[HTML][HTML] Following the design path of isoform-selective Hsp90 inhibitors: small differences, great opportunities

J Dernovšek, T Tomašič - Pharmacology & therapeutics, 2023 - Elsevier
The heat shock protein 90 (Hsp90) family consists of four highly conserved isoforms: the
mitochondrial TRAP-1, the endoplasmic reticulum-localised Grp94, and the cytoplasmic …

Glucocorticoid receptor and RAS: an unexpected couple in cancer

IC Cirstea, HP Moll, J Tuckermann - Trends in Cell Biology, 2023 - cell.com
Constitutively activated rat sarcoma (RAS) GTPases are one of the major drivers of tumor
growth and are difficult drug targets. The glucocorticoid receptor (GR), a nuclear receptor …

Metal-enriched HSP90 nanoinhibitor overcomes heat resistance in hyperthermic intraperitoneal chemotherapy used for peritoneal metastases

Q Wang, P Liu, Y Wen, K Li, B Bi, B Li, M Qiu, S Zhang… - Molecular cancer, 2023 - Springer
Clinical hyperthermic intraperitoneal chemotherapy (HIPEC) is regarded as a potential
treatment that can prolong survival of patients with peritoneal metastases after cytoreductive …

New class of Hsp90 C-terminal domain inhibitors with anti-tumor properties against triple-negative breast cancer

Z Zajec, J Dernovšek, J Cingl, I Ogris… - Journal of medicinal …, 2024 - ACS Publications
Triple-negative breast cancer (TNBC) remains a treatment challenge and requires
innovative therapies. Hsp90, crucial for the stability of numerous oncogenic proteins, has …

Co-targeting HSP90 alpha and CDK7 overcomes resistance against HSP90 inhibitors in BCR-ABL1+ leukemia cells

M Vogt, N Dienstbier, J Schliehe-Diecks… - Cell Death & …, 2023 - nature.com
HSP90 has emerged as an appealing anti-cancer target. However, HSP90 inhibitors
(HSP90i) are characterized by limited clinical utility, primarily due to the resistance …

A silicon-containing aryl/penta-1, 4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without …

YT Liao, XY Du, M Wang, CX Zheng, D Li… - RSC Medicinal …, 2023 - pubs.rsc.org
A pharmacophore-hybridized strategy based on previously reported HSP90 C-terminal
inhibitors was utilized to prepare 32 aryl/penta-1, 4-dien-3-one/amine hybrids. Among them …

Functionalized Nanomaterials for Inhibiting ATP-Dependent Heat Shock Proteins in Cancer Photothermal/Photodynamic Therapy and Combination Therapy

TP Premji, BS Dash, S Das, JP Chen - Nanomaterials, 2024 - mdpi.com
Phototherapies induced by photoactive nanomaterials have inspired and accentuated the
importance of nanomedicine in cancer therapy in recent years. During these light-activated …

Heat shock proteins as hallmarks of cancer: insights from molecular mechanisms to therapeutic strategies

WF Zuo, Q Pang, X Zhu, QQ Yang, Q Zhao… - Journal of Hematology & …, 2024 - Springer
Heat shock proteins are essential molecular chaperones that play crucial roles in stabilizing
protein structures, facilitating the repair or degradation of damaged proteins, and …

[HTML][HTML] Repression motif in HSF1 regulated by phosphorylation

S Gabriel, T Czerny, E Riegel - Cellular Signalling, 2023 - Elsevier
The heat shock factor 1 (HSF1) is a transcription factor that itself is a sensor for stress and
integrates various intrinsic or environmental stress sensing pathways. Thus HSF1 …

Small molecule inhibitors targeting heat shock protein 90: An updated review

Y Li, J Dong, JJ Qin - European Journal of Medicinal Chemistry, 2024 - Elsevier
As a molecular chaperone, heat shock protein 90 (HSP90) plays important roles in the
folding, stabilization, activation, and degradation of over 500 client proteins, and is …