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To gain insights for further improvement
2022-01-29
To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocycli
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br Acknowledgments This work was
2022-01-29
Acknowledgments This work was funded by NIH Grant 2R01 MH066958 (JGT) and NSF CAREER award IOS- 1053716 (NV). We thank Dr. Greti Aguilera for the generous gift of the GRE-Luciferase construct and Dr. Louis Muglia for the generous gift of the GR-GFP construct. Introduction Prostate cancer (PCa
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Various strategies have been pursued in
2022-01-29
Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino Mouse iPSC Chemical Reprogramming Cocktails Kit plus synthesis substitutions of GIP(1–42) [19], and various GI
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N Cadherin facilitated gap junction formation
2022-01-29
N-Cadherin facilitated gap junction formation between embryonic lens R547 by stabilizing membrane appositions (Frenzel and Johnson, 1996). Cx43 has been found to be delivered to N-Cadherin-positive membrane HeLa cells (Shaw et al., 2007), and N-Cadherin determine the localization of Cx43 in cardiac
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The Hippo pathway is a growth control signaling
2022-01-28
The Hippo pathway is a growth control signaling cascade that has been demonstrated to play an important role in regulating cell proliferation and differentiation [5,6]. The core signaling pathway consists of a group of kinases which negatively regulate the expression of transcriptional co-activators
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br Introduction Depressive disorder is a syndrome characteri
2022-01-28
Introduction Depressive disorder is a syndrome characterized by a group of heterogeneous symptoms that affect more than 350 million people worldwide, 4% of world population (WHO, 2012). The WHO estimates depression will be the leading global cause of disability in 2020, with tremendous economic c
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In this study we examined whether zebrafish ionocytes might
2022-01-28
In this study, we examined whether zebrafish ionocytes might also share other types of similarity in transport function with kidney cells. In addition to ion transport, mammalian kidney Prochlorperazine australia also play key roles in xenobiotic elimination, through the action of ATP-Binding Casse
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Here we reported series of carbohydrate
2022-01-28
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 Metabolism Compound Library sale and their polyol structures give them many unique biological properties as we have desc
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br Results br Discussion Using a novel viral
2022-01-28
Results Discussion Using a novel viral vector for norepinephrine-targeted gene deletion, we have shown that glucocorticoid receptor Curcumol from locus coeruleus norepinephrine neurons reduces social interaction specifically in female mice. This effect is not attributable to changes in novelty
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Some of the key aspects of the
2022-01-27
Some of the key aspects of the myofibroblasts’ biology, including their signaling sensitivity and residual regenerative potential, are shaped by their origin. In this respect, lineage studies on myofibroblast precursors are critical for increasing our understanding of the natural history of fibrosis
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Interestingly we have shown that OA
2022-01-27
Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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Recently they reported an enyne chemotype agonist Fig with l
2022-01-27
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral see you through (tmax=15min) and a decent pharmacokinetic profile
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CGP 57380 However T DM and associated hyperglycemia can adve
2022-01-27
However, T1DM and associated hyperglycemia can adversely affect the structure and function of the heart in several mechanisms including inhibiting the anabolic effect of insulin due to its deficiency, generation of higher levels of ROS and induction of lipid peroxidation, and subsequent activation o
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unlikely br Acknowledgments This research was
2022-01-27
Acknowledgments This research was supported by the National Institutes of Health Grants GM58442 and GM084152, as well as the National Institutes of Health Predoctoral Training Grant 5T32GM008700-13. We thank Eric Oldfield (University of Illinois, Urbana-Champaign) for providing the FDPS inhibitor
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MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl q
2022-01-27
MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr
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