Rescue: UnFolding 5 (UnFolding Series)

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Planetary Unfolding

Wang, L. Ghosh, R.

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Harrington, P. ACS Med. Feldman, H. ACS Chem. Concha, N. Waller, D. A covalent cysteine-targeting kinase inhibitor of Ire1 permits allosteric control of endoribonuclease activity. ChemBioChem 17 , — Axten, J. This study reports the discovery of the first selective PERK inhibitor. Rojas-Rivera, D. Cell Death Differ. Smith, A. Halliday, M. Partial restoration of protein synthesis rates by the small molecule ISRIB prevents neurodegeneration without pancreatic toxicity. Cell Death Dis. Boyce, M.

Science , — This study reports the first successful screening to identify small molecules that improve ER proteostasis. Tsaytler, P. Selective inhibition of a regulatory subunit of protein phosphatase 1 restores proteostasis. Science , 91—94 Das, I. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. Carrara, M. Crespillo-Casado, A. Sidrauski, C.

Pharmacological brake-release of mRNA translation enhances cognitive memory.

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Sekine, Y. Stress responses.

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Mutations in a translation initiation factor identify the target of a memory-enhancing compound. Pharmacological dimerization and activation of the exchange factor eIF2B antagonizes the integrated stress response. Zyryanova, A. Tsai, J. Structure of the nucleotide exchange factor eIF2B reveals mechanism of memory-enhancing molecule.

Science , eaaq Rabouw, H. Small molecule ISRIB suppresses the integrated stress response within a defined window of activation. USA , — Hearn, B. Structure-activity studies of bis- O -arylglycolamides: inhibitors of the integrated stress response. ChemMedChem 11 , — Wong, Y. Brain , — Gallagher, C.

This study reports the identification of the first ATF6 inhibitors. Plate, L. Small molecule proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation. Paxman, R.

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Pharmacologic ATF6 activating compounds are metabolically activated to selectively modify endoplasmic reticulum proteins. Blackwood, E. Pharmacologic ATF6 activation confers global protection in widespread disease models by reprograming cellular proteostasis. Urra, H. Endoplasmic reticulum stress and the hallmarks of cancer.

Trends Cancer 2 , — Song, M.

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Kriss, C. Overexpression of TCL1 activates the endoplasmic reticulum stress response: a novel mechanism of leukemic progression in mice. Xie, H. Sheng, X. Atkins, C. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. Hamamura, K.

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Feng, Y. Cancer Discov. Falletta, P.

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Translation reprogramming is an evolutionarily conserved driver of phenotypic plasticity and therapeutic resistance in melanoma. Genes Dev. ER proteostasis control of neuronal physiology and synaptic function. Trends Neurosci. Way, S. Pharmaceutical integrated stress response enhancement protects oligodendrocytes and provides a potential multiple sclerosis therapeutic.

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Vieira, F. PLoS One 10 , e Guanabenz, which enhances the unfolded protein response, ameliorates mutant SOD1-induced amyotrophic lateral sclerosis. Jiang, H. Guanabenz delays the onset of disease symptoms, extends lifespan, improves motor performance and attenuates motor neuron loss in the SOD1 G93A mouse model of amyotrophic lateral sclerosis. Neuroscience , — Moreno, J. Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice. Ounallah-Saad, H. Genetic or pharmacological reduction of PERK enhances cortical-dependent taste learning.

Radford, H. PERK inhibition prevents tau-mediated neurodegeneration in a mouse model of frontotemporal dementia. Acta Neuropathol. Mercado, G. Grande, V. Larhammar, M. Dual leucine zipper kinase-dependent PERK activation contributes to neuronal degeneration following insult. Briggs, D. Johnson, E.

Rescue: UnFolding 5 (UnFolding Series) Rescue: UnFolding 5 (UnFolding Series)
Rescue: UnFolding 5 (UnFolding Series) Rescue: UnFolding 5 (UnFolding Series)
Rescue: UnFolding 5 (UnFolding Series) Rescue: UnFolding 5 (UnFolding Series)
Rescue: UnFolding 5 (UnFolding Series) Rescue: UnFolding 5 (UnFolding Series)
Rescue: UnFolding 5 (UnFolding Series) Rescue: UnFolding 5 (UnFolding Series)
Rescue: UnFolding 5 (UnFolding Series) Rescue: UnFolding 5 (UnFolding Series)
Rescue: UnFolding 5 (UnFolding Series) Rescue: UnFolding 5 (UnFolding Series)

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