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br Conclusion br Competing interests br
2020-11-28

Conclusion Competing interests Authors' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number
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Present malarial chemotherapies mainly rely on a very
2020-11-28

Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa
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P falciparum DHFR TS is a particularly important
2020-11-28

P. falciparum DHFR-TS is a particularly important enzyme, because it is from the protozoan species that is associated with most malaria infections. Since this enzyme is responsible for catalyzing sequential reactions in the thymidylate cycle, its inhibition slows malarial dTMP production and therefo
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BMI-1 inhibitor Studies on the external dehydrogenases of N
2020-11-28

Studies on the external dehydrogenases of N. crassa have shown that the NDE1 protein is a Ca2+-dependent external NADPH dehydrogenase, while NDE2 is characterized as a dehydrogenase oxidizing both cytosolic substrates (external NADH and/or NADPH) (Carneiro et al., 2004, Melo et al., 2001). All three
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br Materials and methods br Acknowledgements
2020-11-28

Materials and methods Acknowledgements SD was supported by a pre-doctoral research fellowship from the Flanders Agency for Innovation and Entrepreneurship (VLAIO-Flanders, Belgium). YB is supported by a postdoctoral fellowship from Research Foundation Flanders (FWO, Belgium). We thank Isabelle
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br Materials and methods br
2020-11-28

Materials and methods Results The monoclonal antibody (mAb), 12G5, reacts specifically with the human fusin protein and recognizes the protein on many T-cell lines such as the SUP-T1 Nocodazole (Endres et al., 1996). As shown in Fig. 1, AMD3100 at 25 μg/ml completely inhibited the binding of
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The identification of CRF receptor subtypes has
2020-11-28

The identification of CRF all trans retinoic acid 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 condition
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In conclusion adipose PGD suppressed
2020-11-28

In conclusion, adipose PGD2 suppressed the lipolysis by decreasing the intracellular cAMP level through DP2R. Therefore, PGD2 enhanced adipocyte differentiation (lipid accumulation) through both repression of the lipolysis via DP2R and activation of the lipogenesis via PPARγ. Thus, L-PGDS and DP2R a
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Both anxiogenic and antinociceptive effects produced by CRF
2020-11-28

Both anxiogenic and antinociceptive effects produced by CRF seem to be selective for the CRF1 receptor, since intra-dPAG microinjection of ASV 30, a CRF2 receptor antagonist, altered neither the anxiety nor the antinociception response. Intra-dPAG ASV 30 was also unable to prevent the anxiogenic (ob
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Under optimized assay conditions very low
2020-11-28

Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO AT9283 membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because little specific bindin
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Introduction Robust evidence suggests that
2020-11-28

Introduction Robust evidence suggests that genetic factors influence an individual's susceptibility to BD (Craddock and Sklar, 2013). Yet, no single, high penetrance gene has been identified with direct causality (Craddock and Sklar, 2009). The largest GWAS to date for identifying genes conferring
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Among the other mediators which have been reported to play
2020-11-28

Among the other mediators which have been reported to play a role in erection are prostaglandins (PGs). Several studies have reported that alprostadil- synthetic PGE1- showed high efficacy in management of erectile dysfunction as it induces corpus cavernosal relaxation. Alprostadil has been first de
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Replacement of the saturated propoxy group
2020-11-27

Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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More importantly Santagata et al have
2020-11-27

More importantly, Santagata et al. have suggested a new breast cancer subtyping method according to ER, androgen receptor (AR), and VDR with a higher prognostic value than the ordinarily used method based on ER, progesterone receptor (PR) and Her2 (Santagata et al., 2014). This implies that such com
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For the current studies we used the
2020-11-27

For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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