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The general synthetic routes leading
2021-09-28
The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic Fmoc-Cys(Trt)-ol australia analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is w
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The transport of glutamate by EAAT from
2021-09-28
The transport of glutamate by EAAT2 from the extracellular fluid into either astrocytes or endothelial cells is an unfavorable and energy-consuming process. This energy is provided by a coupled co-transport of three sodium ions, one proton, and one glutamate molecule in the counter-transport of one
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br Acknowledgements This work was
2021-09-28
Acknowledgements This work was financed by the projects “Mejora Genética del Almendro” (MINECO-Spain, AGL2017-85042-R), “The molecular mechanisms to break flower bud dormancy in fruit trees” to RS-P within the Villum Young Investigator Program and by the VILLUM Research Center for Plant Plasticit
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It is notable that pharmacological
2021-09-28
It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin cond
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In a mouse model of hyperhomocysteinemia a risk
2021-09-27
In a mouse model of hyperhomocysteinemia (a risk factor for the development of vascular dysfunction) it has been shown that myoendothelial communication is enhanced due to increased expression of Cx37 and IK1 Dextran sulfate sodium salt [], allowing the propagation of endothelial signals to VSMC and
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Our observation of LPS induced increase in
2021-09-27
Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary RG-108 towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. However, the possible recrui
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Multiple subsets of Breg cells in mice
2021-09-27
Multiple subsets of Breg cells in mice have been identified that could suppress the T cell-mediated response. However, a lack of consensus surface markers for Breg cells made it difficult to judge whether Breg cells are a special B cell subset or whether all leukotriene receptor antagonists have an
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br Hh Proteins at a Glance Hh family proteins are
2021-09-27
Hh Proteins at a Glance Hh family proteins are evolutionarily conserved morphogens that provide cells with positional information and fate instruction during early embryonic development. After development, Hh ligands contribute to tissue homeostasis and wound healing 1., 2.. Consistent with these
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The compounds f and a e were found to
2021-09-27
The compounds 8f and 9a–e were found to be potent inhibitors of both isoforms of GSK-3 as characterized by IC50 values in the low nanomolar range. In addition, all of them showed good selectivities against other kinases. Substituents in the ortho- and para-positions of structure 8 and 9 lead to pote
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GPR and TRPV co localized in
2021-09-27
GPR35 and TRPV1 co-localized in small- and medium-diameter DRG neurons. Nociceptive (Aδ- and C-fiber) neurons expressing TRPV1 mediate hyperalgesia, neurogenic inflammation, and neuropathic pain [12]. The cAMP-protein kinase A (PKA) dependent modifications of TRPV1 currents have been demonstrated in
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Thus synthesized thienopyrimidine derivatives were evaluated
2021-09-27
Thus synthesized thienopyrimidine derivatives were evaluated in vitro for GPR119 agonistic activity, and the results are summarized in , , . First, we fixed the 4-methylsulfonylphenyl substituent at the R position on the thienopyrimidine ring, and derivatized at the R position. As shown in , and sho
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br Disclosure statement br Acknowledgements We thank Dr Rona
2021-09-27
Disclosure statement Acknowledgements We thank Dr. Rona Carroll for her contribution to the preparation of the manuscript and Dr. Iosif Pediaditakis for his contribution to the preparation of the figures. This work was supported by NIHR01 HD019938 to U.B.K. Introduction The mammalian hypot
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Previous studies have shown that zinc interacts with other
2021-09-27
Previous studies have shown that zinc interacts with other allosteric modulators at the glycine receptor (Kirson et al., 2013, McCracken et al., 2010, McCracken et al., 2013). Of note, the chelation of zinc via tricine decreases the effects of alcohol at α1-, α2-, and α3-containing glycine receptors
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br Introduction Glucokinase GCK hexokinase IV is
2021-09-26
Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter i
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As early as glucagon was shown to increase
2021-09-26
As early as 1957, glucagon was shown to increase Clobetasol propionate expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [
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