PD901, a MEK inhibitor, has been demonstrated of therapeutic efficacy against cholangiocarcinoma (CCA) harboring K-Ras oncogenic mutations. However, most CCA exhibit no K-Ras mutations. In the current study, we investigated the therapeutic potential of PD901, either alone or in combination with th...
CA-074, cathepsin B inhibitor, was used as a negative control. Data were presented as the mean ± S.E.M. Two-way ANOVA followed by Dunnett’s post hoc analysis (F(4, 17) = 55.28, p < 0.0001). *p < 0.05; **p < 0.01; ***p < 0.001. Full size ...
Understanding the genetic underpinnings of PN led to the investigation of targeted thera- pies as medical treatment options, and the MEK1/2 inhibitor selumetinib has shown promising efficacy in pediatric patients with NF1 and symptomatic, inoperable PN. In a phase I/II trial, most children (...
PD-1 treatment as first-line adjuvant therapy. A multivariable logistic regression analysis was also used to estimate propensity scores for BRAF/MEK-inhibitor- and anti-PD-1-treated patients. Melanoma centers were grouped into northern, southern, or middle regions based on their geographical position...
Only recently, caffeine has been described as an inhibitor of PI3K activity with a clear preference for certain PI3K family members in vitro [40]. In combination with isoform-specific PI3K activity assays, this now allows one to look at specific PI3K proteins more closely. For many years it ...
The use of molecularly targeted therapy is becoming widespread in oncology. These agents cause tumour-specific genetic alterations in signal transduction pathways, hence less generalised toxicity. Dabrafenib, a BRAF inhibitor and Trametinib, a MEK inhibi
3.3. Decrease in EGF secretion and claudin-2 expression by MMP inhibitor II EGF was secreted from A549 cells and increased in a time-dependent manner (Fig. 3A). EGF ligands are synthesized as transmembrane precursors and are cleaved to their active form by metalloproteases [26], [27]. We ...
Non-treated HeLa cells, phosphatase inhibitor treated and λ phosphatase treated HeLa cells were subjected to SDS PAGE followed by western blot with 28935-1-AP (Phospho-MEK1 (Thr386) antibody) at dilution of 1:2000 incubated at room temperature for 1.5 hours.Enlarge Image¥...
These results agree with the previous observation that U0126, MEK inhibitor II, and PD98059 display affinity toward the inactive form of MEK-1 (used in the triple cas- cade assays) and not toward the MEK-1 active form (used in the direct MEK-1 and double cascade assays). All these ...
Chondrocytes were treated with TNFα with or without the MEK1/2 inhibitor U0126 for 24 hours. Microarray analysis and real-time PCR analyses were used to identify genes regulated by TNFα in a MEK1/2-dependent fashion. Promoter/reporter, immunoblot, and electrophoretic mobility shift assays were...