Category: Prostate Cancer

Senaparib is a Selective and Orally Active PARP1/2 Inhibitor

Poly(ADP-ribose) polymerase (PARP) is an important protein in DNA repair pathways especially the base excision repair. . PARP proteins compose of two ribose moieties and two phosphates per unit polymer. PARP inhibitors represent a successful example of precision medicine as the first drugs targeting DNA damage response to have...

NSC 80467 is a DNA Damaging Agent and a Selective Survivin Suppressant

Each of the ~1013 cells in the human body receives tens of thousands of DNA lesions per day. These lesions can block genome replication and transcription. If they are not repaired or are repaired incorrectly, they lead to mutations or wider-scale genome aberrations that threaten cell or organism viability....

VERU-111 is an Orally Bioavailable α and β Tubulin Inhibitor

Tubulins play a major role in cell dynamics, thus are important molecular targets for cancer therapy. VERU-111 preferentially represses clinically important, βIII and βIV tubulin isoforms via restoring the expression of miR-200c. VERU-111 (ABI-231) displays optimum activity and has an average IC50 value of 5.2 nM against a large...

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...