MPS1

Enhancing reporting quality and impact of early phase dose-finding clinical trials: CONSORT Dose-finding Extension (CONSORT-DEFINE) guidance

37 views | Dec 18 2023

CONSORT-DEFINE provides international, consensus-driven guidelines for reporting early phase dose-finding trials, emphasizing essential items to enhance transparency, completeness, and reproducibility, thereby promoting clear interpretation and informed decision-making in medical research and practice. [Read the Full Post]

TTK Protein Kinase promotes temozolomide resistance through inducing autophagy in glioblastoma

40 views | Nov 26 2023

Inhibition of TTK Protein Kinase (TTK) using specific inhibitors, in combination with Temozolomide (TMZ) chemotherapy, overcomes TMZ resistance in glioblastoma multiforme (GBM) cells by suppressing autophagy, suggesting a promising therapeutic strategy for improving treatment outcomes in GBM patients. [Read the Full Post]

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

47 views | Nov 22 2023

BOS172722 is a potent spindle assembly checkpoint kinase MPS1 inhibitor that, in combination with paclitaxel, demonstrates significant synergistic effects, inducing chromosomal segregation defects and robust tumor regressions in preclinical models of triple-negative breast cancer, indicating its potential as a promising therapeutic approach for this patient population. [Read the Full Post]

Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity

44 views | Nov 22 2023

The study reveals that TTK inhibitors, particularly those inducing a shift in the glycine-rich loop by binding to the catalytic lysine at position 553, disrupt the catalytic machinery, leading to potent anti-proliferative effects, offering promising avenues for cancer treatment. [Read the Full Post]