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To develop antagonists selective for the mouse
2020-09-05

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic VEGFR Tyrosine Kinase Inhibitor II () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced t
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br Experimental procedures br Acknowledgments br Introductio
2020-09-05

Experimental procedures Acknowledgments Introduction Receptor tyrosine kinases (RTKs) control many fundamental cellular processes, such as cell proliferation, differentiation, migration, and metabolism (Lemmon and Schlessinger, 2010). RTK activity is normally tightly controlled, and dysregu
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Collectively the results presented here provide new insights
2020-09-05

Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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br Results br Discussion Oxysterols and EBI
2020-09-05

Results Discussion Oxysterols and EBI2 have received growing attention in the field of immunology, with works highlighting an important role for EBI2 in immune cell migration. However, these studies are mainly limited to animal models (Chalmin et al., 2015, Hannedouche et al., 2011, Kelly et a
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br Materials and methods br Results Artemis has
2020-09-05

Materials and methods Results Artemis has been reported to possess 5′–3′ exonuclease activity in vitro on ssDNA, as well as DNA-PK-dependent endonuclease activity on single-strand overhang and hairpin DNA structures [11]. However, enzymes within the metallo-β-lactamase family typically contain
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The identification of a gatekeeper mutation also
2020-09-05

The identification of a gatekeeper Midostaurin also suggests that alternative DDR2 inhibitors may be required to overcome acquired resistance. Additional DDR2 inhibitors that have been isolated include the recently identified alkaloid natural products discoipyrroles A-D and the chemotherapeutic Acti
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labetalol hydrochloride The identification of CRF receptor
2020-09-05

The identification of CRF labetalol hydrochloride subtypes has led to a number of studies addressing its functional properties. This paper examines the evidence for CRF1 and CRF2 mediation of fear and anxiety. Recent reviews discussing specific CRF receptor functions associated with other conditions
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It is important to note that CRF
2020-09-05

It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a
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According to this theory the chemical potential
2020-09-05

According to this theory, the chemical potential of the basic hydrate in the equilibrium condition can be calculated as: , and denote the chemical potentials of the basic hydrate, water and gas, respectively. Also, is the number of gas molecules per water molecules in the basic hydrate. After su
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br Allosteric inhibitors In general candidate drugs that bin
2020-09-04

Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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In some of our studies we examined the occurrence of
2020-09-04

In some of our studies we examined the occurrence of ERβ and SHBG and a possible colocalization between them. Fig. 5 shows that there is no big difference in the occurence of ERβ after short time (A) as well as long time (B) treatment with E2. We can find the receptor at the cell membrane as well as
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br Results The AR genotype frequencies are shown in
2020-09-04

Results The AR genotype frequencies are shown in Table 1. Alleles at the two loci are in linkage disequilibrium, as expected for such closely linked loci and consistent with previous findings (Kittles et al., 2001). The genotype frequency for the DBH 1021 polymorphism is similar to previous find
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The data from the Sur lab have showed DNA
2020-09-04

The data from the Sur lab have showed DNA-PK is involved in metabolic gene regulation in response to insulin. DNA-PK regulates fatty h89 receptor synthesis by modulating the protein expression of fatty acid synthase (FAS) in a feeding-dependent manner. DNA-PK induces the activation of Upstream Stimu
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Finally this study described that the lead compound acted as
2020-09-04

Finally, this study described that the lead atomoxetine hcl receptor (1) acted as an efficient alkylating agent for the G4 structure in addition to the previously reported T-T mismatch structure. The shortcoming of probe (1) is the lack of a structure selectivity, but that can be overcome by changi
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During ischemia the impact of CK on mitochondria varies in
2020-09-04

During ischemia, the impact of CK2 on mitochondria varies in different organs/tissues. For example, CK2α upregulation during ischemia leads to disrupted mitochondrial homeostasis and mediates cardiomyocyte ischemic injury [31]. Specifically, ischemia/reperfusion (I/R) progressively increases CK2α to
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