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Our synthetic approach to GPR
2022-05-27

Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic WM-8014 to 4-piperidone by first forming the a
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Introduction Carbohydrates are some of the most
2022-05-26

Introduction Carbohydrates are some of the most stereochemically complex biological molecules found in nature. In addition to their energetic and structural roles in living systems, their role when covalently linked to proteins is critically important in a myriad of molecular recognition processes.
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Shikonin represents naphtoquinonic compound isolated from
2022-05-26

Shikonin represents naphtoquinonic compound isolated from the Chinese plant Lithospermum erythrorhizon[20]. Shikonin treatment inhibits AKT and ERK signaling pathways and induces apoptosis through FOXO transcription factors and mitochondrial pathway [21], [22]. Recent results suggest inhibition of l
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The functionally crucial arginine within
2022-05-26

The functionally crucial arginine within M2 is not encoded by the gluR2 gene, but rather arises within the pre-mRNA by editing of a codon for the neutral glutamine residue25, 26. RNA editing at the Q/R site is specific to GluR2 and is extremely efficient. In neonatal and adult rat brain, almost 100%
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Ropivacaine HCl br Introduction Glucagon is a peptide hormon
2022-05-26

Introduction Glucagon is a peptide hormone that acts to increase blood glucose levels. The secretion of glucagon from the alpha Ropivacaine HCl of the islets of Langerhans in the pancreas is increased during fasting and prevents hypoglycemia. Glucagon increases glycogenolysis and gluconeogenesis
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br Acknowledgments br Introduction Postmenopausal osteoporos
2022-05-26

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by salubrinal deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of
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br Competing interests br Acknowledgements br Introduction F
2022-05-26

Competing interests Acknowledgements Introduction - Factors Regulating Glucose Tolerance Strictly speaking, the incretin effect refers to the amplification of insulin secretion, which occurs when vitamin d3 sources synthesis is taken in orally as compared to infused intravenously [1]. Norma
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br Materials and methods br Chemical synthesis br Declaratio
2022-05-26

Materials and methods Chemical synthesis Declaration of interest Acknowledgements This research was supported by a grant from the National Institute for General Medicine to K.W.M. (GM 58448) and by the Department of Anesthesia, Critical Care & Pain Medicine at Massachusetts General Hospi
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br Medium to long chain fatty acids Medium
2022-05-26

Medium- to long-chain fatty acids Medium- to long-chain fatty acids impart a wide range of physiological effects. Medium-chain and long-chain fatty acids have 6–12 carbons and >12 carbons, respectively. As the energy source, these fatty acids are supplied primarily by food intake, biosynthesis, a
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Binding of FGFs to FGFRs leads
2022-05-26

Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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The ETB receptor has been shown to decrease
2022-05-26

The ETB receptor has been shown to decrease sodium transport in the renal medullary collecting duct and medullary thick ascending limb of Henle10, 11, 12, 13, 18. However, both inhibitory and stimulatory effects of endothelin have been reported in the proximal tubule16, 47, 48, 49. In the rat, endot
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br Author contributions br Declaration of
2022-05-25

Author contributions Declaration of conflict of interest Acknowledgements We are grateful to the Director, National Institute of Immunology for his support. The work was partially supported by J.C. Bose Fellowship to SSM. We acknowledge the help from staff of Small Animal Facility of Nation
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For the SAR study human
2022-05-25

For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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To identify structurally novel autophagy inhibitors a
2022-05-25

To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 Ac-YVAD-CHO stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automate
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The inhibitory concentration of atrial natriuretic factor at
2022-05-25

The 50% inhibitory concentration of atrial natriuretic factor at midgestation and term are –7.4 ± 0.12 and –7.38 ± 0.11, respectively, demonstrating no gestational age dependency in the effect of atrial natriuretic factor on spontaneous contractile activity. Diethyl amine/nitric oxide starts to inh
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