| Grant number: | 17/07253-2 |
| Support type: | Multi-user Equipment Program |
| Duration: | June 01, 2017 - May 31, 2024 |
| Field of knowledge: | Biological Sciences - Parasitology |
| Principal Investigator: | Carsten Wrenger |
| Grantee: | Carsten Wrenger |
| Home Institution: | Instituto de Ciências Biomédicas (ICB). Universidade de São Paulo (USP). São Paulo , SP, Brazil |
| Associated research grant: | 15/26722-8 - Drug discovery against human infectious diseases, AP.TEM |
| As informações de acesso ao Equipamento Multiusuário são de responsabilidade do Pesquisador responsável | |
| EMU web page: | http://cefap.icb.usp.br/core-facilities/pluma/malvern-zetasizer-%c2%b5v-dlssls/ |
| Tipo de equipamento: | Caracterização de Materiais - Propriedades Físicas - Tamanho de partículas Caracterização de Materiais - Propriedades Físicas - Carga superficial (potencial zeta) |
| Fabricante: | Malvern |
| Modelo: | Zetasizer |
Abstract
Infectious diseases are a threat to mankind and currently the causative pathogens are spreading geographically due to globalization and developing drug resistance. Current resistance to chemotherapeutics is occurring to almost all pathogens and therefore new drug targets and/or novel modi of drug target efficacy is urgently needed. In this grant application the focus will be drawn on suicide drug discovery by exploiting the vitamin B1/B6 biosynthetic pathways of the human pathogens Plasmodium falciparum, the parasite responsible for predominate cases of severe malaria, and the multi-resistant bacteria Staphylococcus aureus MRSA. Compounds will be identified and designed for incorporation into pathogens' metabolism after crystal structure evaluation of the respective vitamin B1/B6 biosynthetic enzymes. Thereby the new compounds are intended to poison the respective vitamin-dependent enzyme. Counter selection will be performed against human cells as well as transgenically modified human cells which are expressing nuclear receptors for xenobiotic sensing as reporter gene chimeras. (AU)