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Historically covalent drugs have had great success e g
2021-01-09
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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br Patients and Methods Patients who
2021-01-09
Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl) l
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Next we evaluated whether DPP inhibitor suppressed
2021-01-09
Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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br Introduction Acinetobacter baumannii is a gram negative o
2021-01-09
Introduction Acinetobacter baumannii is a gram-negative opportunistic pathogen that causes nosocomial infections including pneumonia and bloodstream infections which is associated with an increased mortality and multi-drug resistance [[1], [2], [3]]. A. baumannii was rated as one of the critical
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Till date several predictive models have been developed by d
2021-01-09
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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It is noteworthy that epidemiological studies
2021-01-09
It is noteworthy that epidemiological studies have demonstrated that some GAD patients have experienced anxiety symptoms in childhood and young adulthood, whereas others have developed their disorder at a later age (especially persons ≥ 50 years of age) (Hoehn-Saric et al., 1993; Le Roux et al., 200
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br Experimental Procedures br Acknowledgments br Bisphenol A
2021-01-09
Experimental Procedures Acknowledgments Bisphenol A (BPA) has been recognized as one of the most potent endocrine disruptors, functioning even at very low doses. Although it is anticipated that 4-P-PDOT receptor (ER) would mediate these effects of low-dose BPA, studies revealed that BPA boun
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Compared with qualitative analysis by Kalyankar et
2021-01-09
Compared with qualitative analysis by Kalyankar et al. (2013), less sequences were identified in iTRAQ-labelled analysis. It is not surprising with the finding that each of the identified peptide includes the sequence in every sampling point. Glu(51)-Tyr(52) of αs2-casein was observed to have been c
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ICT is a product of
2021-01-09
ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene
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TC-I 2000 br Experimental Procedures br Acknowledgments
2021-01-09
Experimental Procedures Acknowledgments The authors wish to thank P. Costet (University of Bordeaux) and Véronique Guyonnet-Duperat (FR TransBioMed, Plateforme de Vectorologie, University of Bordeaux) and Prof. Nils-Göran Larsson and Dr. Bettina Bertalan (Max Planck Institute for Biology of Ag
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Considering the divergence of multiple DGAT isoforms
2021-01-09
Considering the divergence of multiple DGAT isoforms, we examined whether MiDGAT1 and MiDGAT2s utilized different fatty acids as the substrate to synthesize TAGs. GC-MS analysis indicated that C16:0 and C18:0 were the major components of TAGs in yeast cells, and all three MiDGATs displayed the same
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ppar pathway In conclusion high methylation levels of
2021-01-08
In conclusion, high methylation levels of CDKL2 were observed both in HCC cell lines and tissues, which showed a negative association with mRNA expression. Moreover, treatment with demethylation agent in HCC cell lines could upregulate CDKL2 mRNA expression. The discovery of the epigenetic modificat
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With a favorable spectrum of CRTh
2021-01-08
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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Moreover as shown in Fig f while the knockdown
2021-01-08
Moreover, as shown in Fig. 5f, while the knockdown of SMURF2 in wild-type CL 316243 disodium salt has no significant effect on HSP27, in CK2α/α′(−/−) cells it leads to an increase of HSP27 level. These results suggest that SMURF2 affects HSP27 protein stability only when overexpressed, at least in o
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br Acknowledgements We thank A Devia Barros and S A
2021-01-08
Acknowledgements We thank A. Devia-Barros and S.A. Barrios Latorre for invaluable technical support during the collection, maintenance and exposure of oysters. We are, furthermore, grateful to the municipal marina of Santa Marta for authorizing access to their facilities and to A. Franco for faci
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