Category: Prostate Cancer

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...

IPI-9119 is an Orally Active, Selective and Irreversible FASN Inhibitor

Fatty acid synthase (FASN) is a multi-enzyme protein that catalyzes the synthesis of fatty acids. Its main function is to catalyze the synthesis of palmitate (C16:0) from acetyl CoA and malonyl COA in the presence of NADPH. Specifically, FASN is a key enzyme responsible for the synthesis of fatty...

SR7826 is a Selective and Orally Active LIM kinase (LIMK) Inhibitor

LIM-kinase (Limk) is a serine-threonine protein kinase. Two isoforms are LIM kinase 1 (Limk1) and LIM kinase 2 (Limk2). Limk1 is overexpressed in cancerous prostate cells and tissues. Previous studies shows that the possibility of up-regulated Limk1 as a cellular oncogene and inhibition of Limk1 activity in cancerous prostate...

LQZ-7I is an Orally Active Survivin-Targeting Inhibitor

Survivin is a member of the inhibitor of apoptosis (IAP) protein family that inhibits caspases and blocks cell death. Caspases highly expressed in most cancers and are associate with a poor clinical outcome. The differential expression of survivin in cancer cells compared to normal tissues and its role as...

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...