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Patricia Dranchak Ryan MacArthur Rajarshi Guha William J. Zuercher David H. Drewry Douglas S. Auld James Inglese 《PloS one》2013,8(3)
A library of 367 protein kinase inhibitors, the GSK Published Kinase Inhibitor Set (PKIS), which has been annotated for protein kinase family activity and is available for public screening efforts, was assayed against the commonly used luciferase reporter enzymes from the firefly, Photinus pyralis (FLuc) and marine sea pansy, Renilla reniformis (RLuc). A total of 22 compounds (∼6% of the library) were found to inhibit FLuc with 10 compounds showing potencies ≤1 µM. Only two compounds were found to inhibit RLuc, and these showed relatively weak potency values (∼10 µM). An inhibitor series of the VEGFR2/TIE2 protein kinase family containing either an aryl oxazole or benzimidazole-urea core illustrate the different structure activity relationship profiles FLuc inhibitors can display for kinase inhibitor chemotypes. Several FLuc inhibitors were broadly active toward the tyrosine kinase and CDK families. These data should aid in interpreting the results derived from screens employing the GSK PKIS in cell-based assays using the FLuc reporter. The study also underscores the general need for strategies such as the use of orthogonal reporters to identify kinase or non-kinase mediated cellular responses. 相似文献
33.
KA Hyndman DH Evans 《Comparative biochemistry and physiology. Part A, Molecular & integrative physiology》2009,152(1):58-65
We recently determined that rapid changes in environmental salinity alter endothelin-1 (EDN1) mRNA levels in the euryhaline killifish, Fundulus heteroclitus, so we hypothesized that EDN1 may be a local regulator of gill ion transport in teleost fishes. The purpose of the present study was to examine the effects of changes in environmental salinity on the gill endothelin receptors: EDNRA, EDNRB, and EDNRC. Using quantitative real-time PCR, we determined that after a fresh water (FW) to seawater (SW) transfer, there is a two to threefold increase in gill EDNRA and EDNRB mRNA levels. Likewise, we found a two to three fold increase in gill EDNRA and EDNRB protein concentration. In addition, killifish that have acclimated to FW for 30 days had significantly lower EDNRA mRNA and protein levels than SW killifish. ENDRA were immunolocalized to the mitochondrion-rich cells of the killifish gill, suggesting that EDN1 signaling cascades may affect MRC function. EDNRB were found throughout the gill vasculature and on lamellar pillar cells. We previously immunolocalized EDN1 to the pillar cell suggesting that EDN1 acts as an autocrine signaling molecule and potentially regulates pillar cell tone and lamellar perfusion. We conclude that EDN1 is physiologically active in the teleost gill, and regulated by environmental salinity. Future functional studies examining the physiological role of this system are necessary to completely understand EDN1 in the fish gill. 相似文献
34.
Assembly of the sarcoplasmic reticulum proteins in differentiating rat skeletal muscle cell cultures: localization by immunofluorescence of sarcoplasmic reticulum proteins in differentiating rat skeletal muscle cell cultures 下载免费PDF全文
Immunofluorescent staining techniques were used to study the distribution of the Ca(2) + Mg(2+)-dependent ATPase and calsequestrin in primary cultures of differentiating rat skeletal muscle cells, grown for different periods of time under various culture conditions. In mononucleated myoblasts calsequestrin was detected after 45 h in culture whereas the ATPase was not detected until 60 h. After cell fusion began, both proteins could be identified in all multinucleated cells. Myoblasts grown for longer than 60 h in low Ca(2+) medium contained calsequestrin and the ATPase, even though they were unable to fuse. These studies at the cellular level confirm biochemical findings on the biosynthesis of calsequestrin and the ATPase. Immunofluorescent staining of myoblasts showed that calsequestrin first appears in a well-defined region of the cell near one end of the nucleus. At later times, the staining occupied progressively larger regions adjacent to the nucleus and took on a fibrous appearance. This suggests that calsequestrin first accumulates in the Golgi region and then gradually spreads throughout the cell. In contrast, the ATPase appeared to be concentrated in many small patches or foci throughout the cytoplasm and was never confined to one particular region, although some parts of the cell often stained more intensely than others. In multinucleated cells, alternating dark and fluorescent strands parallel to the longitudinal axis of the cells were evident. 相似文献
35.
