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
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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
The endoplasmic reticulum chaperone BiP is a closure-accelerating cochaperone of Grp94
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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