Small-molecule inhibitors of linear ubiquitin chain assembly complex (LUBAC), HOIPINs, suppress NF-κB signaling.
A549 Cells
Anti-Inflammatory Agents
/ chemistry
Cytokines
/ antagonists & inhibitors
HEK293 Cells
Humans
Inflammation
/ drug therapy
NF-kappa B
/ antagonists & inhibitors
Signal Transduction
/ drug effects
Small Molecule Libraries
/ chemistry
Transcription Factors
/ antagonists & inhibitors
Ubiquitin
/ immunology
Ubiquitin-Protein Ligases
/ antagonists & inhibitors
Ubiquitination
/ drug effects
Cytokine
Enzyme inhibitor
Inflammation
NF-κB
Ubiquitin
Journal
Biochemical and biophysical research communications
ISSN: 1090-2104
Titre abrégé: Biochem Biophys Res Commun
Pays: United States
ID NLM: 0372516
Informations de publication
Date de publication:
12 02 2019
12 02 2019
Historique:
received:
12
12
2018
accepted:
26
12
2018
pubmed:
7
1
2019
medline:
5
11
2019
entrez:
7
1
2019
Statut:
ppublish
Résumé
Nuclear factor-κB (NF-κB) is a crucial transcription factor family involved in the regulation of immune and inflammatory responses and cell survival. The linear ubiquitin chain assembly complex (LUBAC), composed of the HOIL-1L, HOIP, and SHARPIN subunits, specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-κB pathway. We recently identified a chemical inhibitor of LUBAC, which we named HOIPIN-1 (HOIP inhibitor-1). To improve the potency of HOIPIN-1, we synthesized 7 derivatives (HOIPIN-2∼8), and analyzed their effects on LUBAC and NF-κB activation. Among them, HOIPIN-8 suppressed the linear ubiquitination activity by recombinant LUBAC at an IC
Identifiants
pubmed: 30611571
pii: S0006-291X(18)32846-8
doi: 10.1016/j.bbrc.2018.12.164
pii:
doi:
Substances chimiques
Anti-Inflammatory Agents
0
Cytokines
0
NF-kappa B
0
Small Molecule Libraries
0
Transcription Factors
0
Ubiquitin
0
RBCK1 protein, human
EC 2.3.2.27
RNF31 protein, human
EC 2.3.2.27
Ubiquitin-Protein Ligases
EC 2.3.2.27
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
700-706Informations de copyright
Copyright © 2018 Elsevier Inc. All rights reserved.