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To improve the preferential GalR binding we synthesized M wh
2022-07-06
To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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In fish little information about Gpr is
2022-07-05
In fish, little information about Gpr84 is available. We have revealed that lipopolysaccharide (LPS) induces significantly up-regulation of zebrafish , and zebrafish overexpression markedly increased the LPS-stimulated production of the cytokine []. Here we expanded on these studies to further inv
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K02288 br Introduction The fibroblast growth factor receptor
2022-07-05
Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, K02288 progression, metabolism, and survival. In non–small-cell lung cancer, the most fre
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Herein we report the discovery of AM
2022-07-05
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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More recently Vismodegib was administered
2022-07-04
More recently, Vismodegib was administered in combination with Gemcitabine in a pilot clinical trial that enrolled 23 patients affected by metastatic pancreatic adenocarcinoma. This type of malignancy is the most frequent form of pancreas cancer and is ranked in fourth place for cancer mortality in
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We have shown previously that
2022-07-04
We have shown previously that activation of the TGFβ/Smad signaling pathway in keratinocytes regulates 1,2-Dilauroyl-sn-glycerol cytoskeleton organization via non-genomic and genomic mechanisms and that RhoB gene is a target of Smad proteins [12,13]. Although the role of RhoB in early non-genomic T
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To the best of our knowledge this is
2022-07-04
To the best of our knowledge, this is the first study to examine functional GSTO1‐1 activity in the cornea. Therefore, comparative data for human or animals is not available. Moreover, we observed the nonspecific degradation of the GSTO1‐1 substrate 4NPG via an unknown mechanism, which was corrected
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br Introduction The third variable V loop of
2022-07-04
Introduction The third variable (V3) loop of the gp120 envelope glycoprotein (Env) on the surface of human immunodeficiency virus type 1 (HIV-1) becomes exposed after the virus binds CD4, the initial receptor; the V3 loop plays an important role in contacting the coreceptor CCR5 or CXCR4 to media
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br Discussion Our results indicate that marked changes
2022-07-04
Discussion Our results indicate that marked changes in the relative distribution of AMPA receptors in microsomal and synaptic fractions occur during the postnatal period, and that these changes are correlated with changes in different populations of AMPA binding sites. At early postnatal ages (PN
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Extensive pharmacological and structural analysis shows GCGR
2022-07-04
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in Ceftazidime 14, 17, 20. Functionally identical to REMD-477, REMD2.5
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br Acknowledgements This work was supported
2022-07-04
Acknowledgements This work was supported by a fellowship to C.H. under the ‘100 Foreign Expert’ scheme of the Shanxi province government(R100456). Conflict of interest: Dr. Holscher is a named inventor on a patent submitted by Lancaster University on the use of dual GLP-1/GIP analogues in neurode
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In the last years a plethora of studies overstepped the
2022-07-04
In the last years, a plethora of studies overstepped the classic concept of the ENS as purely modulator of GI secretion and motility, focusing on its potential as source of substances acting on immune cells and consequently involved in the control of local inflammatory events, as in the Inflammatory
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br Summary The presented results of the analysis
2022-07-04
Summary The presented results of the analysis of the unfolding of G-quadruplex and i-motif, which may appear within the telomeric DNA region, led to several important conclusions. Namely, determination of the work necessary to unfold of these structures, in biased molecular dynamics involving ste
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In Gallus gallus four FGFRs FGFR have been
2022-07-02
In Gallus gallus, four FGFRs (FGFR1-4) have been identified, along with 13 FGFs (FGF1–4, 8–10, 12, 13, 16, 18–20) (Thisse and Thisse, 2005). FGFRs are tyrosine kinase receptors that contain an extracellular ligand binding domain, a transmembrane domain and an intracellular tyrosine kinase domain. Th
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Although exhibited high inhibitory activity was found to be
2022-07-02
Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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