Pan-and isoform-specific inhibition of Hsp90: Design strategy and recent advances
J Yu, C Zhang, C Song - European Journal of Medicinal Chemistry, 2022 - Elsevier
In the past few decades, the development of heat shock protein 90 (Hsp90) inhibitors for
cancer treatment has not stopped. About twenty compounds have been evaluated in the …
cancer treatment has not stopped. About twenty compounds have been evaluated in the …
Recent advances toward the development of Hsp90 C-terminal inhibitors
Abstract Heat shock protein 90 (Hsp90) is a dynamic protein which serves to ensure proper
folding of nascent client proteins, regulate transcriptional responses to environmental stress …
folding of nascent client proteins, regulate transcriptional responses to environmental stress …
Magnoflorine attenuates inflammatory responses in RA by regulating the PI3K/Akt/NF-κB and Keap1-Nrf2/HO-1 signalling pathways in vivo and in vitro
Y Shen, X Fan, Y Qu, M Tang, Y Huang, Y Peng, Q Fu - Phytomedicine, 2022 - Elsevier
Background As a prolonged autoimmune disorder, rheumatoid arthritis (RA) is characterised
by synovial hyperplasia and the erosion of bone and cartilage. Magnoflorine (MAG) is the …
by synovial hyperplasia and the erosion of bone and cartilage. Magnoflorine (MAG) is the …
Development of a first-in-class small-molecule inhibitor of the C-terminal Hsp90 dimerization
Heat shock proteins 90 (Hsp90) are promising therapeutic targets due to their involvement in
stabilizing several aberrantly expressed oncoproteins. In cancerous cells, Hsp90 expression …
stabilizing several aberrantly expressed oncoproteins. In cancerous cells, Hsp90 expression …
Structure, function, and inhibitors of the mitochondrial chaperone TRAP1
S Kang, BH Kang - Journal of Medicinal Chemistry, 2022 - ACS Publications
Tumor necrosis factor receptor-associated protein 1 (TRAP1) is a mitochondrial molecular
chaperone modulating cellular metabolism and signaling pathways by altering the …
chaperone modulating cellular metabolism and signaling pathways by altering the …
Identification of Hsp90 inhibitors with anti-Plasmodium activity
D Posfai, AL Eubanks, AI Keim, KY Lu… - Antimicrobial agents …, 2018 - Am Soc Microbiol
Malaria remains a global health burden partly due to Plasmodium parasite resistance to first-
line therapeutics. The molecular chaperone heat shock protein 90 (Hsp90) has emerged as …
line therapeutics. The molecular chaperone heat shock protein 90 (Hsp90) has emerged as …
Structure-activity relationships of Benzothiazole-based Hsp90 C-Terminal-domain inhibitors
Heat shock protein 90 (Hsp90) is a chaperone responsible for the maturation of many
cancer-related proteins, and is therefore an important target for the design of new anticancer …
cancer-related proteins, and is therefore an important target for the design of new anticancer …
Modulation of human Hsp90α conformational dynamics by allosteric ligand interaction at the C-terminal domain
DL Penkler, Ö Tastan Bishop - Scientific Reports, 2019 - nature.com
Recent years have seen heat shock protein 90 kDa (Hsp90) attract significant interest as a
viable drug target, particularly for cancer. To date, designed inhibitors that target the ATPase …
viable drug target, particularly for cancer. To date, designed inhibitors that target the ATPase …
[HTML][HTML] Crystal structure of the middle and C-terminal domains of Hsp90α labeled with a coumarin derivative reveals a potential allosteric binding site as a drug target
The 90 kDa heat-shock protein (Hsp90) is an abundant molecular chaperone that is
essential to activate, stabilize and regulate the function of a plethora of client proteins. As …
essential to activate, stabilize and regulate the function of a plethora of client proteins. As …
[HTML][HTML] Dihydropyridines allosterically modulate Hsp90 providing a novel mechanism for heat shock protein co-induction and neuroprotection
Chaperones play a pivotal role in protein homeostasis, but with age their ability to clear
aggregated and damaged protein from cells declines. Tau pathology is a driver of a variety …
aggregated and damaged protein from cells declines. Tau pathology is a driver of a variety …