Design, Synthesis and Biological Evaluation of Arylpyridin-2-yl Guanidine Derivatives and Cyclic Mimetics as Novel MSK1 Inhibitors. An Application in an Asthma Model.


Journal

Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009

Informations de publication

Date de publication:
13 Jan 2021
Historique:
received: 03 12 2020
revised: 08 01 2021
accepted: 11 01 2021
entrez: 16 1 2021
pubmed: 17 1 2021
medline: 8 9 2021
Statut: epublish

Résumé

Mitogen- and Stress-Activated Kinase 1 (MSK1) is a nuclear kinase, taking part in the activation pathway of the pro-inflammatory transcription factor NF-kB and is demonstrating a therapeutic target potential in inflammatory diseases such as asthma, psoriasis and atherosclerosis. To date, few MSK1 inhibitors were reported. In order to identify new MSK1 inhibitors, a screening of a library of low molecular weight compounds was performed, and the results highlighted the 6-phenylpyridin-2-yl guanidine (compound

Identifiants

pubmed: 33450992
pii: molecules26020391
doi: 10.3390/molecules26020391
pmc: PMC7828447
pii:
doi:

Substances chimiques

Guanidines 0
Protein Kinase Inhibitors 0
Ribosomal Protein S6 Kinases, 90-kDa EC 2.7.11.1
mitogen and stress-activated protein kinase 1 EC 2.7.11.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : Association Vaincre la Mucoviscidose
ID : PRTP13/10 2010, RF20140501176, RF2016051629, RF2016052094
Organisme : Laboratory of Excellence Medalis, Initiative of Excellence (IdEx), Strasbourg University, France
ID : NA

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Auteurs

Maud Bollenbach (M)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

Simona Nemska (S)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

Patrick Wagner (P)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

Guillaume Camelin (G)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.

François Daubeuf (F)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.
CNRS, Université de Strasbourg, PCBIS Plate-forme de Chimie Biologique Intégrative de Strasbourg UMS 3286, F-67412 Illkirch, France.

Adeline Obrecht (A)

Institut du Médicament (IMS), F-67000 Strasbourg, France.
CNRS, Université de Strasbourg, PCBIS Plate-forme de Chimie Biologique Intégrative de Strasbourg UMS 3286, F-67412 Illkirch, France.

Pascal Villa (P)

Institut du Médicament (IMS), F-67000 Strasbourg, France.
CNRS, Université de Strasbourg, PCBIS Plate-forme de Chimie Biologique Intégrative de Strasbourg UMS 3286, F-67412 Illkirch, France.

Didier Rognan (D)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

Frédéric Bihel (F)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

Jean-Jacques Bourguignon (JJ)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

Martine Schmitt (M)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

Nelly Frossard (N)

Laboratoire d'Innovation Thérapeutique UMR 7200, CNRS, Faculté de Pharmacie, Université de Strasbourg, F-67400 Illkirch, France.
Institut du Médicament (IMS), F-67000 Strasbourg, France.

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Classifications MeSH