Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature 2019
DOI: 10.3410/f.735124444.793556910
|View full text |Cite
|
Sign up to set email alerts
|

Faculty Opinions recommendation of Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease.

Abstract: A series of imidazo [1,2-b]pyridazin-8-amine kinase inhibitors were discovered to allosterically inhibit the endoribonuclease function of the dual kinase-endoribonuclease inositol-requiring enzyme 1α (IRE1α), a key component of the unfolded protein response in mammalian cells and a potential drug target in multiple human diseases. Inhibitor optimization gave compounds with high kinome selectivity that prevented endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibited endori… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

0
0
0

Publication Types

Select...

Relationship

0
0

Authors

Journals

citations
Cited by 0 publications
references
References 30 publications
(46 reference statements)
0
0
0
Order By: Relevance

No citations

Set email alert for when this publication receives citations?