Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain

Correspondence: calderon@unir.br.

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Auteur principal: Alfonso Ruiz Díaz, Jorge Javier (author)
Autres auteurs: Gómez Garay, Ana Fidelina (author), Makoto Kayano, Anderson (author), Holanda, Rudson (author), Ferreira Francisco, Aleff (author), Collins Kuehn, Christian (author), Martins Soares, Andreimar (author), Vega Gómez, María Celeste (author), de Azevedo Calderon, Leonardo (author)
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Langue:anglais
Publié: 2025
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Accès en ligne:https://doi.org/10.1590/1678-9199-JVATITD-2024-0055
http://hdl.handle.net/20.500.14066/4647
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author Alfonso Ruiz Díaz, Jorge Javier
author2 Gómez Garay, Ana Fidelina
Makoto Kayano, Anderson
Holanda, Rudson
Ferreira Francisco, Aleff
Collins Kuehn, Christian
Martins Soares, Andreimar
Vega Gómez, María Celeste
de Azevedo Calderon, Leonardo
author2_role author
author
author
author
author
author
author
author
author_browse Alfonso Ruiz Díaz, Jorge Javier
Collins Kuehn, Christian
Ferreira Francisco, Aleff
Gómez Garay, Ana Fidelina
Holanda, Rudson
Makoto Kayano, Anderson
Martins Soares, Andreimar
Vega Gómez, María Celeste
de Azevedo Calderon, Leonardo
author_facet Alfonso Ruiz Díaz, Jorge Javier
Gómez Garay, Ana Fidelina
Makoto Kayano, Anderson
Holanda, Rudson
Ferreira Francisco, Aleff
Collins Kuehn, Christian
Martins Soares, Andreimar
Vega Gómez, María Celeste
de Azevedo Calderon, Leonardo
author_role author
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dc.creator.none.fl_str_mv Alfonso Ruiz Díaz, Jorge Javier
Gómez Garay, Ana Fidelina
Makoto Kayano, Anderson
Holanda, Rudson
Ferreira Francisco, Aleff
Collins Kuehn, Christian
Martins Soares, Andreimar
Vega Gómez, María Celeste
de Azevedo Calderon, Leonardo
dc.date.accessioned.none.fl_str_mv 2025-09-15T19:07:03Z
dc.date.available.none.fl_str_mv 2025-09-15T19:07:03Z
dc.date.issued.none.fl_str_mv 2025-02-14
dc.format.extent.es.fl_str_mv 16 páginas
dc.identifier.citation.en.fl_str_mv Alfonso Ruiz Díaz, J. J., Gómez Garay, A. F., Makoto Kayano, A., Holanda, R., Ferreira Francisco, A., Collins Kuehn, C., Martins Soares, A., Vega, C., & de Azevedo Calderon, L. (2025). Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain. Journal of Venomous Animals and Toxins including Tropical Diseases, 31, Article e20240055. https://doi.org/10.1590/1678-9199-JVATITD-2024-0055
dc.identifier.doi.es.fl_str_mv 10.1590/1678-9199-JVATITD-2024-0055
dc.identifier.essn.es.fl_str_mv 1678-9199
dc.identifier.other.es.fl_str_mv https://doi.org/10.1590/1678-9199-JVATITD-2024-0055
dc.identifier.uri.none.fl_str_mv http://hdl.handle.net/20.500.14066/4647
dc.language.iso.es.fl_str_mv eng
dc.publisher.es.fl_str_mv Universidade Estadual Paulista Júlio de Mesquita Filho. Centro de Estudos de Venenos e Animais Peçonhentos
dc.relation.projectCONACYT.es.fl_str_mv PRIA01-19
dc.rights.*.fl_str_mv Atribución/Reconocimiento 4.0 Internacional
dc.rights.accessRights.es.fl_str_mv info:eu-repo/semantics/openAccess
dc.rights.copyright.es.fl_str_mv © The Author(s).
dc.rights.uri.*.fl_str_mv http://creativecommons.org/licenses/by/4.0/
dc.subject.other.es.fl_str_mv Chagas disease
Cruzain
Cystatins
Inhibitors
Snake venom
dc.title.es.fl_str_mv Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
dc.type.es.fl_str_mv info:eu-repo/semantics/article
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description Correspondence: calderon@unir.br.
eu_rights_str_mv openAccess
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identifier_str_mv Alfonso Ruiz Díaz, J. J., Gómez Garay, A. F., Makoto Kayano, A., Holanda, R., Ferreira Francisco, A., Collins Kuehn, C., Martins Soares, A., Vega, C., & de Azevedo Calderon, L. (2025). Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain. Journal of Venomous Animals and Toxins including Tropical Diseases, 31, Article e20240055. https://doi.org/10.1590/1678-9199-JVATITD-2024-0055
10.1590/1678-9199-JVATITD-2024-0055
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language eng
network_acronym_str CONACYT
network_name_str Repositorio Institucional CONACYT
oai_identifier_str oai:repositorio.conacyt.gov.py:20.500.14066/4647
publishDate 2025
publishDateSort 2025
repository.mail.fl_str_mv repositorio.institucional@conacyt.gov.py
repository.name.fl_str_mv Repositorio Institucional CONACYT
repository_id_str
rights_invalid_str_mv Atribución/Reconocimiento 4.0 Internacional
http://creativecommons.org/licenses/by/4.0/
© The Author(s).
