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The discoidin domain receptors DDR
2019-09-05

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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Our data show a site specific interaction of
2019-09-05

Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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c-met Compound A and Compound B Fig were found in our
2019-09-05

Compound A and Compound B (Fig. 4) were found in our in vitro screening assays and have similar CRF1 receptor in vitro profiles (Table 1). When binding was investigated using [125I]-CRF in ex vivo assay, Compound A inhibited binding of [125I]-CRF both in the frontal cortex and the pituitary; however
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Recently we have observed that
2019-09-05

Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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In previous works Wang et al the PR CPA
2019-09-05

In previous works (Wang et al. [4,5]), the PR-CPA EoS has been applied to describe the solubilities of hydrocarbons (including methane, ethane, propane, n-butane, n-pentane, n-hexane, benzene, toluene, and ethyl-benzene) and mercaptans (including methyl mercaptan and ethyl mercaptan) in aqueous MDEA
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In our ongoing investigation of the structure activity relat
2019-09-05

In our ongoing investigation of the structure activity relationship of benzenesulfonamide anti-inflammatory activity, we designed and synthesized a novel set of benzenesulfonamide derivatives starting from commercially available sodium saccharin. The pivotal features of our approach aimed to do some
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br Acknowledgments br Casein kinases CK are serine threonine
2019-09-05

Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro
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Contrary to the downregulation of S PR family GPCRs CLL
2019-09-05

Contrary to the downregulation of S1PR family GPCRs, CLL cells have increased mRNA expression of the lysophosphatidic sto products (LPA) family receptors LPAR1, LPAR3 and LPAR4 compared to normal B cells [47]. Increased LPAR1 mRNA has been shown to be associated with more aggressive disease [47] an
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All known vertebrate TRIMs are
2019-09-05

All known vertebrate TRIMs are categorized in 11 distinct subclasses depending on the types of domains present at their carboxyl-terminals (Fig. 3) [29], [35]. Beyond conserved N-terminal domains, it is the C-terminal that provides specificity of interactions with other proteins. The subclass IV for
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Historically covalent drugs have had great
2019-09-05

Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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Concerning family A GPCRs although it has been described
2019-09-05

Concerning family A GPCRs, although it has been described that several receptors are able to operate as monomers (Arcemisbéhère et al., 2010; Bayburt et al., 2011; Chabre & le Maire, 2005; Ernst, Gramse, Kolbe, Hofmann, & Heck, 2007; Hanson et al., 2007; Kuszak et al., 2009; Whorton et al., 2007), e
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Carbonization and decarbonation are two different phases in
2019-09-05

Carbonization and decarbonation are two different phases in the decomposition of rice husk. Silica in RHA melts around 1440°C [5]. Burning of rice husk at temperature lower than 800°C produces reactive amorphous silica which contains approximately 90% silica, whereas above this temperature some crys
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A growing body of data indicates that endothelial
2019-09-05

A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream (±)-CPSI 1306 molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the concen
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We have previously shown that sustained
2019-09-04

We have previously shown that sustained 8-pCPT treatment favored Ca2+-dependent arrhythmogenic activity in rat ventricular cardiomyocytes [8]. Fig. 2 shows line-scan Ca2+ images of myocyte incubated without (Fig. 2A left) and with 8-pCPT (Fig. 2A right) subjected to a train of electrical stimulation
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br Chondroitin sulfate proteoglycans CSPGs are major
2019-09-04

Chondroitin sulfate proteoglycans (CSPGs) are major components of the extracellular matrix in cartilage. Each CSPG comprises a single core protein and attached chondroitin sulfate (CS), belonging to the glycosaminoglycan family of sugar chains. CSPGs and CS are involved in numerous biological and
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