Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease

Diabetic kidney disease is one of the fastest growing causes of death worldwide. Epigenetic regulators control gene expression and are potential therapeutic targets. There is functional interventional evidence for a role of DNA methylation and the histone post-translational modifications—histone met...

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Autores: Martinez-Moreno, Julio M., Fontecha-Barriuso, Miguel, Martin-Sanchez, Diego, Guerrero-Mauvecin, Juan, Goma-Garces, Elena, Fernández Fernández, Beatriz, Carriazo, Sol, Sánchez Niño, María Dolores, Ramos, Adrian M., Ruiz Ortega, Marta, Ortiz Arduán, Alberto, Sanz, Ana Belén
Formato: artículo
Fecha de publicación:2020
País:España
Recursos:Universidad Autónoma de Madrid
Repositorio:Biblos-e Archivo. Repositorio Institucional de la UAM
Idioma:inglés
OAI Identifier:oai:repositorio.uam.es:10486/694819
Acesso em linha:http://hdl.handle.net/10486/694819
https://dx.doi.org/10.3390/ijms21114113
Access Level:acceso abierto
Palavra-chave:Apabetalone
BET
Chronic kidney disease
Crotonylation
Diabetes
Diabetic kidney disease
DNA methylation
Epigenetic
Farmacia
Medicina
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spelling Epigenetic modifiers as potential therapeutic targets in diabetic kidney diseaseMartinez-Moreno, Julio M.Fontecha-Barriuso, MiguelMartin-Sanchez, DiegoGuerrero-Mauvecin, JuanGoma-Garces, ElenaFernández Fernández, BeatrizCarriazo, SolSánchez Niño, María DoloresRamos, Adrian M.Ruiz Ortega, MartaOrtiz Arduán, AlbertoSanz, Ana BelénApabetaloneBETChronic kidney diseaseCrotonylationDiabetesDiabetic kidney diseaseDNA methylationEpigeneticFarmaciaMedicinaDiabetic kidney disease is one of the fastest growing causes of death worldwide. Epigenetic regulators control gene expression and are potential therapeutic targets. There is functional interventional evidence for a role of DNA methylation and the histone post-translational modifications—histone methylation, acetylation and crotonylation—in the pathogenesis of kidney disease, including diabetic kidney disease. Readers of epigenetic marks, such as bromodomain and extra terminal (BET) proteins, are also therapeutic targets. Thus, the BD2 selective BET inhibitor apabetalone was the first epigenetic regulator to undergo phase-3 clinical trials in diabetic kidney disease with an endpoint of kidney function. The direct therapeutic modulation of epigenetic features is possible through pharmacological modulators of the specific enzymes involved and through the therapeutic use of the required substrates. Of further interest is the characterization of potential indirect effects of nephroprotective drugs on epigenetic regulation. Thus, SGLT2 inhibitors increase the circulating and tissue levels of β-hydroxybutyrate, a molecule that generates a specific histone modification, β-hydroxybutyrylation, which has been associated with the beneficial health effects of fasting. To what extent this impact on epigenetic regulation may underlie or contribute to the so-far unclear molecular mechanisms of cardio-and nephroprotection offered by SGLT2 inhibitors merits further in-depth studies.This research was funded by FIS/FEDER funds (PI15/00298, CP14/00133, PI16/01900, PI18/01386, PI18/0133, PI19/00588, PI19/00815, DTS18/00032, ERA-PerMed-JTC2018 (KIDNEY ATTACK AC18/00064 and PERSTIGAN AC18/00071), ISCIII-RETIC REDinREN RD016/0009), Sociedad Española de Nefrología, FRIAT, Comunidad de Madrid en Biomedicina B2017/BMD- 3686 CIFRA2-CM. Salary support: ISCIII Miguel Servet to ABS and MDS-N, ISCIII Sara Borrell to JM-MM, REDinREN RD016/0009 to MF-B, and MICIU to JG-M.MDPI, Basel, SMwitzerlandDepartamento de FarmacologíaDepartamento de MedicinaFacultad de MedicinaInstituto de Investigación Sanitaria Fundación Jiménez Díaz (IIS-FJD)20202020-06-09research articlehttp://purl.org/coar/resource_type/c_2df8fbb1VoRhttp://purl.org/coar/version/c_970fb48d4fbd8a85info:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10486/694819https://dx.doi.org/10.3390/ijms21114113reponame:Biblos-e Archivo. Repositorio Institucional de la UAMinstname:Universidad Autónoma de MadridInglésengopen accesshttp://purl.org/coar/access_right/c_abf2info:eu-repo/semantics/openAccessoai:repositorio.uam.es:10486/6948192026-06-23T12:46:27Z
dc.title.none.fl_str_mv Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
title Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
spellingShingle Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
Martinez-Moreno, Julio M.
