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A high throughput screening campaign of the
2022-08-12
A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also cont
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gamma secretase inhibitor P gps expressed in cells and
2022-08-12
P-gps, expressed in gamma secretase inhibitor and tissues of human and animals, play an active role in cellular protection against multiple toxicants by transporting them out of a cell. Thus, improving transport activity of P-gp may contribute to removing Cd from living oysters. Cd accumulation in
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Here we reported series of carbohydrate modified compounds c
2022-08-12
Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of GLP-2 (rat) and their polyol structures give them many unique biological properties as we have described earlier. More i
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br Introduction Glucose is the major carbon source in
2022-08-12
Introduction Glucose is the major carbon source in most organisms. Cancer wehi in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mainly mediat
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The regulation of the stem cell compartment in
2022-08-12
The regulation of the stem cell compartment in CML is dynamic, in particular, during disease progression to a blast crisis and might involve a complex cross-regulation of Hh, Wnt, Notch, and hox signaling pathways (). Significant upregulation of Ptch1 and cyclin D1, upon other proteins, marks the bl
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Newt GHS R a proteins expressed in a mammalian cell
2022-08-12
Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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Introduction Risk factors for colorectal cancer
2022-08-12
Introduction Risk factors for colorectal cancer (CRC) include high-fat diets, sedentary lifestyles, obesity, diabetes, and elevated serum levels of toxic bile acids (BAs) (de Aguiar Vallim et al., 2013, Degirolamo et al., 2011, Downes and Liddle, 2008, Font-Burgada et al., 2016, Kuipers et al., 201
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Bupivacaine HCl br Acknowledgments We apologize for the
2022-08-11
Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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nitric oxide synthase inhibitors br An approach for the key
2022-08-11
An approach for the key challenges facing forensic science One of the key challenges for forensic science is to avoid being side-tracked by one of the louder narratives in the media that the big problem forensic science faces is ‘junk science’ and ‘rogue scientists’. These are clearly important i
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br Conclusions In this study we report the genotype frequenc
2022-08-11
Conclusions In this study, we report the genotype frequencies for GSTT1, GSTP1, and GSTM1 in Jamaican children. The frequency of the null genotypes of GSTT1 and GSTM1 are similar to those of African-Americans in the US. The GSTP1 genotype frequency is closer to that of the African-American popula
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Some biguanides can cross the mitochondrial membrane and inc
2022-08-11
Some biguanides can cross the mitochondrial membrane and increase L-lactate formation by inhibiting oxidative Cytidine 5-triphosphate synthesis [34]. On the other hand, it has also been reported that levels of fasting plasma lactate in T2DM patients are similar regardless of whether or not metformin
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In conclusion we have identified ten novel GPCR genes and
2022-08-11
In conclusion, we have identified ten novel GPCR genes and a pseudogene. Transcripts for GPR78, GPR81, GPR94, GPR95, GPR101, GPR103 and P2Y were detected in various CNS and peripheral tissues. Given the high levels of identity observed within paralogous oGPCR gene clusters, future efforts will likel
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GPR is a G protein coupled receptor that has pro
2022-08-11
GPR55 is a G protein-coupled receptor that has pro-oncogenic properties and whose expression correlates with tumor aggressiveness and increased activation of extracellular signal-regulated kinase (ERK) cascade [12]. Elevated expression of GPR55 has been linked to aggressiveness in human pancreatic,
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osi sc 175 br Funding This work was partially
2022-08-11
Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Werth
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Having shown that some of substitutions Cl CF
2022-08-10
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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