Design, synthesis, and evaluation of Bothrops venom serine protease peptidic inhibitors
dc.contributor.author
dc.date.accessioned
2021-02-16T12:18:06Z
dc.date.available
2021-02-16T12:18:06Z
dc.date.issued
2021-01-15
dc.identifier.issn
1678-9199
dc.identifier.uri
dc.description.abstract
Background: In Central and South America, snakebite envenomation is mainly caused by Bothrops spp. snakes, whose venoms feature significant biochemical richness, including serine proteases. The available bothropic antivenoms are efficient in avoiding fatalities, but do not completely neutralize venom serine proteases, which are co-responsible for some disorders observed during envenomation. Methods: In order to search for tools to improve the antivenom’s, 6-mer peptides were designed based on a specific substrate for Bothrops jararaca venom serine proteases, and then synthesized, with the intention to selectively inhibit these enzymes. Results: Using batroxobin as a snake venom serine protease model, two structurally similar inhibitor peptides were identified. When tested on B. jararaca venom, one of the new inhibitors displayed a good potential to inhibit the activity of the venom serine proteases. These inhibitors do not affect human serine proteases as human factor Xa and thrombin, due to their selectivity. Conclusion: Our study identified two small peptides able to inhibit bothropic serine proteases, but not human ones, can be used as tools to enhance knowledge of the venom composition and function. Moreover, one promising peptide (pepC) was identified that can be explored in the search for improving Bothrops spp. envenomation treatment
dc.description.sponsorship
This work was supported by grants from the São Paulo Research
Foundation (FAPESP – 2017/04321-7; Cetics (2013/07467-1),
Coordination for the Improvement of Higher Education
Personnel (CAPES) and Fundação Butantan
dc.format.mimetype
application/pdf
dc.language.iso
eng
dc.publisher
São Paulo State University (UNESP). Center for the Study of Venoms and Venomous Animals (CEVAP)
dc.relation.isformatof
Reproducció digital del document publicat a: https://doi.org/10.1590/1678-9199-JVATITD-2020-0066
dc.relation.ispartof
Journal of Venomous Animals and Toxins including Tropical Diseases (JVATiTD) , 2021, vol. 27, art. núm. e20200066
dc.relation.ispartofseries
Articles publicats (D-Q)
dc.rights
Attribution 4.0 International
dc.rights.uri
dc.subject
dc.title
Design, synthesis, and evaluation of Bothrops venom serine protease peptidic inhibitors
dc.type
info:eu-repo/semantics/article
dc.rights.accessRights
info:eu-repo/semantics/openAccess
dc.type.version
info:eu-repo/semantics/publishedVersion
dc.identifier.doi
dc.identifier.idgrec
032713
dc.type.peerreviewed
peer-reviewed