期刊
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
卷 590, 期 -, 页码 139-144出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2021.12.087
关键词
Mosquito; Larvae; Aedes aegypti; Pacifastin; Digestive enzymes
资金
- Fundacao de Amparoa Pesquisa do Estado de Sao Paulo (FAPESP) [2012/03657-8, 2019/03779-5]
- Conselho Nacional de Desenvolvimento Tecnologico (CNPq) [400835/2014-2, 302703/2017-9]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES/Brazil)
- INCT-Entomologia Molecular
In Brazil, the main vector of arboviruses is Aedes aegypti. A pacifastin protease inhibitor library was constructed and a mutant, TiPI6, was successfully selected to inhibit proteolytic activities of Ae. aegypti larvae. TiPI6 can control all three digestive enzyme activities present in the larval midgut extract and may be a candidate for further larvicidal studies.
In Brazil, the major vector of arboviruses is Aedes aegypti, which can transmit several alpha and flaviviruses. In this work, a pacifastin protease inhibitor library was constructed and used to select mutants for Ae. aegypti larvae digestive enzymes. The library contained a total of 3.25 x 10(5) cfu with random mutations in the reactive site (P2-P2'). The most successfully selected mutant, TiPI6, a versatile inhibitor, was able to inhibit all three Ae. aegypti larvae proteolytic activities, trypsin-like, chymotrypsin-like and elastase-like activities, with IC50 values of 0.212 nM, 0.107 nM and 0.109 nM, respectively. In conclusion, the TiPI mutated phage display library was shown to be a useful tool for the selection of an inhibitor of proteolytic activities combined in a mix. TiPI6 is capable of controlling all three digestive enzyme activities present in the larval midgut extract. To our knowledge, this is the first time that one inhibitor containing a Gln at the P1 position showed inhibitory activity against trypsin, chymotrypsin, and elastase-like activities. TiPI6 can be a candidate for further larvicidal studies. (C) 2021 Published by Elsevier Inc.
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