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Items: 1 to 20 of 81

1.

Exploiting the 2-Amino-1,3,4-thiadiazole Scaffold To Inhibit Trypanosoma brucei Pteridine Reductase in Support of Early-Stage Drug Discovery.

Linciano P, Dawson A, Pöhner I, Costa DM, Sá MS, Cordeiro-da-Silva A, Luciani R, Gul S, Witt G, Ellinger B, Kuzikov M, Gribbon P, Reinshagen J, Wolf M, Behrens B, Hannaert V, Michels PAM, Nerini E, Pozzi C, di Pisa F, Landi G, Santarem N, Ferrari S, Saxena P, Lazzari S, Cannazza G, Freitas-Junior LH, Moraes CB, Pascoalino BS, Alcântara LM, Bertolacini CP, Fontana V, Wittig U, Müller W, Wade RC, Hunter WN, Mangani S, Costantino L, Costi MP.

ACS Omega. 2017 Sep 30;2(9):5666-5683. doi: 10.1021/acsomega.7b00473. Epub 2017 Sep 11.

2.

Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.

Linciano P, Pozzi C, Iacono LD, di Pisa F, Landi G, Bonucci A, Gul S, Kuzikov M, Ellinger B, Witt G, Santarem N, Baptista C, Franco C, Moraes CB, Müller W, Wittig U, Luciani R, Sesenna A, Quotadamo A, Ferrari S, Pöhner I, Cordeiro-da-Silva A, Mangani S, Costantino L, Costi MP.

J Med Chem. 2019 Apr 25;62(8):3989-4012. doi: 10.1021/acs.jmedchem.8b02021. Epub 2019 Apr 9.

PMID:
30908048
3.

Identification of Novel Potential Inhibitors of Pteridine Reductase 1 in Trypanosoma brucei via Computational Structure-Based Approaches and in Vitro Inhibition Assays.

Kimuda MP, Laming D, Hoppe HC, Tastan Bishop Ö.

Molecules. 2019 Jan 1;24(1). pii: E142. doi: 10.3390/molecules24010142.

4.

Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity.

Di Pisa F, Landi G, Dello Iacono L, Pozzi C, Borsari C, Ferrari S, Santucci M, Santarem N, Cordeiro-da-Silva A, Moraes CB, Alcantara LM, Fontana V, Freitas-Junior LH, Gul S, Kuzikov M, Behrens B, Pöhner I, Wade RC, Costi MP, Mangani S.

Molecules. 2017 Mar 8;22(3). pii: E426. doi: 10.3390/molecules22030426.

5.

Structure and reactivity of Trypanosoma brucei pteridine reductase: inhibition by the archetypal antifolate methotrexate.

Dawson A, Gibellini F, Sienkiewicz N, Tulloch LB, Fyfe PK, McLuskey K, Fairlamb AH, Hunter WN.

Mol Microbiol. 2006 Sep;61(6):1457-68.

6.

Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors.

Landi G, Linciano P, Borsari C, Bertolacini CP, Moraes CB, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Costi MP, Pozzi C, Mangani S.

ACS Infect Dis. 2019 May 1. doi: 10.1021/acsinfecdis.8b00358. [Epub ahead of print]

PMID:
31012301
7.

Pharmacophore Mapping, In Silico Screening and Molecular Docking to Identify Selective Trypanosoma brucei Pteridine Reductase Inhibitors.

Dube D, Sharma S, Singh TP, Kaur P.

Mol Inform. 2014 Feb;33(2):124-34. doi: 10.1002/minf.201300023. Epub 2014 Feb 2.

PMID:
27485569
8.

Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development.

Cavazzuti A, Paglietti G, Hunter WN, Gamarro F, Piras S, Loriga M, Allecca S, Corona P, McLuskey K, Tulloch L, Gibellini F, Ferrari S, Costi MP.

Proc Natl Acad Sci U S A. 2008 Feb 5;105(5):1448-53. doi: 10.1073/pnas.0704384105. Epub 2008 Feb 1.

9.

Structure-based design of pteridine reductase inhibitors targeting African sleeping sickness and the leishmaniases.

Tulloch LB, Martini VP, Iulek J, Huggan JK, Lee JH, Gibson CL, Smith TK, Suckling CJ, Hunter WN.

