Category: Prostate Cancer

AZA1 is a Potent Dual Inhibitor of Rac1 and Cdc42

Prostate cancer is the leading cause of cancer and the second leading cause of cancer-related deaths in men. Rho GTPases such as Rac, Cdc42, and RhoA are signaling proteins. They regulate cytoskeleton organization, cell cycle progression, cell survival, and migration directly contributing to tumor growth and progression. Cdc42 additionally...

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...

BAY1082439 is an Orally Active and Selective Balanced PI3Kα/β/δ Inhibitor

Prostate cancer is among the most common malignancy in males. Among the various PI3K isoforms, PTEN-loss-induced prostate cancer in the genetically engineered Pten conditional knockout mouse model predominantly activates the PI3Kβ subunit. However, selective inhibition of PI3Kβ shows no significant anti-tumor efficacy in PTEN-null prostate cancer cell lines. It...

TAK-683 is a Potent Metastin/GPR54 Agonist

Metastin/kisspeptin is a 54 amino acid peptide from human placental tissues. It is also the ligand of an orphan G protein-coupled receptor GPR54. GPR54, the KISS1 gene encodes the KISS1 receptor (KISS1R) and expresses in the rodent and human placenta and brain. In this article, we will introduce a...

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....

BAY1082439 is an Orally Active and Selective PI3Kα/β/δ Inhibitor

Prostate cancer is among the most common malignancy in males. It is also the second leading cause of male cancer-related death in the Western world.  The PI3K pathway is associated with adverse outcomes of prostate cancer. In the Pten conditional knockout mouse model, selective inhibition of PI3Kβ shows no...

ZCL278 is a Selective Cdc42 Inhibitor, with Antiviral Activity

Cdc42 is a member of the Rho GTPase family of low molecular weight G proteins. It is an important regulator of many biological processes. Besides, Cdc42 plays key roles in cytoskeletal organization, vesicular trafficking, cell cycle control, and transcription. As with most GTPases, transduction of signals occurs through the...