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Design of new antibiotics based in the fragment based drug discovery technique from the inhibition of vitamin biosynthesis in Mycobacterium tuberculosis

Grant number: 13/26242-0
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): July 01, 2014
Effective date (End): June 30, 2017
Field of knowledge:Biological Sciences - Microbiology
Cooperation agreement: Coordination of Improvement of Higher Education Personnel (CAPES)
Principal researcher:Marcio Vinicius Bertacine Dias
Grantee:Jademilson Celestino dos Santos
Home Institution: Instituto de Ciências Biomédicas (ICB). Universidade de São Paulo (USP). São Paulo , SP, Brazil
Associated research grant:10/15971-3 - Structural characterization of enzymes from antibiotic biosynthetic pathways with biotechnological interest, AP.JP


Infectious diseases are one serious problems of public health worldwide and are one most import causes of death of human population. Among these diseases, tuberculosis has a pivotal importance, because it is one of the infectious diseases which more decimates people around the world. This event occurs mainly because to the emerging of resistant strains to all medicine in use. Although the known public health problems related to this disease, there is not a strong investment of the pharmaceutical companies in the development of new drugs. Thus, the research using public funding represents an important role in the research and development of new drugs. Among the strategies, the discovery of inhibitors for the enzymes from biosynthesis of vitamins has already been largely investigated in Mycobacterium tuberculosis. The biosynthetic pathways of folate and biotin have target enzymes that can be used in the design of new antibiotics against Mycobacterium tuberculosis. At moment, there is not any antibiotic targeting these pathway in the treatment of tuberculosis. In this project, we intent to use the fragment based drug discovery technique to identify small and simple molecules that may be chemically modified to generated new inhibitors targeting the folate and biotin pathway in M. tuberculosis. To apply this approach, a set of biophysical techniques will be applied in the screening and validation of small molecules that may bind on these enzymes active site. (AU)

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