J Med Chem. 2010 Jan 14;53(1):221-9. doi: 10.1021/jm901059x.

10.

Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1.

Khalaf AI, Huggan JK, Suckling CJ, Gibson CL, Stewart K, Giordani F, Barrett MP, Wong PE, Barrack KL, Hunter WN.

J Med Chem. 2014 Aug 14;57(15):6479-94. doi: 10.1021/jm500483b. Epub 2014 Jul 29.

11.

Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1.

Spinks D, Ong HB, Mpamhanga CP, Shanks EJ, Robinson DA, Collie IT, Read KD, Frearson JA, Wyatt PG, Brenk R, Fairlamb AH, Gilbert IH.

ChemMedChem. 2011 Feb 7;6(2):302-8. doi: 10.1002/cmdc.201000450. Epub 2010 Dec 29.

12.

High-resolution structures of Trypanosoma brucei pteridine reductase ligand complexes inform on the placement of new molecular entities in the active site of a potential drug target.

Dawson A, Tulloch LB, Barrack KL, Hunter WN.

Acta Crystallogr D Biol Crystallogr. 2010 Dec;66(Pt 12):1334-40. doi: 10.1107/S0907444910040886. Epub 2010 Nov 16.

13.

Virtual screening identification of nonfolate compounds, including a CNS drug, as antiparasitic agents inhibiting pteridine reductase.

Ferrari S, Morandi F, Motiejunas D, Nerini E, Henrich S, Luciani R, Venturelli A, Lazzari S, Calò S, Gupta S, Hannaert V, Michels PA, Wade RC, Costi MP.

J Med Chem. 2011 Jan 13;54(1):211-21. doi: 10.1021/jm1010572. Epub 2010 Dec 2.

PMID:
21126022
14.

PTR1: a reductase mediating salvage of oxidized pteridines and methotrexate resistance in the protozoan parasite Leishmania major.

Bello AR, Nare B, Freedman D, Hardy L, Beverley SM.

Proc Natl Acad Sci U S A. 1994 Nov 22;91(24):11442-6.

15.

Biochemical and genetic tests for inhibitors of Leishmania pteridine pathways.

Hardy LW, Matthews W, Nare B, Beverley SM.

Exp Parasitol. 1997 Nov;87(3):157-69.

PMID:
9371081
16.

Structure-guided discovery of thiazolidine-2,4-dione derivatives as a novel class of Leishmania major pteridine reductase 1 inhibitors.

Leite FHA, Santiago PBGDS, Froes TQ, da Silva Filho J, da Silva SG, Ximenes RM, de Faria AR, Brondani DJ, de Albuquerque JFC, Castilho MS.

Eur J Med Chem. 2016 Nov 10;123:639-648. doi: 10.1016/j.ejmech.2016.07.060. Epub 2016 Jul 25.

PMID:
27517809
17.

Toward the development of dual-targeted glyceraldehyde-3-phosphate dehydrogenase/trypanothione reductase inhibitors against Trypanosoma brucei and Trypanosoma cruzi.

Belluti F, Uliassi E, Veronesi G, Bergamini C, Kaiser M, Brun R, Viola A, Fato R, Michels PA, Krauth-Siegel RL, Cavalli A, Bolognesi ML.

ChemMedChem. 2014 Feb;9(2):371-82. doi: 10.1002/cmdc.201300399. Epub 2014 Jan 8.

PMID:
24403089
18.

Crystal structure of Trypanosoma cruzi pteridine reductase 2 in complex with a substrate and an inhibitor.

Schormann N, Pal B, Senkovich O, Carson M, Howard A, Smith C, Delucas L, Chattopadhyay D.

J Struct Biol. 2005 Oct;152(1):64-75.

PMID:
16168672
19.

Dissecting the metabolic roles of pteridine reductase 1 in Trypanosoma brucei and Leishmania major.

Ong HB, Sienkiewicz N, Wyllie S, Fairlamb AH.

J Biol Chem. 2011 Mar 25;286(12):10429-38. doi: 10.1074/jbc.M110.209593. Epub 2011 Jan 14.

20.

New approaches to Leishmania chemotherapy: pteridine reductase 1 (PTR1) as a target and modulator of antifolate sensitivity.

Nare B, Luba J, Hardy LW, Beverley S.

Parasitology. 1997;114 Suppl:S101-10. Review.

PMID:
9309772

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