[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 …

Inhibitors and chemical probes for molecular chaperone networks

JE Gestwicki, H Shao - Journal of Biological Chemistry, 2019 - ASBMB
The molecular chaperones are central mediators of protein homeostasis. In that role, they
engage in widespread protein–protein interactions (PPIs) with each other and with their" …

Design, synthesis, antibacterial activity, and mechanisms of novel 1, 3, 4-thiadiazole derivatives containing an amide moiety

Z Wu, J Shi, J Chen, D Hu, B Song - Journal of Agricultural and …, 2021 - ACS Publications
To discover novel antibacterial agents, a series of novel 1, 3, 4-thiadiazole derivatives
containing an amide moiety were designed and synthesized, and their antibacterial activities …

Hsp90 activator Aha1 drives production of pathological tau aggregates

LB Shelton, JD Baker, D Zheng… - Proceedings of the …, 2017 - National Acad Sciences
The microtubule-associated protein tau (MAPT, tau) forms neurotoxic aggregates that
promote cognitive deficits in tauopathies, the most common of which is Alzheimer's disease …

C-terminal modulators of heat shock protein of 90 kDa (HSP90): State of development and modes of action

D Bickel, H Gohlke - Bioorganic & medicinal chemistry, 2019 - Elsevier
Cells constantly need to adopt to changing environmental conditions, maintaining
homeostasis and proteostasis. Heat shock proteins are a diverse class of molecular …

A progressively disassembled DNA repair inhibitors nanosystem for the treatment of BRCA wild-type triple-negative breast cancer

W Fang, J Wang, X Ma, N Shao, K Ye… - International Journal …, 2023 - Taylor & Francis
Background Olaparib, a poly (adenosine diphosphate-ribose) polymerase (PARP) inhibitor
has demonstrated promising efficacy in patients with triple-negative breast cancer (TNBC) …

Structure-Based Virtual Screening Identifies Novobiocin, Montelukast, and Cinnarizine as TRPV1 Modulators with Anticonvulsant Activity In Vivo

MA Llanos, N Enrique, ML Sbaraglini… - Journal of Chemical …, 2022 - ACS Publications
The transient receptor potential vanilloid 1 (TRPV1) receptor is a nonselective cation
channel, known to be involved in the regulation of many important physiological and …

Design, synthesis, and biological activities of vibsanin B derivatives: a new class of HSP90 C-terminal inhibitors

LD Shao, J Su, B Ye, JX Liu, ZL Zuo, Y Li… - Journal of Medicinal …, 2017 - ACS Publications
Previously, vibsanin B (ViB) was found to preferentially target HSP90β compared to
HSP90α. In this study, multiple experiments, including pull-down assays of biotin-ViB with …

Discovery of novel HSP90 inhibitors that induced apoptosis and impaired autophagic flux in A549 lung cancer cells

Q Wei, JY Ning, X Dai, YD Gao, L Su, BX Zhao… - European Journal of …, 2018 - Elsevier
Abstract Heat shock protein 90 (HSP90) inhibition has aroused increasing enthusiasm in
antitumor strategies in recent years. According to our previous studies, we synthesized a …

[HTML][HTML] The active components of Smilax china L. against cancer by interfering with the interactions among associated proteins

ST Wu, Y Zhao, XL Piao, L Qiu, Y Huang… - Journal of Functional …, 2023 - Elsevier
In tumors, Heat shock protein HSP 90-alpha (Hsp90α) maintains the activity of over-
activated or mutated signal transduction proteins and accelerates the malignant …