HSP90 inhibitors and cancer: Prospects for use in targeted therapies

ZN Li, Y Luo - Oncology reports, 2022 - spandidos-publications.com
Heat shock protein 90 (HSP90) is a vital chaperone protein, regulating signaling pathways
and correcting misfolded proteins in cancer cells by interacting with oncogenic client …

Old and new approaches to target the Hsp90 chaperone

J Sanchez, TR Carter, MS Cohen… - Current cancer drug …, 2020 - ingentaconnect.com
The 90-kDa heat shock protein (Hsp90) is a molecular chaperone that ensures cellular
proteostasis by maintaining the folding, stabilization, activation, and degradation of over 400 …

[HTML][HTML] Pimitespib in patients with advanced gastrointestinal stromal tumor (CHAPTER-GIST-301): a randomized, double-blind, placebo-controlled phase III trial

Y Kurokawa, Y Honma, A Sawaki, Y Naito, S Iwagami… - Annals of …, 2022 - Elsevier
Background Prognosis of advanced gastrointestinal stromal tumors (GIST) refractory to
tyrosine kinase inhibitors (TKIs) is poor. This randomized, placebo-controlled, phase III trial …

Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers

Z Xu, Y Zhuang, Q Chen - European Journal of Medicinal Chemistry, 2023 - Elsevier
Chemotherapeutics occupy a pivotal role in the medication of different types of cancers, but
the prevalence and mortality rates of cancer remain high. The drug resistance and low …

Pimitespib: first approval

SM Hoy - Drugs, 2022 - Springer
Pimitespib (Jeselhy®) is an oral small molecule inhibitor of the α and β isoforms of heat
shock protein 90 (HSP90). HSP90α and HSP90β regulate the stability and activity of a …

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 …

[HTML][HTML] Modulating the HSP90 control over NFκB/NLRP3/Caspase-1 axis is a new therapeutic target in the management of liver fibrosis: insights into the role of TAS …

EA Elmorsy, S Saber, RS Hamad, MA Abdel-Reheim… - Life Sciences, 2024 - Elsevier
Aberrant activation of the NLRP3 inflammasome is recognized to induce a chronic
inflammatory response in the liver, ultimately leading to hepatic fibrosis. HSP90 is suggested …

Early and next-generation KIT/PDGFRA kinase inhibitors and the future of treatment for advanced gastrointestinal stromal tumor

S Bauer, S George, M von Mehren… - Frontiers in …, 2021 - frontiersin.org
The majority of gastrointestinal stromal tumors (GIST) harbor an activating mutation in either
the KIT or PDGFRA receptor tyrosine kinases. Approval of imatinib, a KIT/PDGFRA tyrosine …

[HTML][HTML] Ganetespib (STA-9090) augments sorafenib efficacy via necroptosis induction in hepatocellular carcinoma: Implications from preclinical data for a novel …

S Saber, AM Hasan, OA Mohammed, LA Saleh… - Biomedicine & …, 2023 - Elsevier
Sorafenib, a multikinase inhibitor, is a first-line treatment for advanced hepatocellular
carcinoma, but its long-term effectiveness is limited by the emergence of resistance …

Combination of pimitespib (TAS‐116) with sunitinib is an effective therapy for imatinib‐resistant gastrointestinal stromal tumors

R Teranishi, T Takahashi, Y Obata… - … Journal of Cancer, 2023 - Wiley Online Library
Despite the effectiveness of imatinib, most gastrointestinal stromal tumors (GISTs) develop
resistance to the treatment, mainly due to the reactivation of KIT tyrosine kinase activity …