JAK inhibitors in immune-mediated rheumatic diseases: From a molecular perspective to clinical studies.

Computational drug discovery Immune-mediated diseases Inflammatory diseases JAK Inhibitors drugs JAK-STAT Pathway JAK1 JAK2 Molecular docking Molecular dynamics Molecular mechanics Virtual screening

Journal

Journal of molecular graphics & modelling
ISSN: 1873-4243
Titre abrégé: J Mol Graph Model
Pays: United States
ID NLM: 9716237

Informations de publication

Date de publication:
05 2021
Historique:
received: 06 04 2020
revised: 21 09 2020
accepted: 20 10 2020
pubmed: 21 1 2021
medline: 22 6 2021
entrez: 20 1 2021
Statut: ppublish

Résumé

The Janus Kinase signalling pathway is implicated in the pathogenesis of immune-related diseases. The potency of small-molecule Janus Kinase inhibitors in the treatment of inflammatory diseases demonstrates that this pathway can be successfully targeted for therapeutic purposes. The outstanding relevant questions concerning drugs' efficacy and toxicity challenge the research to enhance the selectivity of these drugs. The promising results of computational techniques, such as Molecular Dynamics and Molecular Docking, coupled with experimental studies, can improve the understanding of the molecular mechanism of Janus Kinase pathway and thus enable the rational design of new more selective inhibitor molecules.

Identifiants

pubmed: 33472140
pii: S1093-3263(20)30578-7
doi: 10.1016/j.jmgm.2020.107789
pii:
doi:

Substances chimiques

Janus Kinase Inhibitors 0
Protein Kinase Inhibitors 0
Janus Kinases EC 2.7.10.2

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

107789

Informations de copyright

Copyright © 2020. Published by Elsevier Inc.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Michela Sperti (M)

PolitoBIOMedLab, Department of Mechanical and Aerospace Engineering, Politecnico di Torino, Italy.

Marta Malavolta (M)

PolitoBIOMedLab, Department of Mechanical and Aerospace Engineering, Politecnico di Torino, Italy.

Gloria Ciniero (G)

PolitoBIOMedLab, Department of Mechanical and Aerospace Engineering, Politecnico di Torino, Italy.

Simone Borrelli (S)

PolitoBIOMedLab, Department of Mechanical and Aerospace Engineering, Politecnico di Torino, Italy.

Marco Cavaglià (M)

PolitoBIOMedLab, Department of Mechanical and Aerospace Engineering, Politecnico di Torino, Italy.

Stefano Muscat (S)

Dalle Molle Institute for Artificial Intelligence (IDSIA), Manno, Switzerland.

Jack Adam Tuszynski (JA)

PolitoBIOMedLab, Department of Mechanical and Aerospace Engineering, Politecnico di Torino, Italy.

Antonella Afeltra (A)

Unit of Allergology, Immunology, Rheumatology, Department of Medicine, Università Campus Bio-Medico di Roma, Italy.

Domenico Paolo Emanuele Margiotta (DPE)

Unit of Allergology, Immunology, Rheumatology, Department of Medicine, Università Campus Bio-Medico di Roma, Italy.

Luca Navarini (L)

Unit of Allergology, Immunology, Rheumatology, Department of Medicine, Università Campus Bio-Medico di Roma, Italy. Electronic address: l.navarini@unicampus.it.

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Classifications MeSH