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By measuring the accumulation of
2022-05-19

By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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br Declarations of interest br Founding information This wor
2022-05-19

Declarations of interest Founding information This work was partially supported by the New Energy and Industrial Technology Development Organization (NEDO) Japan [grant number P03043]; and Grants-in-Aid for Scientific Research [grant number 16H00738 to H.M.] from the Japan Society for the Prom
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br Introduction Before planning population
2022-05-19

Introduction Before planning population-based genetic analysis or GWAS, it is important to annotate the sequence of the gene because these sequences represent the major sites such as promoter and transcription factor cytoskeleton which may ultimately affect the expression of the gene. Similarly,
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The stability and function of the HIF
2022-05-19

The stability and function of the HIF-1α protein are affected by many post-translational modifications (PTMs), including hydroxylation, acetylation, ubiquitination and SUMOylation [[29], [30], [31]]. It has been shown that HIF-1α stability is regulated by LSD1 [25]; in particular, the Set9 histone m
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br Acknowledgements br Introduction Pregnancy brings forth s
2022-05-19

Acknowledgements Introduction Pregnancy brings forth significant metabolic reprogramming that induces a number of metabolic changes to ensure that the nutrient requirements of the mother and fetus are met [[1], [2], [3]]. These adaptations change radically over the period of pregnancy dependin
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arginase inhibitor Cysteine Cys residues are frequently foun
2022-05-18

Cysteine (Cys) residues are frequently found to be highly conserved within functional, regulatory, catalytic, or binding sites of proteins. Thiol or thiolate chemistry imparts active sites with unique properties like nucleophilicity, high affinity metal binding, and disulfide bond assisted multimeri
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The imidazopyridines and related imidazopyrimidines and were
2022-05-18

The imidazopyridines and related imidazopyrimidines – and – were constructed from the key amine intermediates – ( X=CH and Ar=2-FPh, X=N and Ar=2-FPh, X=CH and Ar=5-pyrimidine, X=CH and Ar=2-methyl-5-pyrimidine, and X=CF and Ar=2-methyl-5-pyrimidine). These were synthesized a modified Horner–Emmons
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We previously evaluated the immuno modulatory efficacy of GS
2022-05-18

We previously evaluated the immuno-modulatory efficacy of GSNO in different EAE models and reported prophylactic and therapeutic efficacy of GSNO against the clinical disease of EAE [22], [36]. GSNO inhibited the IL-6-induced STAT3 activation (Tyr705 phosphorylation) by S-nitrosylation of the STAT3
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Exemestane br Family A Receptors as Promiscuous
2022-05-18

Family A Receptors as Promiscuous Sensors for Peptone and Free Fatty Acids (FFAs) In addition to the family C 7TM receptors, several family A 7TM receptors are promiscuous in their ligand preferences, and several respond to organic nutrients from food, notably protein degradation products and FFA
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br Acknowledgments This work was supported by the National I
2022-05-18

Acknowledgments This work was supported by the National Institutes of Health (R01 A1084898) to M.V. Williams and M.E. Ariza. Introduction Female pattern hair loss (FPHL) has emerged as the preferred term for androgenetic alopecia (AGA) in women due to the uncertain relationship between androg
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br Materials and methods br Results br Discussion In this
2022-05-18

Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the fxr agonist coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprinast in the GP
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No compounds in this series showed
2022-05-18

No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma
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57 100 br Acknowledgments This work was supported by
2022-05-18

Acknowledgments This work was supported by the Slovak grant agency VEGA, Grant 2/0084/13. We would like to thank Dr. J. Bauer for careful reading of the manuscript. Introduction Glycine is an important neurotransmitter which regulates both 57 100 inhibitory neurotransmission and excitatory ne
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To this end we evaluated novel D analogs for
2022-05-18

To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell acpt systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-substituted-2-m
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Epidemiological studies revealed that vitamin D deficiency w
2022-05-18

Epidemiological studies revealed that vitamin D deficiency was associated with a wide range of neuropsychiatric disorders and neurodegenerative diseases, in particular, Alzheimer's and Parkinson's disease (Annweiler et al., 2013; Knekt et al., 2010), dementia and cognitive function impairment (Balio
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