Category: Prostate Cancer

LDN193189 is a Selective BMP Type I Receptor Inhibitor

Fibrodysplasia ossificans progressiva (FOP) is a congenital disorder of progressive. It is widespread postnatal ossification of soft tissues and is without known effective treatments. A recent study identified heterozygous mutations in ACVR1, the gene encoding the BMP type I receptor ALK2, in all affected members from seven families. BMP...

PF-06260414 is an Orally Active and Nonsteroidal Selective Androgen Receptor Modulator

The Androgen receptor (AR) is a nuclear receptor. The Androgen receptor is a DNA binding transcription factor that regulates gene expression. Specifically, androgen-regulated genes are essential for the development and maintenance of male sexual phenotypes. Besides, androgen causes slow maturation of bone, but the more effective maturation comes from...

DTHIB is a Direct and Selective Heat Shock Factor 1 (HSF1) Inhibitor

Heat shock factor 1 (HSF1) is a key regulator of the heat shock response. Especially, HSF1 plays an important role in various cancers. In this study, researchers described the identification of a direct HSF1 inhibitor, Direct Targeted HSF1 Inhibitor (DTHIB). DTHIB physically engages HSF1 and selectively stimulates the degradation...

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....