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   Articles with "ire1" as a keyword



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Human cDC1 display constitutive activation of the UPR Sensor IRE1.

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recommendations! Published in 2022 at "European journal of immunology"

DOI: 10.1002/eji.202149774

Abstract: The intracellular mechanisms safeguarding dendritic cell (DC) function are of biomedical interest in several immune-related diseases. Type 1 conventional DCs (cDC1s) are prominent targets of immunotherapy typified by constitutive activation of the unfolded protein response… read more here.

Keywords: biology; ire1; ire1 rnase; upr sensor ... See more keywords

Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes.

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recommendations! Published in 2017 at "Cell metabolism"

DOI: 10.1016/j.cmet.2017.03.018

Abstract: In cells experiencing unrelieved endoplasmic reticulum (ER) stress, the ER transmembrane kinase/endoribonuclease (RNase)-IRE1α-endonucleolytically degrades ER-localized mRNAs to promote apoptosis. Here we find that the ABL family of tyrosine kinases rheostatically enhances IRE1α's enzymatic activities, thereby… read more here.

Keywords: ire1 rnase; abl ire1; targeting abl; ire1 signaling ... See more keywords

Kinase Photoaffinity Labeling Reveals Low Selectivity Profile of the IRE1 Targeting Imidazopyrazine-Based KIRA6 Inhibitor.

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recommendations! Published in 2020 at "ACS chemical biology"

DOI: 10.1021/acschembio.0c00802

Abstract: Inositol-requiring enzyme 1α (IRE1α) is one of three endoplasmic reticulum stress sensors. Upon activation of its kinase domain, IRE1α splices the mRNA substrate XBP1, which activates the unfolded protein response. IRE1α has emerged as a… read more here.

Keywords: inhibitor; kinase; based kira6; kinase photoaffinity ... See more keywords

Discovery of a Compound That Inhibits IRE1α S-Nitrosylation and Preserves the Endoplasmic Reticulum Stress Response under Nitrosative Stress

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recommendations! Published in 2024 at "ACS Chemical Biology"

DOI: 10.1021/acschembio.4c00403

Abstract: Inositol-requiring enzyme 1α (IRE1α) is a sensor of endoplasmic reticulum (ER) stress and drives ER stress response pathways. Activated IRE1α exhibits RNase activity and cleaves mRNA encoding X-box binding protein 1, a transcription factor that… read more here.

Keywords: reticulum stress; stress; response; endoplasmic reticulum ... See more keywords

Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.

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recommendations! Published in 2020 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.0c00344

Abstract: Amino-quinazoline BRaf kinase inhibitor 2 was identified from a library screen as a modest inhibitor of the unfolded protein response (UPR) regulating potential anticancer target IRE1α. A combination of crystallographic and conformational considerations were used… read more here.

Keywords: amino; braf activity; braf; identification braf ... See more keywords

Design, Synthesis, and Cellular Efficacy of Inositol-Requiring Enzyme Type 1 (IRE1α) Inhibitors.

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recommendations! Published in 2025 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.5c00418

Abstract: A library of 66 small molecules targeting IRE1α were designed using a molecular docking approach and prepared by a two-step reaction sequence using diverse substrates. All compounds utilized a 1-amino-4-bromonaphthalene core that was modified via… read more here.

Keywords: ire1 inhibitors; ire1 inhibition; ire1; design synthesis ... See more keywords

PRKCSH contributes to tumorigenesis by selective boosting of IRE1 signaling pathway

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recommendations! Published in 2019 at "Nature Communications"

DOI: 10.1038/s41467-019-11019-w

Abstract: Unfolded protein response (UPR) is an adaptive mechanism that aims at restoring ER homeostasis under severe environmental stress. Malignant cells are resistant to environmental stress, which is largely due to an activated UPR. However, the… read more here.

Keywords: ire1; environmental stress; stress; prkcsh contributes ... See more keywords
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Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands

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recommendations! Published in 2020 at "Nature Communications"

DOI: 10.1038/s41467-020-19974-5

Abstract: Inositol-Requiring Enzyme 1 (IRE1) is an essential component of the Unfolded Protein Response. IRE1 spans the endoplasmic reticulum membrane, comprising a sensory lumenal domain, and tandem kinase and endoribonuclease (RNase) cytoplasmic domains. Excess unfolded proteins… read more here.

Keywords: kinase front; kinase; atp competitive; rnase ... See more keywords

Decoding non-canonical mRNA decay by the endoplasmic-reticulum stress sensor IRE1α

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recommendations! Published in 2021 at "Nature Communications"

DOI: 10.1038/s41467-021-27597-7

Abstract: Inositol requiring enzyme 1 (IRE1) mitigates endoplasmic-reticulum (ER) stress by orchestrating the unfolded-protein response (UPR). IRE1 spans the ER membrane, and signals through a cytosolic kinase-endoribonuclease module. The endoribonuclease generates the transcription factor XBP1s by… read more here.

Keywords: reticulum stress; ire1; decay; endoplasmic reticulum ... See more keywords

IRE1α governs cytoskeleton remodelling and cell migration through a direct interaction with filamin A

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recommendations! Published in 2018 at "Nature Cell Biology"

DOI: 10.1038/s41556-018-0141-0

Abstract: Maintenance of endoplasmic reticulum (ER) proteostasis is controlled by a signalling network known as the unfolded protein response (UPR). Here, we identified filamin A as a major binding partner of the ER stress transducer IRE1α.… read more here.

Keywords: cytoskeleton; cell migration; filamin; ire1 ... See more keywords

Different binding modalities of quercetin to inositol-requiring enzyme 1 of S. cerevisiae and human lead to opposite regulation

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recommendations! Published in 2024 at "Communications Chemistry"

DOI: 10.1038/s42004-023-01092-0

Abstract: The flavonoid Quercetin (Qe) was identified as an activator of Inositol-requiring enzyme 1 (IRE1) in S. cerevisiae ( sc Ire1p), but its impact on human IRE1 ( h IRE1) remains controversial due to the absence… read more here.

Keywords: inositol requiring; ire1; different binding; requiring enzyme ... See more keywords