A KEGG pathway analysis of the differentially expressed genes (DEGs) revealed that the cell cycle pathway was the most enriched pathway, among which TTK protein kinase (TTK) was the only gene with a clinical-grade inhibitor that has been investigated in a clinical trial but had not been ...
TTK inhibitordrug resistanceAPC/CCRISPR/Cas9breast cancerTTK protein kinase (TTK), also known as Monopolar spindle 1 (MPS1), is a key regulator of the spindle assembly checkpoint (SAC), which functions to maintain genomic integrity. TTK has emerged as a promising therapeutic target in human ...
Additionally, BOS172722, a potent TTK inhibitor, is currently being investigated in a Phase 1/1b study in combination with Paclitaxel in patients with advanced solid malignancies (https://clinicaltrials.gov/). Another small-molecule inhibitor, NMS-P715 has previously been shown to inhibit TTK ...
Pharmacological inhibition of TTK by a selective TTK inhibitor BAY-1217389 significantly triggered DNA damage and generate micronuclei formation in TNBC tumor cells. Leakage of dsDNA into cytosolic induced by BAY-1217389 activated cGAS-STING signaling and promoted the expression of type I IFN and ...
However, to date, there have been no clinical trials with TTK inhibitors involving patients with any kind of hematologic malignancies. In 2017, the TTK/MPS1 inhibitor OSU-13 was identified as a potential therapy for breast cancer.31 Here, we provide new data establishing the relevance of TTK ...
Graybug’s most advanced drug candidate, GB-102 is a microparticle formulation of a pan-VEGF inhibitor, sunitinib, for the treatment of wet age-related macular degeneration designed for a twice-per-year intravitreal injection. GB-102 has the potential to also benefit patients with diabetic ...
et al. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer research 70, 10255–10264, doi: 10.1158/0008-5472.CAN-10-2101 (2010). Article CAS PubMed Google Scholar Tanaka, T., Lobato, M. N. & Rabbitts, T. H. Single domain ...
While the first TTK inhibitors have entered clinical trials, little is known about how the inhibition of TTK with small molecule compounds affects cellular activity. We studied the selective TTK inhibitor NTRC 0066鈥 0, which was developed in our own laboratory, together with eleven TTK inhibitors...