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Application of mass spectrometry for the identification of HIV-1 protease inhibitors in plants from Cerrado and Atlantic Rainforest: a modern enzymatic tool for searching new therapeutic agents using the dereplication methodology

Grant number: 06/61795-7
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): April 01, 2007
Effective date (End): August 31, 2011
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Principal Investigator:Vanderlan da Silva Bolzani
Grantee:Otavio Aparecido Flausino Junior
Home Institution: Instituto de Química (IQ). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Associated research grant:03/02176-7 - Conservation and sustainable use of the diversity from Cerrado and Atlantic Forest: chemical diversity and prospecting for potential drugs - phase II, AP.BTA.TEM

Abstract

The discovery of new anti HIV drugs still being a challenge to treat AIDS, due to the high side effects of the medicines on the market nowadays, and also by the resistant virus strains to several medicines used in the AIDS therapy. Among several targets used to discover new anti-HIV drugs, the protease HIV, an essential enzyme of the replication viral process is a target used to discover new drugs. To date, the search for new drugs has had great advances, mainly those with focus on molecular biology, which all facets of cellular, and ultimately systemic functions. The biological assay formats are both in vitro cell based, and simple enzymes designed to serve as reference guide to pharmacology, and so, to handle up large amount of compounds. The high resolution new techniques as ultraviolet, fluorescence and mass spectrometry is available to perform the assays with hundreds samples as plants, fungi and marine organisms. This project deals with development of protease HIV enzyme assay to be used to screening hundreds samples (Semi-High-Throughput Screening - SHTS), using dereplication methodology by HPLC/ESI-MS spectrometry. (AU)