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Exploring epigenetic targets to fight neglected diseases: Selective sirtuin-2 inhibitors as leishmanicidal compounds

Grant number: 13/50677-7
Support Opportunities:Research Grants - Research Partnership for Technological Innovation - PITE
Duration: December 01, 2014 - December 11, 2016
Field of knowledge:Health Sciences - Pharmacy
Convênio/Acordo: GlaxoSmithKline
Principal Investigator:Flavio da Silva Emery
Grantee:Flavio da Silva Emery
Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
Host Company: Glaxosmithkline Brasil Ltda
City: Ribeirão Preto


The disease burden of leishmaniases is widely studied and is an important instrument to plan a strategy to control or prevent this disease. One featured scenario is the lack of innovation in drug discovery toward novel anti-parasitic agents to control and treat leishmaniases. This is an important concern, and the genome sequencing of several Leishmania species is able to accelerate the identification of new drug targets. In this context, the parasites epigenome rises as an interesting target to drug discovery programs. Epigenetics comprises a series of chemical modifications of DNA and their associated histone proteins and it is known to be an especially important aspect of parasite biology, although it is underexplored in drug discovery programs. In this context, this project targets at the parasitic Sirtuins, which are important epigenetic regulator enzymes that acts in the deacetylation of the N-terminal tails of histones. This family of proteins is known to be essential for parasitic growth and the recent identification of sirtuin-related gene from L. amazonensis opened the possibility for the development of novel and specific sirtuin-based drugs. Our proposal is to develop a library of inhibitors for L. amazonensis sirtuin-2 based on a computer-aided drug discovery and classical medicinal chemistry approaches. The proposal is multidisciplinary and brings together molecular parasitology, enzymology, medicinal chemistry, organic synthesis and pharmacology toward the development of a versatile platform to explore the epigenetic of L. amazonensis to find drug candidates to treat leishmaniasis and also diseases caused by other trypanosomatides. (AU)

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Scientific publications (4)
(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)
VAIDERGORN, MIGUEL M.; EMERY, FLAVIO DA SILVA; GANESAN, A.. From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD plus FBDD). Journal of Medicinal Chemistry, v. 64, n. 19, p. 13980-14010, . (17/21146-4, 13/50677-7)
TROSSINI, GUSTAVO H. G.; MALTAROLLO, VINICIUS G.; GARCIA, RICARDO D'A.; PINTO, CLAUDINEIA A. S. O.; VELASCO, MARIA V. R.; HONORIO, KATHIA M.; BABY, ANDRE R.. Theoretical study of tautomers and photoisomers of avobenzone by DFT methods. Journal of Molecular Modeling, v. 21, n. 12, . (13/50677-7)
TROSSINI, GUSTAVO H. G.; MALTAROLLO, VINICIUS G.; SCHMIDT, THOMAS J.. Hologram QSAR Studies of Antiprotozoal Activities of Sesquiterpene Lactones. Molecules, v. 19, n. 7, p. 10546-10562, . (11/11499-0, 13/50677-7)
GIL DE MELO, SHAIANI MARIA; DIAS DE REZENDE, LUCAS CUNHA; PETRILLI, RAQUEL; VIANNA LOPEZ, RENATA FONSECA; GOULART, MARILIA O. F.; EMERY, FLAVIO DA SILVA. Nitrosation of BODIPY dyes and their applications in the development of thiol sensors. DYES AND PIGMENTS, v. 173, . (13/50677-7, 14/18973-8, 11/23342-9, 14/22451-7, 17/21146-4)

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