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Our previous high throughput screening HTS
2021-02-24
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based FAUC-365 receptor assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [
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The mRNA expression of asEP studied by RT
2021-02-24
The mRNA expression of asEP4 studied by RT-PCR shows that EP4 is expressed in many different tissues in Atlantic salmon which is comparable to other species (Sugimoto and Narumiya, 2007) although some distinct differences are present. For example, in mice the expression of EP4 receptor was found to
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In terms of its protease activity MME has a broad
2021-02-24
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other alk5 of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade the insulin recep
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EBI and its ligand s EBI was found in a
2021-02-24
EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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As in our earlier observations the PTPN SNP affected
2021-02-24
As in our earlier observations, the PTPN22 SNP affected the appearance of β-cell autoimmunity, but in contrast to our earlier report, only a borderline effect of the PTPN22 SNP on the progression to clinical disease was observed in the current analysis [22], [27]. The finding of an effect of the PTP
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Many studies reporting on discoveries of DUBs
2021-02-24
Many studies reporting on discoveries of DUBs in the TGFβ and BMP pathways have relied on RNAi strategies to investigate loss-of-function impact. While RNAi strategies are useful tools, there are limitations ranging from limited knockdowns of targets to potential off-target effects. New and better t
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Till date several predictive models
2021-02-24
Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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Gene amplification PCR amplifications were performed using g
2021-02-23
Gene amplification. PCR amplifications were performed using genomic DNA from the different organisms studied as template and two degenerate oligonucleotides (PP1 and PP2) as primersPP1 corresponded to the sense codons of the amino Efavirenz receptor motif AGGI(A/S)EM, and PP2 to the antisense seque
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The mutation in Caucasian people of
2021-02-23
The Δ32 mutation in Caucasian people of European heritage is quite common but extremely rare in Asian and African countries (Huang et al., 1996). We recently reported the presence of this mutation from India (Husain et al., 1998a) and established the complete inheritance pattern (Husain et al., 1998
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Roxithromycin In the course of our program which
2021-02-23
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Transduction of cellular signals by G
2021-02-23
Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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br Conclusions CK inhibition protects young
2021-02-23
Conclusions CK2 inhibition protects young and aging WM function against an ischemic episode by preserving oligodendrocytes and axonal structure by maintaining mitochondrial integrity. CK2 recruits CDK5 and AKT/GSK3ß signaling to mediate WM ischemic injury in a differential spatiotemporal manner
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Fujimoto et al pointed out that RPN
2021-02-23
Fujimoto et al. pointed out that RPN2 knockout alleviated the resistance of GC GSK2606414 australia (MKN74 and KATO III) to docetaxel and DDP [23]. Yuan et al. demonstrated that the depletion of RPN2 resulted in the reduction in resistance of GC cells to drugs such as irinotecan, docetaxel, doxorub
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br Experimental br Results and discussion br Conclusions The
2021-02-23
Experimental Results and discussion Conclusions The fungus Mucor circinelloides MUT44, previously shown to have ene-reductase activity [11], possesses ten genes coding for putative ene-reductases belonging to the Old Yellow Enzymes family. Since the reduction of CC double bonds is one of th
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Mammalian cells contain significant amounts of a relatively
2021-02-23
Mammalian cells contain significant amounts of a relatively lesser known enzyme that shows marked specifity for ether lipids containing AA and other 20–22 carbon fatty acids. This enzyme is called CoA-independent transacylase (CoA-IT), and transfers polyunsaturated moieties of 20–22 carbons, typical
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