Category: Prostate Cancer

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...

SMAP-2 (DT-1154) is an Orally Bioavailable PP2A Activator

Protein Phosphatase 2A (PP2A) is a serine/threonine phosphatase. It regulates multiple signaling cascades implicated in cancer progression, including downstream effectors of KRAS. Inhibition of PP2A contributes to oncogenesis in multiple tumor types, highlighting the importance of this protein in maintaining normal kinase activity. Pancreatic ductal adenocarcinoma (PDA) cells have...

FTI-277 is a Farnesyl Transferase (FTase) Inhibitor

Farnesyl transferase (FTase) is a zinc-dependent enzyme. It adds a 15-carbon isoprenoid called a farnesyl group to proteins bearing a CaaX motif. FTase regulates the activation of oncogenic Ras protein and consequently affects intracellular signal transduction, and cell proliferation. Ras-induced malignant transformation requires Ras farnesylation, a lipid posttranslational modification...