Valente, María Vidal, Antonio E. and González Pacanowska, Dolores 2016. Comprehensive Analysis of Parasite Biology: From Metabolism to Drug Discovery.
Martins Alho, Miriam A. Marrero-Ponce, Yovani Barigye, Stephen J. Meneses-Marcel, Alfredo Machado Tugores, Yanetsy Montero-Torres, Alina Gómez-Barrio, Alicia Nogal, Juan J. García-Sánchez, Rory N. Vega, María Celeste Rolón, Miriam Martínez-Fernández, Antonio R. Escario, José A. Pérez-Giménez, Facundo Garcia-Domenech, Ramón Rivera, Norma Mondragón, Ricardo Mondragón, Mónica Ibarra-Velarde, Froylán Lopez-Arencibia, Atteneri Martín-Navarro, Carmen Lorenzo-Morales, Jacob Cabrera-Serra, Maria Gabriela Piñero, Jose Tytgat, Jan Chicharro, Roberto and Arán, Vicente J. 2014. Antiprotozoan lead discovery by aligning dry and wet screening: Prediction, synthesis, and biological assay of novel quinoxalinones. Bioorganic & Medicinal Chemistry, Vol. 22, Issue. 5, p. 1568.
Munday, J. C. Eze, A. A. Baker, N. Glover, L. Clucas, C. Aguinaga Andres, D. Natto, M. J. Teka, I. A. McDonald, J. Lee, R. S. Graf, F. E. Ludin, P. Burchmore, R. J. S. Turner, C. M. R. Tait, A. MacLeod, A. Maser, P. Barrett, M. P. Horn, D. and De Koning, H. P. 2014. Trypanosoma brucei aquaglyceroporin 2 is a high-affinity transporter for pentamidine and melaminophenyl arsenic drugs and the main genetic determinant of resistance to these drugs. Journal of Antimicrobial Chemotherapy, Vol. 69, Issue. 3, p. 651.
Ritt, Jean-François Raymond, Frédéric Leprohon, Philippe Légaré, Danielle Corbeil, Jacques Ouellette, Marc and Jardim, Armando 2013. Gene Amplification and Point Mutations in Pyrimidine Metabolic Genes in 5-Fluorouracil Resistant Leishmania infantum. PLoS Neglected Tropical Diseases, Vol. 7, Issue. 11, p. e2564.
Arakaki, Tracy L. Buckner, Frederick S. Gillespie, J. Robert Malmquist, Nicholas A. Phillips, Margaret A. Kalyuzhniy, Oleksandr Luft, Joseph R. DeTitta, George T. Verlinde, Christophe L. M. J. Van Voorhis, Wesley C. Hol, Wim G. J. and Merritt, Ethan A. 2008. Characterization of Trypanosoma brucei dihydroorotate dehydrogenase as a possible drug target; structural, kinetic and RNAi studies. Molecular Microbiology, Vol. 68, Issue. 1, p. 37.
Goudela, Sophia Reichard, Utz Amillis, Sotiris and Diallinas, George 2008. Characterization and kinetics of the major purine transporters in Aspergillus fumigatus. Fungal Genetics and Biology, Vol. 45, Issue. 4, p. 459.
Gould, Matthew K. Vu, Xuan Lan Seebeck, Thomas and de Koning, Harry P. 2008. Propidium iodide-based methods for monitoring drug action in the kinetoplastidae: Comparison with the Alamar Blue assay. Analytical Biochemistry, Vol. 382, Issue. 2, p. 87.
Papageorgiou, I. De Koning, H.P. Soteriadou, K. and Diallinas, G. 2008. Kinetic and mutational analysis of the Trypanosoma brucei NBT1 nucleobase transporter expressed in Saccharomyces cerevisiae reveals structural similarities between ENT and MFS transporters. International Journal for Parasitology, Vol. 38, Issue. 6, p. 641.
Vlanti, Anna and Diallinas, George 2008. The Aspergillus nidulans FcyB cytosine-purine scavenger is highly expressed during germination and in reproductive compartments and is downregulated by endocytosis. Molecular Microbiology, Vol. 68, Issue. 4, p. 959.
Amillis, Sotiris Hamari, Zsuzsanna Amillis, Sotiris Hamari, Zsuzsanna Roumelioti, Katerina Scazzocchio, Claudio and Diallinas, George 2007. Regulation of expression and kinetic modeling of substrate interactions of a uracil transporter inAspergillus nidulans. Molecular Membrane Biology, Vol. 24, Issue. 3, p. 206.
de Koning, Harry P. 2007. Pyrimidine transporters of trypanosomes – a class apart?. Trends in Parasitology, Vol. 23, Issue. 5, p. 190.
Gudin, Simon Quashie, Neils B. Candlish, Denise Al-Salabi, Mohammed I. Jarvis, Simon M. Ranford-Cartwright, Lisa C. and de Koning, Harry P. 2006. Trypanosoma brucei: A survey of pyrimidine transport activities. Experimental Parasitology, Vol. 114, Issue. 2, p. 118.
de Koning, Harry P. Bridges, Daniel J. and Burchmore, Richard J.S. 2005. Purine and pyrimidine transport in pathogenic protozoa: From biology to therapy. FEMS Microbiology Reviews, Vol. 29, Issue. 5, p. 987.
While purine transport has been widely studied in protozoa, almost nothing is known about their capacity to salvage pyrimidines. Here, we report a Leishmania major transporter with high affinity for uracil (Km=0·32±0·07 μM) which we designated LmU1. This transporter displayed a high degree of specificity, as it had virtually no affinity for cytosine, thymine or purine nucleobases, nor did it transport pyrimidine nucleosides. Highest affinity was for 5-fluorouracil. The results show that the permeant binding site of LmU1 interacts strongly with the keto groups of uracil, as shown by a low affinity for 2-thio- and 4-thiouracil. LmU1 appears to further bind uracil through a weak hydrogen bond with N(1)H of the pyrimidine ring in addition to a stronger H-bond with N(3)H. Substrate binding and selectivity were strikingly similar to that of the U1 transporter in the related kinetoplastid Trypanosoma brucei. Uracil analogues likely to be transported by LmU1 were also screened for antileishmanial activity, with 5-fluorouracil displaying strong activity against promastigotes and intracellular amastigotes. Overall, the results show that, like purine nucleobase transport, pyrimidine nucleobase transport function is very similar in L. major and T. brucei insect forms.
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