterin metabolism with drug resistance in trypanosomatid parasites , 2001, Nature Structural Biology.
[5] J. Dann,et al. Large-scale purification and characterization of dihydrofolate reductase from a methotrexate-resistant strain of Lactobacillus casei. , 1976, The Biochemical journal.
[6] L. Hardy,et al. New approaches to Leishmania chemotherapy: pteridine reductase 1 (PTR1) as a target and modulator of antifolate sensitivity , 1997, Parasitology.
[7] Maria Paola Costi,et al. Thymidylate synthase structure, function and implication in drug discovery. , 2005, Current medicinal chemistry.
[8] Stephen M Beverley,et al. Structures of Leishmania major pteridine reductase complexes reveal the active site features important for ligand binding and to guide inhibitor design. , 2005, Journal of molecular biology.
[9] S. Sundar,et al. Short-course of oral miltefosine for treatment of visceral leishmaniasis. , 2000, Clinical infectious diseases : an official publication of the Infectious Diseases Society of America.
[10] L. Hardy,et al. PTR1: a reductase mediating salvage of oxidized pteridines and methotrexate resistance in the protozoan parasite Leishmania major. , 1994, Proceedings of the National Academy of Sciences of the United States of America.
[11] R. Then. Antimicrobial Dihydrofolate Reductase Inhibitors - Achievements and Future Options: Review , 2004, Journal of chemotherapy.
[12] D. Herries. Enzyme Kinetics: Behaviour and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems: By Irwin H. Segel. John Wiley & Sons, 1975. pp xxii + 957. Boards, £15.00 , 1976 .
[13] G. Maley,et al. Properties of a defined mutant of Escherichia coli thymidylate synthase. , 1988, The Journal of biological chemistry.
[14] C. Plowe,et al. Mechanisms of Resistance of Malaria Parasites to Antifolates , 2005, Pharmacological Reviews.
[15] F. Lombardo,et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings , 1997 .
[16] D. Santi,et al. Purification and characterization of the bifunctional thymidylate synthetase-dihydrofolate reductase from methotrexate-resistant Leishmania tropica. , 1985, Biochemistry.
[17] R. Lambert,et al. A model for the efficacy of combined inhibitors , 2003, Journal of applied microbiology.
[18] V. Cody,et al. Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent. , 2000, Journal of medicinal chemistry.
[19] D. Hanahan. Studies on transformation of Escherichia coli with plasmids. , 1983, Journal of molecular biology.
[20] S. Castanys,et al. A pteridine reductase gene ptr1 contiguous to a P-glycoprotein confers resistance to antifolates in Trypanosoma cruzi. , 1997, Molecular and biochemical parasitology.
[21] J. Montgomery,et al. Preparation of 6-(bromomethyl)-2,4-pteridinediamine hydrobromide and its use in improved syntheses of methotrexate and related compounds. , 1977, The Journal of organic chemistry.
[22] L. Hardy,et al. Biochemical and Genetic Tests for Inhibitors ofLeishmaniaPteridine Pathways , 1997 .
[23] N. Schormann,et al. Trypanosoma cruzi genome encodes a pteridine reductase 2 protein. , 2003, Molecular and biochemical parasitology.
[24] V. Zilberfarb,et al. Destruction of Leishmania mexicana amazonensis amastigotes by leucine methyl ester: protection by other amino acid esters , 1987, Parasitology.
[25] P K Gessner,et al. Isobolographic analysis of interactions: an update on applications and utility. , 1995, Toxicology.
[26] R. Titus,et al. Regulation of Differentiation to the Infective Stage of the Protozoan Parasite Leishmania major by Tetrahydrobiopterin , 2001, Science.
[27] E. Shaw,et al. The Synthesis of 6-Hydroxymethylypteridines , 1964 .
[28] I. H. Segel. Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems , 1975 .
[29] G. Maley,et al. High-level expression of human thymidylate synthase. , 1997, Protein expression and purification.
[30] M. Ouellette,et al. Inactivation of the Leishmania tarentolae Pterin Transporter (BT1) and Reductase (PTR1) Genes Leads to Viable Parasites with Changes in Folate Metabolism and Hypersensitivity to the Antifolate Methotrexate* , 2004, Journal of Biological Chemistry.
[31] J. Montgomery,et al. A convenient synthesis of aminopterin and homologs via 6-(bromomethyl)-2,4-diaminopteridine hydrobromide , 1974 .
[32] A. Fairlamb,et al. Structure and reactivity of Trypanosoma brucei pteridine reductase: inhibition by the archetypal antifolate methotrexate , 2006, Molecular microbiology.
[33] D. Santi,et al. Purification and characterization of recombinant Pneumocystis carinii thymidylate synthase. , 1991, Protein expression and purification.
[34] Vivian Cody,et al. Understanding the role of Leu22 variants in methotrexate resistance: comparison of wild-type and Leu22Arg variant mouse and human dihydrofolate reductase ternary crystal complexes with methotrexate and NADPH. , 2005, Acta crystallographica. Section D, Biological crystallography.
[35] Maria Paola Costi,et al. Quinoxaline chemistry. Part 15. 4-[2-Quinoxalylmethylenimino]-benzoylglutamates and -benzoates, 4-[2-quinoxalylmethyl-N-methylamino]-benzoylglutamates as analogues of classical antifolate agents. Synthesis, elucidation of structures and in vitro evaluation of antifolate and anticancer activities. , 2003, Farmaco.
[36] Maria Paola Costi,et al. Quinoxaline chemistry. Part 11. 3-Phenyl-2[phenoxy- and phenoxymethyl]-6(7) or 6,8-substituted quinoxalines and N-[4-(6(7)-substituted or 6,8-disubstituted-3-phenylquinoxalin-2-yl)hydroxy or hydroxymethyl] benzoylglutamates. Synthesis and evaluation of in vitro anticancer activity and enzymatic inhi , 1998, Farmaco.
[37] D. Santi,et al. Cloning, expression and characterization of thymidylate synthase from Crypto coccus neoformans , 1994 .
[38] John J McGuire,et al. Anticancer antifolates: current status and future directions. , 2003, Current pharmaceutical design.
[39] L. DeLucas,et al. Crystal structure of Trypanosoma cruzi pteridine reductase 2 in complex with a substrate and an inhibitor. , 2005, Journal of structural biology.
[40] S. Piras,et al. Quinoxaline chemistry. Part XVII. Methyl [4-(substituted 2-quinoxalinyloxy) phenyl] acetates and ethyl N-([4-(substituted 2-quinoxalinyloxy) phenyl] acetyl) glutamates analogs of methotrexate: synthesis and evaluation of in vitro anticancer activity. , 2004, Farmaco.