Mastl inhibitor
WebMoreover, GKI-1, the first-in-class small molecule inhibitor of MASTL kinase, phenocopied MASTL depletion in enhancing the outcome of cisplatin treatment in OSCC cells, at a dose substantially lower than that needed to disrupt mitotic entry. Finally, GKI-1 exhibited promising efficacy in a mouse tumor xenograft model, in conjunction with ... WebJan 4, 2024 · To improve inhibitor potency, 10058-F4 and 10074-G5 were covalently linked to create a bitopic inhibitor, leading to a modest improvement in binding affinity . A later study also sought to optimize 10058-F4 potency through functional group modification, leading to improved inhibition of the growth of c-Myc-expressing cells .
Mastl inhibitor
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WebJul 1, 2024 · This study showed the new MASTL inhibitor, MKI 1 (MASTL Kinase Inhibitor 1), with antitumor activity and radiosensitizing effect in breast cancer in vitro and in vivo. … WebSep 28, 2024 · The MASTL-ENSA-PP2A/B55 axis modulates cisplatin resistance in oral squamous cell carcinoma Platinum-based chemotherapy is the standard first-line treatment for oral squamous cell carcinoma (OSCC) that is inoperable, recurrent, or metastatic. Platinum sensitivity is a major determinant of patient survival in advanced OSCC.
WebJul 5, 2024 · Our data showed that MKI-2 inhibited recombinant MASTL activity and cellular MASTL activity with IC50 values of 37.44 nM and 142.7 nM, respectively, in breast cancer cells. In addition, MKI-2... WebNational Center for Biotechnology Information
WebNational Center for Biotechnology Information WebOct 25, 2024 · Recent mechanistic reports have described MASTL (microtubule-associated serine/threonine kinase-like) as a promising target for anticancer treatment, but very …
WebAlthough MASTL is an attractive target for anticancer treatment, MASTL inhibitors with nM range potency and anticancer efficacy have not been reported. The present study newly …
WebSep 25, 2024 · On the other hand, treatment of Mastl(ED/ED) mice with Ampk, Pka, or Pkc inhibitors delayed embolism formation as well as embolism-induced death in the presence of the thrombocytopenia-associated mutation. Altogether, these data suggest that Mastl E166D–mutant platelets display an aberrant phosphorylation pattern that may contribute … michael tracey tazedWebMKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in … michael track comicWebFeb 29, 2016 · Development of specific MASTL inhibitors should assist the study of this pathway in the future. In addition to delaying checkpoint recovery, depletion of MASTL also triggered premature activation ... michael tracey taserWebNov 1, 2014 · The study thus calls for immediate research efforts in the characterization of kinase inhibitors that specifically target Mastl, and validation of these inhibitors for cancer therapy. Considering that Mastl upregulation in a substantial portion of cancer cells and tissues, the therapeutic strategy of targeting Mastl may yield broad potential in ... how to change wifi pldtWebJul 1, 2024 · Abstract. Although microtubule-associated serine threonine kinase like (MASTL) is an emerging target for selective anticancer treatment, a small-molecule inhibitor of MASTL with antitumor activity had not been reported yet. This study showed the new MASTL inhibitor, MKI 1 (MASTL Kinase Inhibitor 1), with antitumor activity and … michael trading cardsWebJul 5, 2024 · Although microtubule-associated serine/threonine kinase-like (MASTL) is a promising target for selective anticancer treatment, MASTL inhibitors with nano range … michael tracey young turksWebmki-1 是微管相关丝氨酸/苏氨酸样激酶 (mastl) 抑制剂 (ic50= 9.9 μm)。mki-1 通过激活乳腺癌中的pp2a 发挥放射增敏和抗肿瘤活性。 michael trachtman lawyer