Glucose regulated protein 94 (Grp94) is the endoplasmic reticulum resident of the heat shock protein 90 kDa (Hsp90) family of molecular chaperones. Grp94 associates with many proteins involved in cell adhesion and signaling, including integrins, Toll-like receptors, immunoglobulins, and mutant myocilin.
JAm Chem Soc 137(13):4358–4367 Lee SC, Min HY, Choi H et al (2015b) Synthesis ... anticancer agents targeting Hsp90. Eur J Med Chem 119:17–33 Oh SH, Woo JK, ...
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 for these diseases.
The European Journal of Medicinal Chemistry is a global journal that publishes studies on the main aspects of medicinal chemistry. It provides a medium for publication of original research papers and also welcomes critical review papers. A typical paper would report on the design (with or without ….
Dec 06, 2021 · Glucose-regulated protein 94 (Grp94), localized in the endoplasmic reticulum (ER), is a member of the heat shock protein 90 (HSP90) molecular chaperone family (12). Grp94 is a canonical hallmark of ER stress whose expression is induced by unfolded protein response (13).
Design and synthesis of Grp94 selective inhibitors based on Phe199 induced fit mechanism and their anti-inflammatory effects. ... [Eur. J. Med. Chem. 134(2017) 133 ...
The European Journal of Medicinal Chemistry is a global journal that publishes studies on the main aspects of medicinal chemistry. It provides a medium for publication of original research papers and also welcomes critical review papers.
Glucose-regulated protein 94 (Grp94), a member of the Heat shock protein 90 (Hsp90) family, is implicated in many human diseases, including cancer, neurodegeneration, inflammatory, and infectious diseases. Here, we describe our effort to design and develop a new series of Grp94 inhibitors based on P …
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 for these diseases.
The European Journal of Medicinal Chemistry is a global journal that publishes studies on the main aspects of medicinal chemistry. It provides a medium for publication of original research papers and also welcomes critical review papers. A typical paper would report on …
05.11.2021 · Glucose-regulated protein 94 (Grp94), a member of the Heat shock protein 90 (Hsp90) family, is implicated in many human diseases, including cancer, neurodegeneration, inflammatory, and infectious diseases. Here, we describe our effort to design and develop a new series of Grp94 inhibitors based on Phe199 induced fit mechanism.
MedChem in the USA ... Chemistry‐A European Journal, Medicinal Research Reviews, ... were pursued to develop more potent and selective Grp94 inhibitors.
Nov 05, 2021 · Glucose-regulated protein 94 (Grp94), a member of the Heat shock protein 90 (Hsp90) family, is implicated in many human diseases, including cancer, neurodegeneration, inflammatory, and infectious diseases. Here, we describe our effort to design and develop a new series of Grp94 inhibitors based on Phe199 induced fit mechanism.
Stefan Ochiana received his PhD in organic chemistry in 2013 from ... series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94. J Med Chem.