Category: Prostate Cancer

Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis

Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...

AZD4635 (HTL1071) is a Selective and Orally Active A2AR Antagonist

Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes (A1R, A2AR, A2BR, A3R) have been cloned and identified in different tissues. Adenosine receptors play an important role in sleep, the development of cancers and hearing...

ABBV-744 is a First-in-Class, Orally Active and Selective BET BDII Inhibitor

The proteins of BET (bromodomain and extra-terminal) domain family are epigenetic readers. BET domain family proteins bind acetylated histones through their bromodomains to regulate gene transcription. BET domain family proteins consist of BRD2, BRD3, BRD4 and BRDT. They contain BDI, BDII and the extra-terminal (ET) domain. Interestingly, BDII of...

Proxalutamide (GT0918) is a Potent Androgen Receptor (AR) Antagonist

Androgen receptors (ARs) mediate cell differentiation and development of prostate cancer. The target is a common therapeutic target in prostate cancer. Proxalutamide (GT0918) design is based on the core structure of MDV3100 but is optimized by computer-aided design. It is an innovative compound for prostate cancer and advanced breast...

Capivasertib (AZD5363) is an Orally Active pan-AKT Kinase Inhibitor

Akt/PKB (Protein kinase B), usually called Akt, is a serine/threonine protein kinase with antiapoptotic activity. In addition, Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis. Akt possesses a protein...

ARV-110 is an Orally Active, Specific Androgen Receptor (AR) PROTAC Degrader

Proteolysis targeting chimeras also names PROTAC protein degraders. PROTACs are emerging as an excellent class of small molecule therapies for cancer and other diseases. As we all know, conventional inhibitors or antagonists usually block the enzymatic or signaling activity of target proteins. PROTACs harness a system present within every...

NU9056 is a Selective Tip60 (KAT5) Histone Acetyltransferase Inhibitor

Histone acetylation and deacetylation are key events in the regulation of chromatin structure. Additionally, Histone acetyltransferases (HATs) can catalyze acetyl groups to the ε-amino terminus of lysine residues within histones. Acetylation results in an open chromatin structure by removing positive charges from histones. As a result, it induces protein...