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kisspeptin To directly address whether pharmacological atten
2021-12-13
To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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Taken together our results show that at
2021-12-13
Taken together, our results show that, at least in the in vitro cell line model, methylation within the proximal promoter region of GHSR is an important determinant of its expression; however, to determine whether this represents a physiologically and or pathophysiologically relevant event, further
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In conclusion starting from the weakly potent
2021-12-13
In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic src kinase inhibitor led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally report
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br Acknowledgements This work was
2021-12-13
Acknowledgements This work was supported under the National Natural Science Foundation of China (Grant numbers 31200576, 21472197, 21675162), Beijing Natural Science Foundation (Grant No. 7182189), and Project supported by the Joint Funds of the National Natural Science Foundation of China (Grant
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br Materials and methods br Results and discussion
2021-12-13
Materials and methods Results and discussion In order to identify genes required for photoautotrophic growth, we screened a random insertion mutant library of Synechocystis 6803 and obtained many mutants with impaired photoautotrophic growth. About 6000 random insertion colonies of the mutant
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br Acknowledgments This study was financially supported by N
2021-12-13
Acknowledgments This study was financially supported by National Science Center Poland grant No DEC-2011/02/A/NZ4/00031 (KKK), Jagiellonian University Medical College (Poland) grants: K/ZDS/007130 (SM) and K/ZDS/007131 (SM), COST Action CA15135 (DŁ, HS, KKK) and DFG INST 208/664-1 FUGG (HS). Than
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br Materials and methods br Results br Discussion Several
2021-12-13
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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Pharmacologic approaches of inhibiting GSNOR activity have r
2021-12-10
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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The Berlin patient is a unique case
2021-12-10
The Berlin patient is a unique case and dependent on the histocompatibility-matched CCR5Δ32/Δ32 homozygous donors. These donors occur at a little higher rate in the European Caucasian population, but they are very rare in Asians and Africans.15, 16, 17 The recently developed genome-editing technolog
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Armed with this knowledge we looked at ways to
2021-12-10
Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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In this report we characterized
2021-12-10
In this report, we characterized MRJP-containing TPMPA and other (glyco)proteins from honey. Honey glycoproteins demonstrated potent anti-C. elegans activity. It has been reported that molecules that kill C. elegans are likely to be toxic to parasitic nematodes (Burns et al., 2015). To examine mole
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Shikonin represents naphtoquinonic compound isolated
2021-12-10
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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br Conclusion The mitochondrial and glycolytic energy metabo
2021-12-10
Conclusion The mitochondrial and glycolytic energy metabolism of the brain is coordinated by HKI binding to MOM, although the molecular mechanism of such a regulation is not yet clear. The 2449 for HKI in MOM are VDACs [[5], [6], [7]], mainly the VDAC1 isoform [8]. Using a computational model, w
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Initial experiments confirmed that RBC effectively
2021-12-09
Initial experiments confirmed that RBC8 effectively inhibited both RalA and RalB activation in an identical, dose-dependent manner following platelet stimulation with the GPVI-specific ligand, CRP (Fig. 1Ai). Non-specific, upper bands were observed when immunoblotting for activated RalB, with the sp
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PSB 0777 ammonium salt The differentially expressed proteins
2021-12-09
The differentially expressed proteins during somatic embryogenesis are described as the proteins that are induced by oxidative stress and respond to higher cell division activity including ascorbate peroxidase, dehydroascorbate reductase, glutathione transferase and mitochondrial manganese superoxid
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