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Anti apoptotic Bcl proteins have
2021-11-15
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients wi
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Introduction Hepatocellular carcinoma HCC is
2021-11-15
Introduction Hepatocellular carcinoma (HCC) is the fifth most lethal malignant tumor worldwide and is the second leading cause of cancer-related death [1]. For HCC patients, mocetinostat virus (HBV) infection is the important causative risk factor in Asia-Pacific regions [[2], [3], [4]]. In China,
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The neotropical fish Prochilodus lineatus has been widely
2021-11-15
The neotropical fish Prochilodus lineatus has been widely used in experimental designs for being sensitive to variations in water quality and tolerant to laboratory conditions (Camargo and Martinez, 2006, Cazenave et al., 2014, da Silva and Martinez, 2014, Vieira et al., 2016). Concern and reports a
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br Introduction The Ras superfamily of small GTPases
2021-11-15
Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches
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We compared the age BMI and relevant laboratory variables
2021-11-12
We compared the age, BMI and relevant laboratory variables between the two groups of risk factor multiplicity. The results are presented in Table 7 for the women and in Table 8 for the men. The individuals with an increased erythrocyte adhesiveness/aggregation can clearly be seen to be older, more o
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Next we focused on B part the phthalazine ring While
2021-11-12
Next, we focused on B-part, the phthalazine ring. While both nitrogen atoms of the phthalazine ring were found to be important (data not shown), replacing the benzene ring of the phthalazine part was attempted, and shows the results of the substituted pyridazine rings with bearing 2-methoxy benzene
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AS601245 Analysis of the GHSR screening
2021-11-12
Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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br Neural circuits that control hunger
2021-11-12
Neural circuits that control hunger Ghrelin & cognitive control of feeding Ghrelin is a 28 amino Aminoallyl-dUTP - Cy3 receptor orexigenic peptide that stimulates food intake in rodents and patients (Andrews, 2011, Cummings, 2006, Horvath et al., 2001, Müller et al., 2015, Nakazato et al., 200
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Two excellent GSMs with clear pharmacological effect
2021-11-12
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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We tested formyl MYVKWPWYVWL which we
2021-11-12
We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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In conclusion we have demonstrated that the
2021-11-12
In conclusion, we have demonstrated that the ejection of structural zinc ions from G9a and GLP in the presence of selenium-, and sulfur-containing electrophilic small DS2 leads to inhibition of these two biomedically important epigenetic enzymes. Our work demonstrates that clinically used ebselen, d
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br The HDC knockout mouse as a pathophysiological
2021-11-12
The HDC knockout mouse as a pathophysiological model of TS The implication of a hypomorphic allele of the Hdc gene as a rare cause of TS (Ercan-Sencicek et al., 2010) created a rare opportunity for the generation of a pathophysiologically grounded model of the disorder. Modeling pathophysiology o
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Ultimately the change of maturation ratio of the
2021-11-12
Ultimately, the change of maturation ratio of the Leydig cell caused reducing of INSL3 expression undoubtedly. INSL3 (insulin-like 3) is a hormone produced mainly in gonadal tissues. It was discovered to participate in development of urogenital tract. The mutations of this gene is one cause of crypt
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Finally worth of mention are few papers that
2021-11-12
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Tetrazole library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series o
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br Experimental br Acknowledgments The
2021-11-11
Experimental Acknowledgments The authors are grateful to Fundamental Scientific Research Fund of Chinese Academy of Medical Sciences (No. 2016ZX350030) for financial support. Introduction 2-Lysophosphatidylcholines (1-acyl-glycero-3-phosphocholines, 2-LPC) are blood derived factors involve
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