Discovery and development of ASK1 inhibitors.

Drug Development Drug Discovery Humans MAP Kinase Kinase Kinase 5 / antagonists & inhibitors Molecular Structure Protein Kinase Inhibitors / chemical synthesis Small Molecule Libraries / chemical synthesis
Cell death Endoplasmatic reticulum stress Fibrosis Inflammation JNK MAP3K Oxidative stress p38

Journal

Progress in medicinal chemistry
ISSN: 0079-6468
Titre abrégé: Prog Med Chem
Pays: Netherlands
ID NLM: 0376452

Informations de publication

Date de publication:
2020
Historique:
entrez: 5 5 2020
pubmed: 5 5 2020
medline: 27 11 2020
Statut: ppublish

Résumé

Aberrant activation of mitogen-activated protein kinases (MAPKs) like c-Jun N-terminal kinase (JNK) and p38 is an event involved in the pathophysiology of numerous human diseases. The apoptosis signal-regulating kinase 1 (ASK1) is an upstream target that gets activated only under pathological conditions and as such is a promising target for therapeutic intervention. In the first part of this review the molecular mechanisms leading to ASK1 activation and regulation will be described as well as the evidences supporting a pathogenic role for ASK1 in human disease. In the second part, an update on drug discovery efforts towards the discovery and development of ASK1-targeting therapies will be provided.

Identifiants

DOI: 10.1016/bs.pmch.2020.02.001 PMID: 32362327
pubmed: 32362327
pii: S0079-6468(20)30001-1
doi: 10.1016/bs.pmch.2020.02.001
pii:
doi:

Substances chimiques

Protein Kinase Inhibitors 0
Small Molecule Libraries 0
MAP Kinase Kinase Kinase 5 EC 2.7.11.25
MAP3K5 protein, human EC 2.7.11.25

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

101-179

Informations de copyright

© 2020 Elsevier B.V. All rights reserved.

Auteurs

Reginald Brys (R)

Galapagos NV, Mechelen, Belgium.

Karl Gibson (K)

Sandexis Medicinal Chemistry Ltd, Innovation House Discovery ParkSandwich, Kent, United Kingdom.

Tanja Poljak (T)

Fidelta Ltd, Zagreb, Croatia.

Steven Van Der Plas (S)

Galapagos NV, Mechelen, Belgium.

David Amantini (D)

Galapagos SASU, Romainville, France. Electronic address: david.amantini@glpg.com.

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Classifications MeSH

questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Discovery and development of ASK1 inhibitors.
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Discovery and development of ASK1 inhibitors.
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery and development of ASK1 inhibitors.
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Protein-Serine-Threonine Kinases › MAP Kinase Kinase Kinases › MAP Kinase Kinase Kinase 5 › Discovery and development of ASK1 inhibitors.
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Discovery and development of ASK1 inhibitors.
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Discovery and development of ASK1 inhibitors.
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Bibliothèques de petites molécules › Discovery and development of ASK1 inhibitors.