Apabetalone
BET
Chronic kidney disease
Crotonylation
Diabetes
Diabetic kidney disease
DNA methylation
Epigenetic
Farmacia
Medicina
title_short Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
title_full Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
title_fullStr Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
title_full_unstemmed Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
title_sort Epigenetic modifiers as potential therapeutic targets in diabetic kidney disease
dc.creator.none.fl_str_mv Martinez-Moreno, Julio M.
Fontecha-Barriuso, Miguel
Martin-Sanchez, Diego
Guerrero-Mauvecin, Juan
Goma-Garces, Elena
Fernández Fernández, Beatriz
Carriazo, Sol
Sánchez Niño, María Dolores
Ramos, Adrian M.
Ruiz Ortega, Marta
Ortiz Arduán, Alberto
Sanz, Ana Belén
author Martinez-Moreno, Julio M.
author_facet Martinez-Moreno, Julio M.
Fontecha-Barriuso, Miguel
Martin-Sanchez, Diego
Guerrero-Mauvecin, Juan
Goma-Garces, Elena
Fernández Fernández, Beatriz
Carriazo, Sol
Sánchez Niño, María Dolores
Ramos, Adrian M.
Ruiz Ortega, Marta
Ortiz Arduán, Alberto
Sanz, Ana Belén
author_role author
author2 Fontecha-Barriuso, Miguel
Martin-Sanchez, Diego
Guerrero-Mauvecin, Juan
Goma-Garces, Elena
Fernández Fernández, Beatriz
Carriazo, Sol
Sánchez Niño, María Dolores
Ramos, Adrian M.
Ruiz Ortega, Marta
Ortiz Arduán, Alberto
Sanz, Ana Belén
author2_role author
author
author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Departamento de Farmacología
Departamento de Medicina
Facultad de Medicina
Instituto de Investigación Sanitaria Fundación Jiménez Díaz (IIS-FJD)
dc.subject.none.fl_str_mv Apabetalone
BET
Chronic kidney disease
Crotonylation
Diabetes
Diabetic kidney disease
DNA methylation
Epigenetic
Farmacia
Medicina
topic Apabetalone
BET
Chronic kidney disease
Crotonylation
Diabetes
Diabetic kidney disease
DNA methylation
Epigenetic
Farmacia
Medicina
description Diabetic kidney disease is one of the fastest growing causes of death worldwide. Epigenetic regulators control gene expression and are potential therapeutic targets. There is functional interventional evidence for a role of DNA methylation and the histone post-translational modifications—histone methylation, acetylation and crotonylation—in the pathogenesis of kidney disease, including diabetic kidney disease. Readers of epigenetic marks, such as bromodomain and extra terminal (BET) proteins, are also therapeutic targets. Thus, the BD2 selective BET inhibitor apabetalone was the first epigenetic regulator to undergo phase-3 clinical trials in diabetic kidney disease with an endpoint of kidney function. The direct therapeutic modulation of epigenetic features is possible through pharmacological modulators of the specific enzymes involved and through the therapeutic use of the required substrates. Of further interest is the characterization of potential indirect effects of nephroprotective drugs on epigenetic regulation. Thus, SGLT2 inhibitors increase the circulating and tissue levels of β-hydroxybutyrate, a molecule that generates a specific histone modification, β-hydroxybutyrylation, which has been associated with the beneficial health effects of fasting. To what extent this impact on epigenetic regulation may underlie or contribute to the so-far unclear molecular mechanisms of cardio-and nephroprotection offered by SGLT2 inhibitors merits further in-depth studies.
publishDate 2020
dc.date.none.fl_str_mv 2020
2020-06-09
dc.type.none.fl_str_mv research article
http://purl.org/coar/resource_type/c_2df8fbb1
VoR
http://purl.org/coar/version/c_970fb48d4fbd8a85
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv http://hdl.handle.net/10486/694819
https://dx.doi.org/10.3390/ijms21114113
url http://hdl.handle.net/10486/694819
https://dx.doi.org/10.3390/ijms21114113
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv MDPI, Basel, SMwitzerland
publisher.none.fl_str_mv MDPI, Basel, SMwitzerland
dc.source.none.fl_str_mv reponame:Biblos-e Archivo. Repositorio Institucional de la UAM
instname:Universidad Autónoma de Madrid
instname_str Universidad Autónoma de Madrid
reponame_str Biblos-e Archivo. Repositorio Institucional de la UAM
collection Biblos-e Archivo. Repositorio Institucional de la UAM
repository.name.fl_str_mv
repository.mail.fl_str_mv
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