A Phenyl-Pyrrolidine Derivative Reveals a Dual Inhibition Mechanism of Myocardial Mitochondrial Permeability Transition Pore, Which Is Limited by Its Myocardial Distribution.

Animals Biological Transport Cytosol / drug effects Heart / drug effects Male Mice Mice, Inbred C57BL Mitochondria, Heart / drug effects Mitochondrial Permeability Transition Pore / antagonists & inhibitors Myocardium / cytology Pyrrolidines / chemistry

Journal

The Journal of pharmacology and experimental therapeutics
ISSN: 1521-0103
Titre abrégé: J Pharmacol Exp Ther
Pays: United States
ID NLM: 0376362

Informations de publication

Date de publication:
03 2021
Historique:
received: 30 09 2020
accepted: 08 12 2020
pubmed: 12 12 2020
medline: 28 4 2021
entrez: 11 12 2020
Statut: ppublish

Résumé

Mitochondrial permeability transition pore (mPTP) opening is a key event in cell death during myocardial ischemia reperfusion. Inhibition of its modulator cyclophilin D (CypD) by cyclosporine A (CsA) reduces ischemia-reperfusion injury. The use of cyclosporine A in this indication is debated; however, targeting mPTP remains a major goal to achieve. We investigated the protective effects of a new original small-molecule cyclophilin inhibitor C31, which was specifically designed to target CypD. CypD peptidylprolyl

Identifiants

DOI: 10.1124/jpet.120.000359 PMID: 33303698
pubmed: 33303698
pii: jpet.120.000359
doi: 10.1124/jpet.120.000359
doi:

Substances chimiques

Mitochondrial Permeability Transition Pore 0
Pyrrolidines 0
pyrrolidine LJU5627FYV

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

348-357

Informations de copyright

Copyright © 2021 by The American Society for Pharmacology and Experimental Therapeutics.

Déclaration de conflit d'intérêts

Conflict of interests: Inserm Transfert is the owner of patent EP 09306294.1 covering the family of cyclophilin inhibitors, including the C31 compound, for which A.A.-B., J.-F.G. and J.-M.P. are inventors. All other authors declare no competing financial interests.

Auteurs

Mathieu Panel (M)

U955 - IMRB, Inserm, UPEC, Ecole Nationale Vétérinaire d'Alfort, Créteil, France (M.P., B.G., D.M.);Université Paris-Est, UMR S955, UPEC, Créteil, France (A.A.B., I.R., J.M.P.); INSERM U955, Team « Viruses, Hepatology, Cancer », Hôpital Henri Mondor, Créteil, France (A.A.B., J.M.P., I.R.); Centre de Biochimie Structurale (CBS), INSERM U1054, CNRS UMR5048, Université de Montpellier, Montpellier, France (J.F.G.); and Department of Virology, Hôpital Henri Mondor, Créteil, France (J.M.P.).

Abdelhakim Ahmed-Belkacem (A)

U955 - IMRB, Inserm, UPEC, Ecole Nationale Vétérinaire d'Alfort, Créteil, France (M.P., B.G., D.M.);Université Paris-Est, UMR S955, UPEC, Créteil, France (A.A.B., I.R., J.M.P.); INSERM U955, Team « Viruses, Hepatology, Cancer », Hôpital Henri Mondor, Créteil, France (A.A.B., J.M.P., I.R.); Centre de Biochimie Structurale (CBS), INSERM U1054, CNRS UMR5048, Université de Montpellier, Montpellier, France (J.F.G.); and Department of Virology, Hôpital Henri Mondor, Créteil, France (J.M.P.).

Isaac Ruiz (I)

U955 - IMRB, Inserm, UPEC, Ecole Nationale Vétérinaire d'Alfort, Créteil, France (M.P., B.G., D.M.);Université Paris-Est, UMR S955, UPEC, Créteil, France (A.A.B., I.R., J.M.P.); INSERM U955, Team « Viruses, Hepatology, Cancer », Hôpital Henri Mondor, Créteil, France (A.A.B., J.M.P., I.R.); Centre de Biochimie Structurale (CBS), INSERM U1054, CNRS UMR5048, Université de Montpellier, Montpellier, France (J.F.G.); and Department of Virology, Hôpital Henri Mondor, Créteil, France (J.M.P.).

Jean-François Guichou (JF)

U955 - IMRB, Inserm, UPEC, Ecole Nationale Vétérinaire d'Alfort, Créteil, France (M.P., B.G., D.M.);Université Paris-Est, UMR S955, UPEC, Créteil, France (A.A.B., I.R., J.M.P.); INSERM U955, Team « Viruses, Hepatology, Cancer », Hôpital Henri Mondor, Créteil, France (A.A.B., J.M.P., I.R.); Centre de Biochimie Structurale (CBS), INSERM U1054, CNRS UMR5048, Université de Montpellier, Montpellier, France (J.F.G.); and Department of Virology, Hôpital Henri Mondor, Créteil, France (J.M.P.).

Jean-Michel Pawlotsky (JM)

U955 - IMRB, Inserm, UPEC, Ecole Nationale Vétérinaire d'Alfort, Créteil, France (M.P., B.G., D.M.);Université Paris-Est, UMR S955, UPEC, Créteil, France (A.A.B., I.R., J.M.P.); INSERM U955, Team « Viruses, Hepatology, Cancer », Hôpital Henri Mondor, Créteil, France (A.A.B., J.M.P., I.R.); Centre de Biochimie Structurale (CBS), INSERM U1054, CNRS UMR5048, Université de Montpellier, Montpellier, France (J.F.G.); and Department of Virology, Hôpital Henri Mondor, Créteil, France (J.M.P.).

Bijan Ghaleh (B)

U955 - IMRB, Inserm, UPEC, Ecole Nationale Vétérinaire d'Alfort, Créteil, France (M.P., B.G., D.M.);Université Paris-Est, UMR S955, UPEC, Créteil, France (A.A.B., I.R., J.M.P.); INSERM U955, Team « Viruses, Hepatology, Cancer », Hôpital Henri Mondor, Créteil, France (A.A.B., J.M.P., I.R.); Centre de Biochimie Structurale (CBS), INSERM U1054, CNRS UMR5048, Université de Montpellier, Montpellier, France (J.F.G.); and Department of Virology, Hôpital Henri Mondor, Créteil, France (J.M.P.) didier.morin@inserm.fr.

Didier Morin (D)

U955 - IMRB, Inserm, UPEC, Ecole Nationale Vétérinaire d'Alfort, Créteil, France (M.P., B.G., D.M.);Université Paris-Est, UMR S955, UPEC, Créteil, France (A.A.B., I.R., J.M.P.); INSERM U955, Team « Viruses, Hepatology, Cancer », Hôpital Henri Mondor, Créteil, France (A.A.B., J.M.P., I.R.); Centre de Biochimie Structurale (CBS), INSERM U1054, CNRS UMR5048, Université de Montpellier, Montpellier, France (J.F.G.); and Department of Virology, Hôpital Henri Mondor, Créteil, France (J.M.P.) didier.morin@inserm.fr.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Métabolisme › Transport biologique › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Cytosol › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Système cardiovasculaire › Coeur › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée C57BL › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Mitochondries › Mitochondries du muscle › Mitochondries du myocarde › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines mitochondriales › Protéines de transport de la membrane mitochondriale › Pore de transition de perméabilité mitochondriale › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Tissus › Muscles › Muscle strié › Myocarde › A Phenyl-Pyrrolidine Derivative Reveals a Dual...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrrolidines › A Phenyl-Pyrrolidine Derivative Reveals a Dual...