Focal adhesion kinase (FAK) is a widely expressed nonreceptor protein-tyrosine kinase implicated in integrin-mediated signal transduction pathways and in the process of oncogenic transformation by v-Src. Elevation of FAK's phosphotyrosine content, following both cell adhesion to extracellular matrix substrata and cell transformation by Rous sarcoma virus, correlates directly with an increased k...

Bcr-Abl tyrosine kinase inhibitors (TKI) are effective in inducing remissions in chronic myelogenous leukemia (CML) patients but do not eliminate primitive CML hematopoietic cells. There is a need to identify mechanisms that contribute to retention of CML progenitors. Src family tyrosine kinases have been identified as potential mediators of Bcr-Abl-induced leukemogenesis. Dasatinib (BMS-354825...

Angiotensin II (Ang II) induces hypertrophy of cardiac myocytes and hyperplasia of cardiac fibroblasts. To determine the molecular mechanism by which Ang II displayed different effects on cardiac myocytes and fibroblasts, we examined signal transduction pathways leading to activation of extracellular signal-regulated kinases (ERKs). Ang II-induced ERK activation was abolished by pretreatment wi...

The current model for regulation of the Src family kinase member Lck postulates a strict correlation between structural condensation of the kinase backbone and catalytic activity. The key regulatory tyrosine 505, when phosphorylated, interacts with the Src homology 2 domain on the same molecule, effectively suppressing tyrosine kinase activity. Dephosphorylation of Tyr(505) upon TCR engagement ...

The src family of nonreceptor protein tyrosine kinases share extensive sequence homology, except for 80 NH2-terminal amino acids, thought to comprise a "unique" domain. This region is presumed to mediate interactions specific to each kinase. Recently, we identified three NH2-terminal lysine residues, crucial for pp60v-src membrane association. Surprisingly, these lysines are conserved among sev...

IgE/antigen-dependent mast cell activation plays a central role in immediate hypersensitivity and other allergic reactions. The Src family tyrosine kinase (SFK) Lyn is activated by the cross-linking of high-affinity IgE receptors (FcepsilonRI). Activated Lyn phosphorylates the FcepsilonRI subunits, beta and gamma, leading to subsequent activation of various signaling pathways. Lyn also plays a ...

in this work, different ethyl 2,4-dioxo-4-arylbutanoate derivatives were prepared and evaluated for their src kinase inhibitory activity. for this purpose, the appropriate substituted acetophenone derivatives reacted with diethyl oxalate in the presence of sodium ethoxide in dried ethanol to give the corresponding products. all compounds showed moderate activities comparing with staurosporine a...

The skin produces a plethora of antimicrobial peptides that not only exhibit activities against invading pathogens but also display various functions, including the production cytokines/chemokines, and migration, proliferation differentiation host cells. Human β-defensins (hBDs) are most well characterized skin-derived peptides. We recently reported hBD-3 accelerated wound healing process promo...