Tag: AR

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...

UT-34 is an Orally Active pan-Androgen Receptor Degrader (SARD)

Prostate cancer drugs targeting the androgen receptor (AR) are mainly competitive ligand-binding domain (LBD) binding antagonists. A common mechanism of drug resistance can inactivate it. Specifically, AR is a nuclear receptor that is activated by binding to any androgen. In addition, radical prostatectomy combined with gonadotropin and androgen synthetase...

ARCC-4 is a Highly Potent PROTAC Androgen Receptor Degrader

Androgen receptor (AR) signaling is crucial for normal prostate development. It also drives the growth and survival of prostate cancer cells. AR signaling suppression is a common strategy for treating prostate cancer. Like other occupancy-based inhibitors, the antiandrogen enzalutamide requires high saturating drug concentrations to achieve its clinical benefit....

BI 167107 is a Highly Potent Agonist of the β2 Adrenergic Receptor

G protein-coupled receptors (GPCRs) exhibit a spectrum of functional behaviors in response to natural and synthetic ligands. Researchers generated the human β2 adrenergic receptor (β2AR) that exhibits G protein-like behavior. The active G protein-coupled state of the β2AR exhibits characteristic functional properties. Agonists promote Gs binding to the β2AR...

ORIC-101, a Potent Steroidal Glucocorticoid Receptor Antagonist for Cancer Research

The glucocorticoid receptor (GR) is a nuclear receptor, with the synonym of NR3C1. The receptor exhibits almost all cells of the body, regulates genes. And the latter ones control the development, metabolism, and immune response. In addition, cortisol and other glucocorticoids bind to the receptor, regulate gene transcription. Once...