Category: Prostate Cancer

NEO2734 is an Orally Active Dual p300/CBP and BET Bromodomain Selective Inhibitor

NUT midline carcinoma (NMC) is a rare, aggressive subtype of squamous carcinoma. This kind of cancer is usually driven by BRD4-NUT fusion oncoprotein. BRD4, a BET protein, binds to chromatin through its two bromodomains. At the same time, NUT recruits the p300 HAT to activate oncogenic target genes transcription....

D-3263 is a TRPM8 Agonist with Potential Antineoplastic Activity

The transient receptor potential melastatin (TRPM) family is a part of the TRP protein superfamily. TRP protein superfamily contains TRPM1 to TRPM8 and involves various processes including temperature sensing, ion homeostasis, and redox sensing. Transient receptor potential melastatin (TRPM) ion channels play an important role in many physiological processes....

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...