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Pharmacological targeting of endoplasmic reticulum stress in disease
The accumulation of misfolded proteins in the endoplasmic reticulum (ER) leads to ER
stress, resulting in activation of the unfolded protein response (UPR) that aims to restore …
stress, resulting in activation of the unfolded protein response (UPR) that aims to restore …
Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology
M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …
Structure and molecular mechanism of ER stress signaling by the unfolded protein response signal activator IRE1
CJ Adams, MC Kopp, N Larburu, PR Nowak… - Frontiers in molecular …, 2019 - frontiersin.org
The endoplasmic reticulum (ER) is an important site for protein folding and maturation in
eukaryotes. The cellular requirement to synthesize proteins within the ER is matched by its …
eukaryotes. The cellular requirement to synthesize proteins within the ER is matched by its …
[HTML][HTML] Endoplasmic reticulum stress signaling in cancer cells
SA Oakes - The American journal of pathology, 2020 - Elsevier
To survive, cancer cells must resist numerous internal and environmental insults associated
with neoplasia that jeopardize proteostasis within the endoplasmic reticulum (ER). Solid and …
with neoplasia that jeopardize proteostasis within the endoplasmic reticulum (ER). Solid and …
Endoplasmic reticulum stress signalling–from basic mechanisms to clinical applications
A Almanza, A Carlesso, C Chintha… - The FEBS …, 2019 - Wiley Online Library
The endoplasmic reticulum (ER) is a membranous intracellular organelle and the first
compartment of the secretory pathway. As such, the ER contributes to the production and …
compartment of the secretory pathway. As such, the ER contributes to the production and …
Tumorigenic and immunosuppressive effects of endoplasmic reticulum stress in cancer
JR Cubillos-Ruiz, SE Bettigole, LH Glimcher - Cell, 2017 - cell.com
Malignant cells utilize diverse strategies that enable them to thrive under adverse conditions
while simultaneously inhibiting the development of anti-tumor immune responses. Hostile …
while simultaneously inhibiting the development of anti-tumor immune responses. Hostile …
[HTML][HTML] Targeting DGAT1 ameliorates glioblastoma by increasing fat catabolism and oxidative stress
Glioblastoma (GBM), a mostly lethal brain tumor, acquires large amounts of free fatty acids
(FAs) to promote cell growth. But how the cancer avoids lipotoxicity is unknown. Here, we …
(FAs) to promote cell growth. But how the cancer avoids lipotoxicity is unknown. Here, we …
SEL1L–HRD1 endoplasmic reticulum-associated degradation controls STING-mediated innate immunity by limiting the size of the activable STING pool
Stimulator of interferon genes (STING) orchestrates the production of proinflammatory
cytokines in response to cytosolic double-stranded DNA; however, the pathophysiological …
cytokines in response to cytosolic double-stranded DNA; however, the pathophysiological …
Modulation of the proteostasis network promotes tumor resistance to oncogenic KRAS inhibitors
Despite substantial advances in targeting mutant KRAS, tumor resistance to KRAS inhibitors
(KRASi) remains a major barrier to progress. Here, we report proteostasis reprogramming as …
(KRASi) remains a major barrier to progress. Here, we report proteostasis reprogramming as …
IRE1α determines ferroptosis sensitivity through regulation of glutathione synthesis
Cellular sensitivity to ferroptosis is primarily regulated by mechanisms mediating lipid
hydroperoxide detoxification. We show that inositol-requiring enzyme 1 (IRE1α), an …
hydroperoxide detoxification. We show that inositol-requiring enzyme 1 (IRE1α), an …