<abstract xmlns="http://www.w3.org/1999/xhtml">

<p>Protein kinases are enzymes involved in essential biological processes such as signal transduction, transcription, metabolism, and the cell cycle. Human kinases are targets for several drugs approved by the US Food and Drug Administration. Therefore, the identification and classification of kinases in other organisms, including pathogenic parasites, is an interesting subject of study. Monogeneans are platyhelminths, mainly ectoparasites, capable of causing health problems in farmed fish. Although some genomes and transcriptomes are available for monogenean species, their full repertoire of kinases is unknown. The aim of this study was to identify and classify the putative kinases in the transcriptomes of two monogeneans, <italic>Rhabdosynochus viridisi</italic> and <italic>Scutogyrus longicornis</italic>, and then to predict potential monogenean drug targets (MDTs) and selective inhibitor drugs using computational approaches. Monogenean kinases having orthologs in the lethal phenotype of <italic>C. elegans</italic> but not in fish or humans were considered MDTs. A total of 160 and 193 kinases were identified in <italic>R. viridisi</italic> and <italic>S. longicornis</italic>, respectively. Of these, 22 kinases, belonging mainly to the major groups CAMK, AGC, and TK, were classified as MDTs, five of which were evaluated further. Molecular docking analysis indicated that dihydroergotamine, ergotamine, and lomitapide have the highest affinity for the kinases BRSK and MEKK1. These well-known drugs could be evaluated in future studies for potential repurposing as anti-monogenean agents. The present study contributes valuable data for the development of new antiparasitic candidates for finfish aquaculture.</p>
</abstract>

Protein kinases are enzymes involved in essential biological processes such as signal transduction, transcription, metabolism, and the cell cycle. Human kinases are targets for several drugs approved by the US Food and Drug Administration. Therefore, the identification and classification of kinases in other organisms, including pathogenic parasites, is an interesting subject of study. Monogeneans are platyhelminths, mainly ectoparasites, capable of causing health problems in farmed fish. Although some genomes and transcriptomes are available for monogenean species, their full repertoire of kinases is unknown. The aim of this study was to identify and classify the putative kinases in the transcriptomes of two monogeneans, Rhabdosynochus viridisi and Scutogyrus longicornis, and then to predict potential monogenean drug targets (MDTs) and selective inhibitor drugs using computational approaches. Monogenean kinases having orthologs in the lethal phenotype of C. elegans but not in fish or humans were considered MDTs. A total of 160 and 193 kinases were identified in R. viridisi and S. longicornis, respectively. Of these, 22 kinases, belonging mainly to the major groups CAMK, AGC, and TK, were classified as MDTs, five of which were evaluated further. Molecular docking analysis indicated that dihydroergotamine, ergotamine, and lomitapide have the highest affinity for the kinases BRSK and MEKK1. These well-known drugs could be evaluated in future studies for potential repurposing as anti-monogenean agents. The present study contributes valuable data for the development of new antiparasitic candidates for finfish aquaculture.

Identifying potential drug targets in the kinomes of two monogenean species

Universidad Autónoma de Occidente, Unidad Regional Mazatlán

Instituto de Ciencias del Mar y Limnología

Universidad Nacional Autónoma de México

Helminthologia

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

{"article-title":"Identifying potential drug targets in the kinomes of two monogenean species"}

Protein kinases are enzymes involved in essential biological processes such as signal transduction, transcription, metabolism, and the cell cycle. Human...

Identifying potential drug targets in the kinomes of two monogenean species

Publicado en línea: 16 jul 2024

Páginas: 142 - 150

Recibido: 12 sept 2023

Aceptado: 24 may 2024

DOI: https://doi.org/10.2478/helm-2024-0020

Palabras clave
Ergotamine, aquaculture, fish parasites, genomics, Diplectanidae, Dactylogyridae

© 2024 V. H. Caña-Bozada et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Identifying potential drug targets in the kinomes of two monogenean species

Publicado en línea: 16 jul 2024

Páginas: 142 - 150

Recibido: 12 sept 2023

Aceptado: 24 may 2024

DOI: https://doi.org/10.2478/helm-2024-0020

Palabras claveErgotamine, aquaculture, fish parasites, genomics, Diplectanidae, Dactylogyridae

© 2024 V. H. Caña-Bozada et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Palabras clave
Ergotamine, aquaculture, fish parasites, genomics, Diplectanidae, Dactylogyridae