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br Recent insights into EAAT structure function aspects
2022-05-21

Recent insights into EAAT structure/function aspects The EAATs are secondary-active transporters coupling the movement of one Glu with the symport of three Na+ and one proton and the counter-transport of one K+ [3, 4]. The transporters are trimeric assemblies of protomers that function independe
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BX-912 This GluR A independent mechanism by which the associ
2022-05-21

This GluR-A-independent mechanism, by which the associative strength of spatial locations can be increased (and/or decreased) gradually over many trials, and which presumably underlies spatial reference memory acquisition during tasks such as the Morris watermaze or the radial maze (Zamanillo et al.
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Despite the potential promise of both
2022-05-21

Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty A 967079 mg dervatisation of related regulatory peptides res
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Paprotrain synthesis br GLP R expression in the vascular end
2022-05-21

GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS
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Analysis of the GHSR screening data for inactive library
2022-05-21

Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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Both preclinical and clinical studies
2022-05-21

Both preclinical and clinical studies have identified a distributed set of CNS nuclei that participate in cognitive control of feeding behavior. Preclinical studies that utilize restricted access feeding schedules (RFS) indicate that rodents learn to anticipate delivery of scheduled meals as indicat
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GOAT belongs to the super family of
2022-05-21

GOAT belongs to the super family of membrane-bound O-acyltransferases (MBOATs). It is encoded by the gene MBOAT4 in human. The protein GOAT is highly conserved from zebrafish to human (Yanagi et al., 2018). GOAT is ubiquitously expressed with abundant expression in the stomach and intestine (Sakata
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EPZ5676 Further we examined the degradation of Cx Autophagy
2022-05-21

Further, we examined the degradation of Cx43. Autophagy and the proteasome system have previously been implicated in Cx43 degradation (Falk et al., 2014). DEX inhibited communication between EPZ5676 by promoting the degradation of Cx43 through autophagy in osteocytes (Gao et al., 2016). In our exper
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Amongst oxidants that we have studied
2022-05-21

Amongst oxidants that we have studied, PMS is unique in having a greater effect in deoxygenated cells. The resulting phenotype shows some similarities with the increased cation permeability shown by deoxygenated sickle 740 Y-P [27]. It is interesting to consider why PMS has this effect. PMS functio
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br Chemistry Analog has been previously reported by
2022-05-21

Chemistry Analog 12 has been previously reported by our group. Experimental procedures for the synthesis and characterization of 13–32 are available in Scheme 1, Schemes S1–S9 and Table S1 in Supplementary data. Preparation of 30 and 31 is depicted in Scheme 1 as the representative example. Commo
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In summary the SAR of
2022-05-21

In summary, the SAR of a series of phenylpropanoic acid-free fatty CU CPT 22 receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust effic
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Conclusions br Author information The obtained models of com
2022-05-21

Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu
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Despite their undisputed importance however FPR receptors ar
2022-05-21

Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis
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With the nitrogen containing heterocycle components and the
2022-05-21

With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic Gefitinib (, and ), followed by deprotection by TFA, smoothly provided the
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In conclusion a novel series of
2022-05-21

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen BAY 87-2243 had a remarkable effect on the GPR40 agonistic activity
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