New opportunities for targeting the androgen receptor in prostate cancer

MM Centenera, LA Selth… - Cold Spring …, 2018 - perspectivesinmedicine.cshlp.org
Recent genomic analyses of metastatic prostate cancer have provided important insight into
adaptive changes in androgen receptor (AR) signaling that underpin resistance to androgen …

[HTML][HTML] Effects of ginsenoside Rb1 on oxidative stress injury in rat spinal cords by regulating the eNOS/Nrf2/HO‑1 signaling pathway

X Liu, X Gu, M Yu, Y Zi, H Yu… - Experimental and …, 2018 - spandidos-publications.com
The present study aimed to investigate whether ginsenoside Rb1 (G‑Rb1) attenuates spinal
cord injury‑associated oxidative stress in rats by regulating the endothelial nitric oxide …

Harnessing the heterogeneity of prostate cancer for target discovery using patient-derived explants

MM Centenera, AD Vincent, M Moldovan, HM Lin… - Cancers, 2022 - mdpi.com
Simple Summary There is a widespread push toward more biologically relevant pre-clinical
models of prostate cancer that can improve the discovery and translation of new drugs and …

Targeting the Hsp90 C-terminal domain to induce allosteric inhibition and selective client downregulation

KM Goode, DP Petrov, RE Vickman, SA Crist… - … et Biophysica Acta (BBA …, 2017 - Elsevier
Abstract Background Inhibition of Hsp90 is desirable due to potential downregulation of
oncogenic clients. Early generation inhibitors bind to the N-terminal domain (NTD) but C …

Synthesis and Biological Activity of 3-(Heteroaryl)quinolin-2(1H)-ones Bis-Heterocycles as Potential Inhibitors of the Protein Folding Machinery Hsp90

EL Larghi, A Bruneau, F Sauvage, M Alami… - Molecules, 2022 - mdpi.com
In the context of our SAR study concerning 6BrCaQ analogues as C-terminal Hsp90
inhibitors, we designed and synthesized a novel series of 3-(heteroaryl) quinolin-2 (1 H), of …

Identification of novel response and predictive biomarkers to Hsp90 inhibitors through proteomic profiling of patient-derived prostate tumor explants

EV Nguyen, MM Centenera, M Moldovan, R Das… - Molecular & Cellular …, 2018 - ASBMB
Inhibition of the heat shock protein 90 (Hsp90) chaperone is a promising therapeutic
strategy to target expression of the androgen receptor (AR) and other oncogenic drivers in …

Total synthesis of the reported structure of stresgenin B enabled by the diastereoselective cyanation of an oxocarbenium

WC Chan, K Koide - Organic letters, 2018 - ACS Publications
We report the first total synthesis of the reported structure of the heat shock protein
expression inhibitor stresgenin B. The synthesis features (1) diastereoselective cyanation of …

Structural basis of the key residue W320 responsible for Hsp90 conformational change

S Peng, RL Matts, J Deng - Journal of Biomolecular Structure and …, 2023 - Taylor & Francis
The 90-kDa heat shock protein (Hsp90) is a homodimeric molecular chaperone with ATPase
activity, which has become an intensely studied target for the development of drugs for the …

Native size exclusion chromatography-based mass spectrometry (SEC-MS) identifies novel components of the Heat Shock Protein 90-dependent proteome

RS Samant, S Batista, M Larance, B Ozer, CI Milton… - BioRxiv, 2022 - biorxiv.org
The molecular chaperone heat shock protein 90 (HSP90) works in concert with co-
chaperones to stabilize its client proteins, which include multiple drivers of oncogenesis and …

[PDF][PDF] Identification of novel response and predictive biomarkers to Hsp90 inhibitors through mass spectrometry-based proteomic profiling of patient-derived prostate …

EV Nguyen, MM Centenera, M Moldovan… - Mol Cell …, 2018 - researchgate.net
Inhibition of the heat shock protein 90 (Hsp90) chaperone is a promising therapeutic
strategy to target expression of the androgen receptor (AR) and other oncogenic drivers in …