Tag: Low Toxicity

BCI-215 is a Tumor Cell-Selective DUSP-MKP Inhibitor

Mitogen-activated protein kinase phosphatases (MKPs) belongs to the dual-specificity phosphatase (DUSP) family. DUSP-MKPs dephosphorylate and inactivate the MAPKs extracellular signal-regulated kinase (ERK), JNK/SAPK, and p38 on tyrosine and threonine residues. As a result, they result in regulating the duration and amplitude of mitogenic and survival signaling. There exists a ...

CSRM617 is a Transcription Factor ONECUT2 Inhibitor for Prostate Cancer

The transcription factor ONECUT2 (OC2) is a master regulator of androgen receptor networks in mCRPC (metastatic castration-resistant prostate cancer ). OC2 acts as a survival factor in mCRPC models. OC2 is a potential drug target in the metastatic phase of aggressive PC. CSRM617,  a well-tolerated novel small-molecule inhibitor of...

RRx-001 Triggers Apoptosis and Overcomes Drug Resistance in Myeloma

The hypoxic bone-marrow (BM) microenvironment confers growth/survival and drug-resistance in myeloma. Novel therapies via targeting hypoxic-BM milieu may overcome drug resistance. A study from Deepika Sharma Das reported a hypoxia-selective epigenetic agent, RRx-001. In this study, RRx-001 decreases the viability of MM cell lines, as well as overcomes drug-resistance....

MS31 is a Highly Selective Spindlin 1 Inhibitor

SPIN1 (Spindlin 1) is a chromatin reader protein. It recognizes trimethylated histone H3 lysine 4 (H3K4me3) through the protein-protein interaction at the defined “aromatic cage” in Tudor domain II. The interaction between asymmetrically dimethylated histone H3 arginine 8 (H3R8me2a) and Tudor domain I further increases the affinity. On the...

ZT-12-037-01, a Specific STK19 Inhibitor, Inhibits NRAS-driven Melanomagenesis

Activating mutations in NRAS account for 20%-30% of melanoma. but, there are no effective anti-NRAS therapies. Originally, it reports that the serine/threonine-protein kinase 19 (STK19) phosphorylate a-casein at serine/threonine residues and histones at serine residues. However, the role of STK19 in cancer initiation and development is poorly appreciated. Importantly,...