Hsp90: from cellular to organismal proteostasis

M Somogyvári, S Khatatneh, C Sőti - Cells, 2022 - mdpi.com
Assuring a healthy proteome is indispensable for survival and organismal health. Proteome
disbalance and the loss of the proteostasis buffer are hallmarks of various diseases. The …

[HTML][HTML] Methods to validate Hsp90 inhibitor specificity, to identify off-target effects, and to rethink approaches for further clinical development

L Neckers, B Blagg, T Haystead, JB Trepel… - Cell Stress and …, 2018 - Elsevier
The molecular chaperone Hsp90 is one component of a highly complex and interactive
cellular proteostasis network (PN) that participates in protein folding, directs misfolded and …

Dynamically shaping chaperones. Allosteric modulators of HSP90 family as regulatory tools of cell metabolism in neoplastic progression

C Sanchez-Martin, SA Serapian, G Colombo… - Frontiers in …, 2020 - frontiersin.org
Molecular chaperones have recently emerged as fundamental regulators of salient
biological routines, including metabolic adaptations to environmental changes. Yet, many of …

Assay design and development strategies for finding Hsp90 inhibitors and their role in human diseases

M Banerjee, I Hatial, BM Keegan, BSJ Blagg - Pharmacology & therapeutics, 2021 - Elsevier
Abstract Heat shock protein 90 (Hsp90) is a molecular chaperone that facilitates the
maturation of its client proteins including protein kinases, transcription factors, and steroid …

Discovery of new molecular entities able to strongly interfere with Hsp90 C-terminal domain

S Terracciano, A Russo, MG Chini, MC Vaccaro… - Scientific reports, 2018 - nature.com
Abstract Heat shock protein 90 (Hsp90) is an ATP dependent molecular chaperone deeply
involved in the complex network of cellular signaling governing some key functions, such as …

Synthesis and Structure–Activity Relationships of Inhibitors That Target the C-Terminal MEEVD on Heat Shock Protein 90

MN Rahimi, LK Buckton, SS Zaiter, J Kho… - ACS Medicinal …, 2017 - ACS Publications
Herein, we describe the synthesis and structure–activity relationships of cyclic peptides
designed to target heat shock protein 90 (Hsp90). Generating 19 compounds and evaluating …

The role of heat shock proteins in cisplatin resistance

Z Krawczyk, A Gogler-Pigłowska… - Anti-Cancer Agents …, 2018 - ingentaconnect.com
Background: Cisplatin (CDDP), a small molecule platinum-based compound, is an effective
anticancer drug used against a wide range of human neoplasms. Long-term clinical use of …

[HTML][HTML] Targeting protein-protein interactions in drug discovery: Modulators approved or in clinical trials for cancer treatment

C Camps-Fajol, D Cavero, J Minguillón… - Pharmacological …, 2024 - Elsevier
Protein-protein interactions (PPIs) form complex cellular networks fundamental to many key
biological processes, including signal transduction, cell proliferation and DNA repair. In …

Discovery of 5-aryl-3-thiophen-2-yl-1H-pyrazoles as a new class of Hsp90 inhibitors in hepatocellular carcinoma

S Mohamady, MI Ismail, SM Mogheith, YM Attia… - Bioorganic …, 2020 - Elsevier
Although hepatocellular carcinoma (HCC)-related mortality has increased over the past
decades, treatment options are still very limited, underlining the need for developing new …

HSP90 inhibitor, NVP-AUY922, improves myelination in vitro and supports the maintenance of myelinated axons in neuropathic mice

VG Chittoor-Vinod, H Bazick, AG Todd… - ACS Chemical …, 2019 - ACS Publications
Hereditary demyelinating neuropathies linked to peripheral myelin protein 22 (PMP22)
involve the disruption of normal protein trafficking and are therefore relevant targets for …