Search results for " TYR"
showing 10 items of 362 documents
Src proteins/src genes: from sponges to mammals
2004
The genome of marine sponge Suberites domuncula, a member of the most ancient and most simple metazoan phylum Porifera, encodes at least five genes for Src-type proteins, more than, i.e., Caenorhabditis elegans or Drosophila melanogaster (two in each). Three proteins, SRC1SD, SRC2SD and SRC3SD, were fully characterized. The overall homology (identity+similarity) among the three S. domuncula Srcs (68-71%) is much lower than the sequence conservation between orthologous Src proteins from freshwater sponges (82-85%). It is therefore very likely that several src genes/proteins were already present in the genome of Urmetazoa, the hypothetical metazoan ancestor. We have identified in the S. domun…
Immunoglobulin-like domain is present in the extracellular part of the receptor tyrosine kinase from the marine sponge Geodia cydonium.
1994
We have isolated and characterized two cDNAs from the marine sponge Geodia cydonium coding for a new member of a receptor tyrosine kinase of class II. The deduced amino acid sequence shows two characteristic domains: (i) the tyrosine kinase domain; and (ii) and immunoglobulin-like domain. The latter part shows high homology to the vertebrate C2 type immunoglobulin domain. This result demonstrates that immunoglobulin domains are not recent achievements of higher animals but exist also in those animals which have diverged from other organisms about 800 million years ago.
Thiocarbamate-Linked Polysulfonate–Peptide Conjugates As Selective Hepatocyte Growth Factor Receptor Binders
2014
The capacity of many proteins to interact with natural or synthetic polyanions has been exploited for modulating their biological action. However, the polydispersity of these macromolecular polyanions as well as their poor specificity is a severe limitation to their use as drugs. An emerging trend in this field is the synthesis of homogeneous and well-defined polyanion–peptide conjugates, which act as bivalent ligands, with the peptide part bringing the selectivity of the scaffold. Alternately, this strategy can be used for improving the binding of short peptides to polyanion-binding protein targets. This work describes the design and first synthesis of homogeneous polysulfonate–peptide con…
Activation of TRPC6 calcium channels by diacylglycerol (DAG)-containing arachidonic acid: A comparative study with DAG-containing docosahexaenoic acid
2006
We synthesized a diacylglycerol (DAG)-containing arachidonic acid, i.e., 1-stearoyl-2-arachidonyl-sn-glycerol (SAG), and studied its implication in the modulation of canonical transient receptor potential sub-type 6 (TRPC6) channels in stably-transfected HEK-293 cells. SAG induced the influx of Ca(2+), and also of other bivalent cations like Ba(2+) and Sr(2+), in these cells. SAG-evoked Ca(2+) influx was not due to its metabolites as inhibitors of DAG-lipase (RHC80267) and DAG-kinase (R50922) failed to inhibit the response of the same. To emphasise that SAG exerts its action via its DAG configuration, but not due to the presence of stearic acid at sn-1 position, we synthesized 1-palmitoyl-2…
Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells
2014
Background: In hepatocellular carcinoma (HCC), different signaling pathways are de-regulated, and among them, the expression of the epidermal growth factor receptor (EGFR). Tyrphostin AG-1478 is a lipophilic low molecular weight inhibitor of EGFR, preferentially acting on liver tumor cells. In order to overcome its poor drug solubility and thus improving its anticancer activity, it was entrapped into nanostructured lipid carriers (NLC) by using safe ingredients for parenteral delivery. Results: Nanostructured lipid carriers (NLC) carrying tyrphostin AG-1478 were prepared by using the nanoprecipitation method and different matrix compositions. The best system in terms of mean size, PDI, zeta…
Gefitinib in lung cancer therapy. Clinical results, predictive markers of response and future perspectives.
2009
Over the past few years, epidermal growth factor receptor has emerged as one of the most important targets in tumorgenesis and several drugs targeting signal transduction pathways have been developed. The first among these agents to be approved for the treatment of NSCLC was gefitinib, a potent, selective and reversible inhibitor of HER1/EGFR tyrosine kinase activity. The review summarizes its clinical development and the new therapeutic options, with particular focus on predictive markers of susceptibility to this drug.
Recycled Tyre Rubber Modified Bitumens for road asphalt mixtures: A literature review
2013
AbstractNowadays, only a small percentage of waste tyres are being land-filled. The Recycled Tyre Rubber is being used in new tyres, in tyre-derived fuel, in civil engineering applications and products, in moulded rubber products, in agricultural uses, recreational and sports applications and in rubber modified asphalt applications. The benefits of using rubber modified asphalts are being more widely experienced and recognized, and the incorporation of tyres into asphalt is likely to increase. The technology with much different evidence of success demonstrated by roads built in the last 40years is the rubberised asphalt mixture obtained through the so-called “wet process” which involves the…
TREATMENT AND DISPOSAL OF TYRES: TWO EU APPROACHES. A REVIEW
2015
The treatment and disposal of tyres from vehicles has long been of considerable environmental importance. The main problem lies in the mixed composition of the tyres. Studies have been undertaken to modify the structure of the tyres, especially with reference to the percentage of granulated rubber incorporated, in order to improve their performance, and also to reduce their environmental impact during normal functioning (noise, particulates, etc.) and facilitate recycling and final disposal. The aim of the present study is to review and compare how used tyres are treated and disposed of in two different EU countries. The first is Italy, which has been part of the European Union since its in…
Trawling disturbance effects on the trophic ecology of two co-generic Astropectinid species
2015
Physical disturbance by trawling can have both negative and positive effects on populations of scavenging benthic organisms. In the present study the impact of fishing activity on feeding behaviour of the two Astropectinids, Astropecten bispinosus and A. irregularis , was assessed based on stomach contents analysis. The study was carried out along trawled seabed highlighting the positive response of the two facultative scavengers to carrion generated by trawl disturbance. Furthermore, there was greater food specialization in areas that were more heavily exploited by trawling. This specialisation could be linked to the availability of certain prey that results from the passage of fishing gea…
Exosomes released by k562 chronic myeloid leukemia cells promote endothelial cell tubular differentiation through uptake and cell-to-cell transfer
2012
Exosomes, microvesicles of endocytic origin released by normal and tumor cells, play an important role in cell-to-cell ommunication. Angiogenesis has been shown to regulate progression of chronic myeloid leukemia (CML). The mechanism through which this happens has not been elucidated. We isolated and characterized exosomes from K562 CML cells and evaluated their effects on human umbilical endothelial cells (HUVECs). Fluorescent-labeled exosomes were nternalized by HUVECs during tubular differentiation on Matrigel. Exosome localization was perinuclear early in differentiation, moving peripherally in cells undergoing elongation and connection. Exosomes move within and between nanotubular stru…