The capsaicin receptor TRPV1 is a nonselective cation channel that is expressed in sensory neurons. In this study, we examined the role of the nonreceptor cellular tyrosine kinase c-Src kinase in the modulation of the rat TRPV1. Capsaicin-induced currents in identified colonic dorsal root ganglion neurons were blocked by the c-Src kinase inhibitor PP2 and enhanced by the tyrosine phosphatase in...

BACKGROUND Tyrosine kinase inhibitors, such as imatinib, are not considered curative for chronic myeloid leukemia--regardless of the significant reduction of disease burden during treatment--since they do not affect the leukemic stem cells. However, the stochastic nature of hematopoiesis and recent clinical observations suggest that this view must be revisited. DESIGN AND METHODS We studied t...

In this study, we aimed to determine VEGFR-2, EGFR and PDGFR-β tyrosine kinase inhibitory activities of some pyrrolo[2,3-d]pyrimidine derivatives previously synthesized and showed potent cytotoxic and apoptotic effects against several cancer cell lines by our group and to evaluate the relationships between inhibitory activities and binding properties of the active compounds by molecular docking...

we have investigated the effect of theophylline on the kinetics of the catalytic subunit of protein kinase and related factors in lung tissue. the results show that the point of highest concentration of the c subunit of protein kinase which is active in casein phosphorylation is at 3h of incubation time, but in the presence of 100 ilg/ inl and 10µg/ml theophylline, this is shifted to i.s and 2....

The selection and expansion of tumor cells with de novo genetic alterations in specific genes has been described as a mechanism of resistance to targeted therapy. Unfortunately, in the metastatic setting it is often not possible to examine the multiple lesions present in an individual to determine the presence and mechanism of acquired resistance during therapy. Circulating tumor DNA (ctDNA) ca...

OBJECTIVE The effects of mitotane on the pharmacokinetics (PK) of co-administered drugs are mostly unknown. The aim of the present study was to describe the effects of mitotane on the PK of the phenotypic probe midazolam and of the tyrosine kinase inhibitor sunitinib. DESIGN A serendipitous observation was made in two of nine patients who volunteered in a sunitinib pharmacokinetic study. Both...

The completely N1-selective Pd-catalyzed arylation of unsymmetric imidazoles with aryl halides and triflates is described. This study showed that imidazoles have a strong inhibitory effect on the in situ formation of catalytically-active Pd(0)-ligand complex. The efficacy of the N-arylation reaction was improved drastically by the use of pre-activated solution of Pd2(dba)3 and L1. From these fi...

Rat 3Y1 cells acquire metastatic potential when transformed with v-src, and this potential is enhanced by double transformation with v-src and v-los (Taniguchi, S., T. Kawano, T. Mitsudomi, G. Kimura, and T. Baba. 1986. Jpn. J. Cancer Res. 77:11931197). We compared the activity of cadherin cell adhesion molecules of normal 3Y1 cells with that of v-src transformed (SR3Y1) and v-src and v-los dou...

Chronic lymphocytic leukemia (CLL) is the most prevalent leukemia in the adult population. Current efforts are focused on better understanding the intricate pathophysiology of the disease to develop successful targeted therapies. Ibrutinib is emerging as an important agent in this new age of targeted treatment for CLL. As a Bruton's tyrosine kinase inhibitor, it blocks the signaling pathway tha...

Background/Aim: Non-small cell lung cancer patients with epidermal growth factor receptor (EGFR) mutation have been shown to a good response erlotinib, tyrosine kinase inhibitor of EGFR. In this study, we found that the death pathways activated by erlotinib in 2D and 3D culture systems are different. Materials Methods: The induced were evaluated flow cytometry immunoblotting both EGFR mutant ce...