scholarly journals KDM4B as a Target for Prostate Cancer: Structural Analysis and Selective Inhibition by a Novel Inhibitor

2014 ◽  
Vol 57 (14) ◽  
pp. 5975-5985 ◽  
Author(s):  
Chia-Han Chu ◽  
Ling-Yu Wang ◽  
Kai-Cheng Hsu ◽  
Chung-Chin Chen ◽  
Hsing-Hung Cheng ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Structural Analysis ◽  
Selective Inhibition

scholarly journals Selective degradation of AR-V7 to overcome castration resistance of prostate cancer

2021 ◽  
Vol 12 (10) ◽  
Author(s):  
Yuan Liu ◽  
Cuifu Yu ◽  
Zhenlong Shao ◽  
Xiaohong Xia ◽  
Tumei Hu ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Selective Inhibition ◽  
Castration Resistant Prostate Cancer ◽  
Castration Resistance ◽  
Selective Degradation ◽  
Castration Resistant ◽  
Novel Drugs ◽  
The Stability ◽  
Androgen Receptor Splice Variant

AbstractAndrogen receptor splice variant 7 (AR-V7), a form of ligand-independent and constitutively activating variant of androgen receptor (AR), is considered as the key driver to initiate castration-resistant prostate cancer (CRPC). Because AR-V7 lacks ligand-binding domain, the AR-targeted therapies that aim to inactivate AR signaling through disrupting the interaction between AR and androgen are limited in CRPC. Thus, the emergence of AR-V7 has become the greatest challenge for treating CRPC. Targeting protein degradation is a recently proposed novel avenue for cancer treatment. Our previous studies have been shown that the oncoprotein AR-V7 is a substrate of the proteasome. Identifying novel drugs that can trigger the degradation of AR-V7 is therefore critical to cure CRPC. Here we show that nobiletin, a polymethoxylated flavonoid derived from the peel of Citrus fruits, exerts a potent anticancer activity via inducing G0/G1 phase arrest and enhancing the sensitivity of cells to enzalutamide in AR-V7 positive PC cells. Mechanically, we unravel that nobiletin selectively induces proteasomal degradation of AR-V7 (but not AR). This effect relies on its selective inhibition of the interactions between AR-V7 and two deubiquitinases USP14 and USP22. These findings not only enrich our understanding on the mechanism of AR-V7 degradation, but also provide an efficient and druggable target for overcoming CRPC through interfering the stability of AR-V7 mediated by the interaction between AR-V7 and deubiquitinase.

Structural analysis of the C-CAM1 molecule for its tumor suppression function in human prostate cancer

The Prostate ◽  
1999 ◽  
Vol 41 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Jer-Tsong Hsieh ◽  
Karen Earley ◽  
Rey-Chen Pong ◽  
Yan Wang ◽  
Nguyen T. Van ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Structural Analysis ◽  
Tumor Suppression ◽  
Human Prostate ◽  
Human Prostate Cancer

scholarly journals Structural analysis of metalloform-selective inhibition of methionine aminopeptidase

2006 ◽  
Vol 62 (4) ◽  
pp. 425-432 ◽  
Author(s):  
Sheng-Xue Xie ◽  
Wei-Jun Huang ◽  
Ze-Qiang Ma ◽  
Min Huang ◽  
Robert P. Hanzlik ◽  
...  
Keyword(s):  
Structural Analysis ◽  
Selective Inhibition ◽  
Methionine Aminopeptidase

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Nature ◽  
2020 ◽  
Vol 578 (7794) ◽  
pp. 306-310 ◽  
Author(s):  
Emily J. Faivre ◽  
Keith F. McDaniel ◽  
Daniel H. Albert ◽  
Srinivasa R. Mantena ◽  
Joshua P. Plotnik ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Selective Inhibition

Oncogenicity and Selective Inhibition of ERG Splicing Variants in Prostate Cancer

2012 ◽  
Author(s):  
Luca Cartegni ◽  
George Boutsalis ◽  
Gina Rocco ◽  
Francesca Zammarchi
Keyword(s):  
Prostate Cancer ◽  
Selective Inhibition ◽  
Splicing Variants

scholarly journals Structural analysis of inhibition of E. coli methionine aminopeptidase: implication of loop adaptability in selective inhibition of bacterial enzymes

2007 ◽  
Vol 7 (1) ◽  
pp. 84 ◽  
Author(s):  
Ze-Qiang Ma ◽  
Sheng-Xue Xie ◽  
Qing-Qing Huang ◽  
Fa-Jun Nan ◽  
Thomas D Hurley ◽  
...  
Keyword(s):  
Structural Analysis ◽  
Selective Inhibition ◽  
Methionine Aminopeptidase ◽  
Bacterial Enzymes ◽  
E Coli
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