Tag: Androgen Receptor

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...

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...

PF-06260414 is an Orally Active and Nonsteroidal Selective Androgen Receptor Modulator

The Androgen receptor (AR) is a nuclear receptor. The Androgen receptor is a DNA binding transcription factor that regulates gene expression. Specifically, androgen-regulated genes are essential for the development and maintenance of male sexual phenotypes. Besides, androgen causes slow maturation of bone, but the more effective maturation comes from...

EPI-001 is a Selective Inhibitor of Androgen Receptor with Anti-tumor Activity

The androgen receptor (AR) is a type of nuclear receptor and a modular steroid hormone receptor transcription factor. Specifically, the androgen receptor is activated by binding any of the androgenic hormones then translocating into the nucleus. Besides, the main function of the androgen receptor is to regulate gene expression...

Y06137 is a Selective BET Inhibitor for Treatment of CRPC

Prostate cancer arises as an androgen driven disease. Therefore the mainstay of systemic therapy for patients with advanced disease is androgen deprivation therapy. Despite of significant responses, nearly all patients ultimately progress and castration resistance ensues. Castration resistant prostate cancer therefore represents a stage in the continuum of the...

A Novel Potent and Specific BET Inhibitor Y06036 For Prostate Cancer

Prostate cancer is the most common malignancy and the fifth leading cause of death from malignancy in men. Since androgen receptor (AR) signaling has a pivotal role in prostate cancer, androgen deprivation therapy (ADT) with surgical or chemical castration is the standard treatment with most patients going to remission....