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We show that pharmacological inactivation of GSTP over a sus
2022-08-24
We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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Further our study provides the first evidence that
2022-08-24
Further, our study provides the first evidence that zaprinast and kynurenic tyrosine kinase receptor administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effec
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Because of its excellent GPR potency
2022-08-24
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Oseltamivir acid was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive pa
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Depressed survival rate body weight and
2022-08-24
Depressed survival rate, body weight, and colon length along with elevated clinical score comprise the essential characteristics of IBD (Hung et al., 2014; Shen et al., 2011; Sun et al., 2010). In the present study, we found that SB improved the survival rate, body weight, and colon length and decre
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br Acknowledgments This work was supported by the Russian Fo
2022-08-24
Acknowledgments This work was supported by the Russian Foundation for Basic Research [grant number 16-04-00205], The Russian Science Foundation [grant number 16-15-00235], Czech Academy of Sciences [grant number RVO 61388963], and the Technology Agency of the Czech Republic [grant number TE010200
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Ability of D Ala GIP to attenuate the neurobehavioral
2022-08-23
Ability of D-Ala2GIP to attenuate the neurobehavioral sequelae in QA-induced Huntington's disease model by reduction in lipid peroxidation, restoration of endogenous antioxidants and decreased striatal monoamine levels is of potential interest. Considerable preclinical evidence now exists of the pot
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Calcium Gluceptate Knowing that our strongest phenotypic dif
2022-08-23
Knowing that our strongest phenotypic differences between the genotypes involved feeding behavior in various contexts, we decided to examine the case of restricted feeding and food anticipatory activity. Animals faced with a restricted schedule of food availability develop a series of anticipatory b
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In this study we demonstrate that the ETS
2022-08-23
In this study, we demonstrate that the ETS transcription factor ETV5 is involved in the regulation of ghrelin system in response to the altered nutritional state. In the recent multiple GWAS studies, three single nucleotide polymorphisms (SNPs) of ETV5, rs7647305 (Thorleifsson et al., 2009; Willer e
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K-Ras(G12C) inhibitor 12 Cytokines and hormones influence bo
2022-08-23
Cytokines and hormones influence both gap junctions [106] and endocrine activity in the pituitary [3]. Long-term treatment (2 h) with the proinflammatory cytokines interleukin-1β (Il-1β) and tumor necrosis factor-α (TNF-α) transiently increases Cx43 expression and cell coupling in TtT/GF K-Ras(G12C)
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Pharmacological inhibition of PKR seems to be an interesting
2022-08-23
Pharmacological inhibition of PKR seems to be an interesting strategy for revealing the role of PKR in oxytosis and ferroptosis. The oxindole/imidazole derivative C16 was identified by screening a library of 26 different ATP-binding site-directed inhibitors of varying structure that is more selectiv
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The release of FBPase and aldolase from subcellular
2022-08-23
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle 5 03 was about 6–7 times higher in the presence o
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MST are involved in signalling pathways following along
2022-08-22
MST1/2 are involved in signalling pathways following along the canonical and noncanonical Hippo pathway. The canonical pathway is highly conserved between D. melanogaster and mammals and a master regulator of tissue growth. During development and within the canonical pathway, MST1/2 seem to have red
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Introduction Breast cancer is the
2022-08-22
Introduction Breast cancer is the most common cancer among women worldwide, representing 30% of new cancer diagnoses. In addition, it is the second leading cause of cancer deaths among women [1]. With regard to the risk of breast cancer, proper diagnosis and stratification of tumors for individuali
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The selection of mutations in
2022-08-22
The selection of mutations in vivo with antivirals is a complex process involving, among other things, the frequency of a given mutation prior to treatment, the effect of that mutation on viral protein function, and the interplay of a given mutation pattern with host immune mechanisms. Investigation
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Despite the rapid development of synthetic ligands the endog
2022-08-22
Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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