Pharmacological targeting of IRE1 in cancer

DP Raymundo, D Doultsinos, X Guillory, A Carlesso… - Trends in cancer, 2020 - cell.com
IRE1α (inositol requiring enzyme 1 alpha) is one of the main transducers of the unfolded
protein response (UPR). IRE1α plays instrumental protumoral roles in several cancers, and …

Structural and molecular bases to IRE1 activity modulation

T Langlais, D Pelizzari-Raymundo… - Biochemical …, 2021 - portlandpress.com
The Unfolded Protein response is an adaptive pathway triggered upon alteration of
endoplasmic reticulum (ER) homeostasis. It is transduced by three major ER stress sensors …

Structure-Based Drug Design for Targeting IRE1: An in Silico Approach for Treatment of Cancer

A Poustforoosh, S Faramarz, MH Nematollahi… - Drug …, 2024 - thieme-connect.com
Background Endoplasmic Reticulum (ER) stress and Unfolded Protein Response (UPR)
play a key role in cancer progression. The aggregation of incorrectly folded proteins in the …

Deciphering the selectivity of inhibitor MKC9989 towards residue K907 in IRE1α; a multiscale in silico approach

SJ Mahdizadeh, A Carlesso, LA Eriksson - RSC advances, 2020 - pubs.rsc.org
The selectivity of the ligand MKC9989, as inhibitor of the Inositol-Requiring Enzyme 1α
(IRE1α) transmembrane kinase/ribonuclease protein, towards the residue K907 in the …

Modeling and exploring human IRE1 as a strategy to design novel inhibitors: a computational approach

A Carlesso - 2019 - gupea.ub.gu.se
Inositol Requiring Enzyme 1 (IRE1) is a bifunctional serine/threonine kinase and
endoribonuclease that is the major mediator of the Unfolded Protein Response (UPR) …