Development of capillary columns enzymatic to application of screening of selective inhibitors for the enzyme NTPDase- 2 of Leishmania infantun

• Grant number: 12/10749-6
• Support Opportunities: Scholarships in Brazil - Doctorate
• Start date: December 01, 2012
• End date: April 30, 2015
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Carmen Lúcia Cardoso
• Grantee: Luana Magalhães
• Host Institution: Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto (FFCLRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Associated research grant: 08/04371-5 - Development and applications of enzymatic columns in selective inhibitors screening and in the natural products studies, AP.JP

Abstract

One of the strategies used in the development of new drugs involves the discovery of compounds that modulate the enzymatic activity which is important in the infectious process of pathogenic agents. One interesting approach in the new ligands screening is the use of methods based in the enzyme immobilization in chromatographic supports coupling liquid chromatography systems multi and/or unidimensional. The use of IMERs (immobilized enzyme reactors) as stationary phase coupling high performance liquid chromatography is a fast and efficient screening method of compounds libraries or natural extracts. There are several advantages on using immobilized enzyme against the use of the enzyme in solution such as: easy separation of formed products, improvement in the enzyme stability and use of small amount of sample. The enzyme NTPDase2 of Leishmania favors the pathogen infection, it inhibits the host immune answer allowing a silent infection. The inhibitors screening for this enzyme can bring important alternatives for the treatment of leishmaniose and provide better life quality to affected populations by endemics diseases. In this study the NTPDase2 will be immobilized for the construction of ICERs (Immobilized Capillary Enzyme Reactors) that will be applied in the identification of active substances in synthetic and/or natural compounds libraries using chromatographic systems.

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

MAGALHAES, LUANA; CAVALCANTE DE OLIVEIRA, ARTHUR HENRIQUE; VASCONCELLOS, RAPHAEL DE SOUZA; MARIOTINI-MOURA, CHRISTIANE; FIRMINO, RAFAELA DE CASSIA; RANGEL FIETTO, JULIANA LOPES; CARDOSO, CARMEN LUCIA. Label-free assay based on immobilized capillary enzyme reactor of Leishmania infantum nucleoside triphosphate diphosphohydrolase (LicNTPDase-2-ICER-LC/UV). JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, v. 1008, p. 98-107, JAN 1 2016. (13/01710-1, 12/10749-6)