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The lysine demethylase, KDM4B, is a key molecule in androgen receptor signalling and turnover
The androgen receptor (AR) is a key molecule involved in prostate cancer (PC) development and progression. Post-translational modification of the AR by co-regulator proteins can modulate itsExpand
Deubiquitinating Enzyme Usp12 Is a Novel Co-activator of the Androgen Receptor*
Background: Androgen receptor (AR) is the principle therapeutic target in prostate cancer. Result: We have established that Usp12 deubiquitinates and stabilizes the AR resulting in increasedExpand
KDM4B is a Master Regulator of the Estrogen Receptor Signalling Cascade
The importance of the estrogen receptor (ER) in breast cancer (BCa) development makes it a prominent target for therapy. Current treatments, however, have limited effectiveness, and hence theExpand
SETD6 controls the expression of estrogen-responsive genes and proliferation of breast carcinoma cells
The lysine methyltransferase SETD6 modifies the histone variant H2AZ, a key component of nuclear receptor-dependent transcription. Herein, we report the identification of several factors thatExpand
Development and exploitation of a novel mutant androgen receptor modelling strategy to identify new targets for advanced prostate cancer therapy
The persistence of androgen receptor (AR) signalling in castrate-resistant prostate cancer (CRPC) highlights the unmet clinical need for the development of more effective AR targeting therapies. AExpand
Determining direct binders of the Androgen Receptor using a high-throughput Cellular Thermal Shift Assay
Androgen Receptor (AR) is a key driver in prostate cancer. Direct targeting of AR has valuable therapeutic potential. However, the lack of disease relevant cellular methodologies capable ofExpand
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors
Many small molecule inhibitors of the cMET receptor tyrosine kinase have been evaluated in clinical trials for the treatment of cancer and resistance-conferring mutations of cMET are beginning to beExpand
Abstract 3848: Preclinical profile of AZD3514: A small molecule-targeting androgen receptor function with a novel mechanism of action and the potential to treat castration-resistant prostate cancer
The androgen receptor (AR), an important molecular target in the aetiology and progression of prostate cancer, has been found recently to drive key signalling responses in castration resistantExpand
Abstract B107: Characterization of a small molecule selective androgen receptor downregulator: A novel approach for the treatment of castration-resistant prostate cancer.
The androgen receptor (AR), an important molecular target in the aetiology and progression of prostate cancer, has been found recently to drive key signalling responses in castration resistantExpand
Nutlin-3 inhibits androgen receptor-driven c-FLIP expression, resulting in apoptosis of prostate cancer cells
Inhibition of androgen receptor (AR) signalling represents the conventional medical management of prostate cancer. Ultimately this treatment fails because tumors develop an incurable, castrateExpand