spelling 366005246009e4d774e-94cb-4d48-89c2-5514637cdcad600d62a9e27-e838-4930-8a1c-ee955a9122f7600f6994e64-295e-4e9f-b275-4d3b12ed318060062c0ede8-145b-4850-9f33-574c00e6e7d6600d45e8f58-9a60-400e-a716-f4743ef2cf2760011456000000-0001-6291-4316d0edc25a-6b0a-4625-b770-a7285baf8e126002025-09-15T19:07:03Z2025-09-15T19:07:03Z2025-02-14Alfonso Ruiz Díaz, J. J., Gómez Garay, A. F., Makoto Kayano, A., Holanda, R., Ferreira Francisco, A., Collins Kuehn, C., Martins Soares, A., Vega, C., & de Azevedo Calderon, L. (2025). Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain. Journal of Venomous Animals and Toxins including Tropical Diseases, 31, Article e20240055. https://doi.org/10.1590/1678-9199-JVATITD-2024-0055https://doi.org/10.1590/1678-9199-JVATITD-2024-0055http://hdl.handle.net/20.500.14066/464710.1590/1678-9199-JVATITD-2024-00551678-9199Correspondence: calderon@unir.br.Background: Chagas disease (CD), caused by Trypanosoma cruzi, affects approximately seven million individuals worldwide, with the highest number of cases in Latin America. CD has two phases, of which the chronic phase is characterized by reduced efficacy in drug therapies. This and other factors make developing new strategies that aim to identify molecules capable of becoming alternatives to or complement current chemotherapy vitally important. Methods: Cruzain and AsCystatin were obtained recombinantly through expression in E. coli. Bioinformatic assays were conducted with both molecules, followed by in vitro enzyme inhibition assays. Subsequently, in silico studies allowed for the design of peptides, which were then assessed for molecular interactions with cruzain. The designed peptides were synthesized, and their inhibitory potential on cruzain and their trypanocidal and cytotoxic effects in vitro were finally assessed. Results: AsCystatin, a potential inhibitor of cysteine proteases, was identified from previously published scientific literature. In silico assays suggested that AsCystatin interacts with key regions of cruzain, and was subsequently produced through heterologous expression, obtaining a protein with a high degree of purity. Next, the inhibition of AsCystatin on the activity of cruzain was assessed, observing that approximately 20 μM of cystatin could inhibit 50% of the catalytic activity of the recombinant enzyme. Based on the in-silico analysis performed previously, original, and modified peptides were designed and tested, which allowed for identifying four peptides with inhibitory capacity on the enzymatic activity of cruzain. Finally, three of these peptides showed trypanocidal activity on epimastigote forms of T. cruzi in in vitro models. Conclusion: It was possible to identify AsCystatin and four peptides derived from this protein with inhibitory activity on cruzain, highlighting the trypanocidal effect of these peptides observed in in vitro assays.Consejo Nacional de Ciencia y TecnologíaPrograma Paraguayo para el Desarrollo de la Ciencia y Tecnología. Programa Nacional de Incentivo a los InvestigadoresPrograma Paraguayo para el Desarrollo de la Ciencia y Tecnología. Programa de inserción de capital humano avanzado16 páginasengUniversidade Estadual Paulista Júlio de Mesquita Filho. Centro de Estudos de Venenos e Animais PeçonhentosAtribución/Reconocimiento 4.0 Internacionalhttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccess© The Author(s).Chagas diseaseCruzainCystatinsInhibitorsSnake venomCystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzaininfo:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionJournal of Venomous Animals and Toxins including Tropical DiseasesPRIA01-1931Alfonso Ruiz Díaz, Jorge JavierGómez Garay, Ana FidelinaMakoto Kayano, AndersonHolanda, RudsonFerreira Francisco, AleffCollins Kuehn, ChristianMartins Soares, AndreimarVega Gómez, María Celestede Azevedo Calderon, LeonardoORIGINALCystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain.pdfCystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain.pdfArtículo científicoapplication/pdf2770589http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4647/1/Cystatin%20from%20Austrelaps%20superbus%20snake%20venom%20as%20a%20model%20for%20identifying%20potential%20inhibitors%20of%20Trypanosoma%20cruzi%20cruzain.pdf20787e62a2c76b8f7c51cc5103f97f32MD51CC-LICENSElicense_rdflicense_rdfapplication/rdf+xml; charset=utf-8908http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4647/2/license_rdf0175ea4a2d4caec4bbcc37e300941108MD52LICENSElicense.txtlicense.txttext/plain; charset=utf-81698http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4647/3/license.txt858b22fda432bd774e469302988c1974MD53THUMBNAILCystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain.jpgCystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain.jpgVista de primera página de artículo científicoimage/jpeg418499http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4647/4/Cystatin%20from%20Austrelaps%20superbus%20snake%20venom%20as%20a%20model%20for%20identifying%20potential%20inhibitors%20of%20Trypanosoma%20cruzi%20cruzain.jpg19eefb91f79a3efd64b8d150e6140ccbMD54TEXTCystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain.pdf.txtCystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain.pdf.txtExtracted texttext/plain70686http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4647/5/Cystatin%20from%20Austrelaps%20superbus%20snake%20venom%20as%20a%20model%20for%20identifying%20potential%20inhibitors%20of%20Trypanosoma%20cruzi%20cruzain.pdf.txt23914ad55ca271b1e489f9d156639885MD5520.500.14066/4647oai:repositorio.conacyt.gov.py:20.500.14066/46472026-02-12 19:30:42.414Repositorio Institucional CONACYTrepositorio.institucional@conacyt.gov.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
spellingShingle Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
Alfonso Ruiz Díaz, Jorge Javier
Chagas disease
Cruzain
Cystatins
Inhibitors
Snake venom
status_str publishedVersion
title Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
title_full Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
title_fullStr Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
title_full_unstemmed Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
title_short Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
title_sort Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain
topic Chagas disease
Cruzain
Cystatins
Inhibitors
Snake venom
url https://doi.org/10.1590/1678-9199-JVATITD-2024-0055
http://hdl.handle.net/20.500.14066/4647