Articles with "grp94" as a keyword



Effects of purine-scaffold inhibitors on HUVECs: Involvement of the purinergic pathway and interference with ATP. Implications for preventing the adverse effects of extracellular Grp94

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Published in 2019 at "Biochemistry and Biophysics Reports"

DOI: 10.1016/j.bbrep.2019.100661

Abstract: Background Extracellular Glucose-regulated protein94 (Grp94) is linked to pathological conditions disrupting the obligatory intracellular location of this Heat Shock Protein (HSP). In plasma, Grp94 is linked to IgG in complexes that drive adverse effects on… read more here.

Keywords: grp94 igg; purine scaffold; scaffold inhibitors; grp94 ... See more keywords

Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.

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Published in 2018 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.8b00800

Abstract: As the endoplasmic reticulum paralogue of Hsp90, Grp94 chaperones a small set of client proteins associated with some diseases, including cancer, primary open-angle glaucoma, and inflammatory disorders. Grp94-selective inhibition has been a potential therapeutic strategy… read more here.

Keywords: grp94 selective; potent grp94; efficacy; mouse model ... See more keywords

Trifunctional High-Throughput Screen Identifies Promising Scaffold To Inhibit Grp94 and Treat Myocilin-Associated Glaucoma.

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Published in 2018 at "ACS chemical biology"

DOI: 10.1021/acschembio.7b01083

Abstract: Gain-of-function mutations within the olfactomedin (OLF) domain of myocilin result in its toxic intracellular accumulation and hasten the onset of open-angle glaucoma. The absence of myocilin does not cause disease; therefore, strategies aimed at eliminating… read more here.

Keywords: myocilin; associated glaucoma; biology; myocilin associated ... See more keywords

Conformationally Restricted Grp94-Selective Inhibitors

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Published in 2025 at "ACS Omega"

DOI: 10.1021/acsomega.4c06661

Abstract: Selective inhibition of glucose regulated protein 94 (Grp94), the most structurally unique isoform of heat shock protein 90 (Hsp90), has been implicated in the treatment of various disease states, including primary open-angle glaucoma and metastatic… read more here.

Keywords: restricted grp94; conformationally restricted; selective inhibitors; grp94 selective ... See more keywords

The endoplasmic reticulum chaperone BiP is a closure-accelerating cochaperone of Grp94

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Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"

DOI: 10.1073/pnas.2118793119

Abstract: Significance The endoplasmic reticulum (ER) is the site at which secreted proteins (such as the hormone insulin) and membrane-bound proteins are folded. ATP-dependent chaperones within the ER help proteins fold. This study describes how two… read more here.

Keywords: endoplasmic reticulum; closure; grp94; bip grp94 ... See more keywords

GRP94 promotes brain metastasis by engaging pro-survival autophagy.

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Published in 2019 at "Neuro-oncology"

DOI: 10.1093/neuonc/noz198

Abstract: BACKGROUND GRP94 is a glucose-regulated protein critical for survival in endoplasmic reticulum stress. Expression of GRP94 is associated with cellular transformation and increased tumorigenicity in breast cancer. Specifically, over-expression of GRP94 predicts brain metastasis in… read more here.

Keywords: pro survival; autophagy; brain metastasis; grp94 ... See more keywords

A Novel Small-Molecule GRP94 Modulator Increases PCSK9 Secretion and Promotes LDLR Degradation

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Published in 2025 at "Life"

DOI: 10.3390/life15081321

Abstract: The endoplasmic reticulum (ER) maintains protein homeostasis through chaperone-mediated folding and ER-associated degradation (ERAD). Disruption of this quality control, particularly involving the ER chaperone GRP94, contributes to diseases such as hypercholesterolemia, cancer, and immune disorders,… read more here.

Keywords: increases pcsk9; degradation; secretion promotes; pcsk9 secretion ... See more keywords