Receptor tyrosine kinases are involved in regulation of key processes in endothelial biology, including proliferation, migration, and angiogenesis. It is now generally accepted that receptor tyrosine kinase signaling occurs intracellularly and on the plasma membrane, although many important details remain to be worked out. Endocytosis and subsequent intracellular trafficking spatiotemporally re...

In this paper, a set of 3-methylquniazolinone derivatives were designed, synthesised, and studied the preliminary structure-activity relationship for antiproliferative activities. All target compounds performed significantly inhibitory effects against wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) tumour cells (A431, A549, MCF-7, NCI-H1975). particular, compound 4d 3-flu...

Quercetin and daidzin are flavonoid glycoside type compounds that have been found in many plants nutraceuticals. This study aims to examine the vitro cytotoxic selectivity properties of quercetin on breast cervical cancers their molecular interaction stability epidermal growth factor receptor tyrosine kinase (EGFR-TK) by applying docking dynamics (MD) simulations. In anticancer activity was per...

Background: The transformation of epidermal growth factor receptor (EGFR)-mutant lung adenocarcinoma (LUAD) into small cell cancer (SCLC) accounts for 3–14% the resistance mechanism to EGFR tyrosine kinase inhibitors (TKIs). At present, there is no relevant research explore dynamic expression EGFR-mutant proteins and genomic evolution in transformed SCLC/neuroendocrine carcinoma (NEC).

The ability of dopamine D(4) and D(2) receptors to activate extracellular signal-regulated kinases (ERKs) 1 and 2 was compared using Chinese hamster ovary (CHO-K1) cells transfected with D(4.2), D(4.4), D(4.7), and D(2L) receptors. Dopamine stimulation of D(4) or D(2L) receptors produced a transient, dose-dependent increase in ERK1/2 activity. Receptor-specific activation of the ERK mitogen-act...

rho-kinase is an effector molecule of rhoa, a monomeric gtp-binding protein, and causes ca2+ sensitization through inactivation of myosin phosphatase. the major physiological functions of rho/rho-kinase cascade include contraction, proliferation and migration in cells.there are some excellent reviews about rho/rho-kinase signal pathway, most of which focus on the specific proteins of the pathwa...

Nociceptors, or pain-sensitive receptors, are unique among sensory receptors in that their sensitivity is increased by noxious stimulation. This process, called sensitization or hyperalgesia, is mediated by a variety of proinflammatory factors, including bradykinin, ATP and NGF, which cause sensitization to noxious heat stimuli by enhancing the membrane current carried by the heat- and capsaici...

This issue of Circulation Research includes 3 interesting studies that represent new concepts of AT1 receptor–mediated cell signaling in the cardiovascular system, which is currently of intense interest. The AT1 receptor mediates many important cardiovascular responses, including vasoconstriction, vascular and cardiac remodeling (cell proliferation, hypertrophy, and production of extracellular ...

The insulin-like growth factor-I (IGF-I) receptor is a member of a large family of transmembrane signal transducing molecules. The defining characteristic of this class of receptors is the intrinsic tyrosine kinase activity of the cytoplasmic domain. While it has been demonstrated that this tyrosine kinase activity is necessary for the action of a number of transmembrane tyrosine kinase recepto...