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Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae)

Protease inhibitors are widely studied since the unrestricted activity of proteases can cause extensive organ lesions. In particular, elastase activity is involved in the pathophysiology of acute lung injury, for example during SARS-CoV-2 infection, while serine proteases and thrombin-like proteases...

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Autores principales: Fratini, Emiliano, Rossi, Marianna Nicoletta, Spagoni, Lucrezia, Riccieri, Alessandra, Mancini, Emiliano, Polticelli, Fabio, Bologna, Marco Alberto, Mariottini, Paolo, Cervelli, Manuela
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9312475/
https://www.ncbi.nlm.nih.gov/pubmed/35883544
http://dx.doi.org/10.3390/biom12070988
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author Fratini, Emiliano
Rossi, Marianna Nicoletta
Spagoni, Lucrezia
Riccieri, Alessandra
Mancini, Emiliano
Polticelli, Fabio
Bologna, Marco Alberto
Mariottini, Paolo
Cervelli, Manuela
author_facet Fratini, Emiliano
Rossi, Marianna Nicoletta
Spagoni, Lucrezia
Riccieri, Alessandra
Mancini, Emiliano
Polticelli, Fabio
Bologna, Marco Alberto
Mariottini, Paolo
Cervelli, Manuela
author_sort Fratini, Emiliano
collection PubMed
description Protease inhibitors are widely studied since the unrestricted activity of proteases can cause extensive organ lesions. In particular, elastase activity is involved in the pathophysiology of acute lung injury, for example during SARS-CoV-2 infection, while serine proteases and thrombin-like proteases are involved in the development and/or pathology of the nervous system. Natural protease inhibitors have the advantage to be reversible and with few side effects and thus are increasingly considered as new drugs. Kunitz-type protease inhibitors (KTPIs), reported in the venom of various organisms, such as wasps, spiders, scorpions, and snakes, have been studied for their potent anticoagulant activity and widespread protease inhibitor activity. Putative KTPI anticoagulants have been identified in transcriptomic resources obtained for two blister beetle species, Lydus trimaculatus and Mylabris variabilis. The KTPIs of L. trimaculatus and M. variabilis were characterized by combined transcriptomic and bioinformatics methodologies. The full-length mRNA sequences were divided on the base of the sequence of the active sites of the putative proteins. In silico protein structure analyses of each group of translational products show the biochemical features of the active sites and the potential protease targets. Validation of these genes is the first step for considering these molecules as new drugs for use in medicine.
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spelling pubmed-93124752022-07-26 Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae) Fratini, Emiliano Rossi, Marianna Nicoletta Spagoni, Lucrezia Riccieri, Alessandra Mancini, Emiliano Polticelli, Fabio Bologna, Marco Alberto Mariottini, Paolo Cervelli, Manuela Biomolecules Article Protease inhibitors are widely studied since the unrestricted activity of proteases can cause extensive organ lesions. In particular, elastase activity is involved in the pathophysiology of acute lung injury, for example during SARS-CoV-2 infection, while serine proteases and thrombin-like proteases are involved in the development and/or pathology of the nervous system. Natural protease inhibitors have the advantage to be reversible and with few side effects and thus are increasingly considered as new drugs. Kunitz-type protease inhibitors (KTPIs), reported in the venom of various organisms, such as wasps, spiders, scorpions, and snakes, have been studied for their potent anticoagulant activity and widespread protease inhibitor activity. Putative KTPI anticoagulants have been identified in transcriptomic resources obtained for two blister beetle species, Lydus trimaculatus and Mylabris variabilis. The KTPIs of L. trimaculatus and M. variabilis were characterized by combined transcriptomic and bioinformatics methodologies. The full-length mRNA sequences were divided on the base of the sequence of the active sites of the putative proteins. In silico protein structure analyses of each group of translational products show the biochemical features of the active sites and the potential protease targets. Validation of these genes is the first step for considering these molecules as new drugs for use in medicine. MDPI 2022-07-15 /pmc/articles/PMC9312475/ /pubmed/35883544 http://dx.doi.org/10.3390/biom12070988 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Fratini, Emiliano
Rossi, Marianna Nicoletta
Spagoni, Lucrezia
Riccieri, Alessandra
Mancini, Emiliano
Polticelli, Fabio
Bologna, Marco Alberto
Mariottini, Paolo
Cervelli, Manuela
Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae)
title Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae)
title_full Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae)
title_fullStr Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae)
title_full_unstemmed Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae)
title_short Molecular Characterization of Kunitz-Type Protease Inhibitors from Blister Beetles (Coleoptera, Meloidae)
title_sort molecular characterization of kunitz-type protease inhibitors from blister beetles (coleoptera, meloidae)
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9312475/
https://www.ncbi.nlm.nih.gov/pubmed/35883544
http://dx.doi.org/10.3390/biom12070988
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