Role of cryptic genes in microbial evolution 总被引:24,自引:1,他引:23
Cryptic genes are phenotypically silent DNA sequences, not normally
expressed during the life cycle of an individual. They may, however, be
activated in a few individuals of a large population by mutation,
recombination, insertion elements, or other genetic mechanisms. A
consideration of the microbial literature concerning biochemical evolution,
physiology, and taxonomy provides the basis for a hypothesis of microbial
adaptation and evolution by mutational activation of cryptic genes.
Evidence is presented, and a mathematical model is derived, indicating that
powerful and biologically important mechanisms exist to prevent the loss of
cryptic genes. We propose that cryptic genes persist as a vital element of
the genetic repertoire, ready for recall by mutational activation in future
generations. Cryptic genes provide a versatile endogenous genetic reservoir
that enhances the adaptive potential of a species by a mechanism that is
independent of genetic exchange.
相似文献
36.
Navas F Bishop MJ Garrison DT Hodson SJ Speake JD Bigham EC Drewry DH Saussy DL Liacos JH Irving PE Gobel MJ 《Bioorganic & medicinal chemistry letters》2002,12(4):575-579
A series of 2'-heteroaryl and 2'-oxime anilinomethylimidazolines was prepared and evaluated in in vitro functional assays for cloned human alpha1A, alpha1B, and alpha1D receptor subtypes. Potent and selective alpha1A agonists have been identified in these series. 相似文献
37.
Toxoplasma gondii (T. gondii) is a parasitic protist that can infect nearly all nucleated cell types and tissues of warm‐blooded vertebrate hosts. T. gondii utilises a unique form of gliding motility to cross cellular barriers, enter tissues, and penetrate host cells, thus enhancing spread within an infected host. However, T. gondii also disseminates by hijacking the migratory abilities of infected leukocytes. Traditionally, this process has been viewed as a route to cross biological barriers such as the blood–brain barrier. Here, we review recent findings that challenge this view by showing that infection of monocytes downregulates the program of transendothelial migration. Instead, infection by T. gondii enhances Rho‐dependent interstitial migration of monocytes and macrophages, which enhances dissemination within tissues. Collectively, the available evidence indicates that T. gondii parasites use multiple means to disseminate within the host, including enhanced motility in tissues and translocation across biological barriers. 相似文献
38.
Ethan DH Kim Ashish Sabharwal Adrian R Vetta Mathieu Blanchette 《Algorithms for molecular biology : AMB》2010,5(1):34
Background
Affinity purification followed by mass spectrometry identification (AP-MS) is an increasingly popular approach to observe protein-protein interactions (PPI) in vivo. One drawback of AP-MS, however, is that it is prone to detecting indirect interactions mixed with direct physical interactions. Therefore, the ability to distinguish direct interactions from indirect ones is of much interest. 相似文献39.
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SplitsTree: analyzing and visualizing evolutionary data 总被引:15,自引:0,他引:15
MOTIVATION: Real evolutionary data often contain a number of different and
sometimes conflicting phylogenetic signals, and thus do not always clearly
support a unique tree. To address this problem, Bandelt and Dress (Adv.
Math., 92, 47-05, 1992) developed the method of split decomposition. For
ideal data, this method gives rise to a tree, whereas less ideal data are
represented by a tree-like network that may indicate evidence for different
and conflicting phylogenies. RESULTS: SplitsTree is an interactive program,
for analyzing and visualizing evolutionary data, that implements this
approach. It also supports a number of distances transformations, the
computation of parsimony splits, spectral analysis and bootstrapping.
相似文献