Desmoplakin CSM models unravel mechanisms regulating the binding to intermediate filaments and putative therapeutics for cardiocutaneous diseases.


Journal

Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288

Informations de publication

Date de publication:
05 Oct 2024
Historique:
received: 21 05 2024
accepted: 19 09 2024
medline: 6 10 2024
pubmed: 6 10 2024
entrez: 5 10 2024
Statut: epublish

Résumé

Arrhythmogenic cardiomyopathy (AC) is a common cause of sudden cardiac arrest and death in young adults. It can be induced by different types of mutations throughout the desmoplakin gene including the R2834H mutation in the extreme carboxyterminus tail of desmoplakin (DP CT) which remains structurally uncharacterized and poorly understood. Here, we have created 3D models of DP CT which show the structural effects of AC-inducing mutations as well as the implications of post-translational modifications (PTMs). Our results suggest that, in absence of PTMs, positively charged wildtype DP CT likely folds back onto negatively-charged plectin repeat 14 of nearby plakin repeat domain C (PRD C) contributing to the recruitment of intermediate filaments (IFs). When phosphorylated and methylated, negatively-charged wildtype DP CT would then fold back onto positively-charged plectin repeat 17 of PRD C, promoting the repulsion of intermediate filaments. However, by preventing PTMs, the R2834H mutation would lead to the formation of a cytoplasmic mutant desmoplakin with a constitutively positive DP CT tail that would be aberrantly recruited by cytoplasmic IFs instead of desmosomes, potentially weakening cell-cell contacts and promoting AC. Virtual screening of FDA-approved drug libraries identified several promising drug candidates for the treatment of cardiocutaneous diseases through drug repurposing.

Identifiants

pubmed: 39369039
doi: 10.1038/s41598-024-73705-0
pii: 10.1038/s41598-024-73705-0
doi:

Substances chimiques

Desmoplakins 0
DSP protein, human 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

23206

Informations de copyright

© 2024. The Author(s).

Références

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Auteurs

Cedric Badowski (C)

Institute of Medical Biology (IMB), Agency for Science, Technology and Research (A*STAR), Singapore, 138648, Singapore. cedricb2023@hotmail.com.

Paula Benny (P)

Institute of Medical Biology (IMB), Agency for Science, Technology and Research (A*STAR), Singapore, 138648, Singapore.
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, 1E Kent Ridge Rd, Level 12 NUHS Tower Block, Singapore, 119228, Singapore.
NUS Bia-Echo Asia Centre of Reproductive Longevity and Equality, Yong Loo Lin School of Medicine, National University of Singapore, Immunos Building, 8A Biomedical Grove, Singapore, Singapore.

Chandra S Verma (CS)

Bioinformatics Institute (BII), Agency for Science, Technology and Research (A*STAR), Singapore, 138671, Singapore.

E Birgitte Lane (EB)

Institute of Medical Biology (IMB), Agency for Science, Technology and Research (A*STAR), Singapore, 138648, Singapore. birgit.lane@sris.a-star.edu.sg.
Skin Research Institute of Singapore, Agency for Science, Technology and Research (A*STAR), Immunos Building, 8A Biomedical Grove, Singapore, 138648, Singapore. birgit.lane@sris.a-star.edu.sg.

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