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Secondly leptin has been shown to enhance aromatase mRNA exp
2024-08-15

Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer procollagen c proteinase by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites
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Finally the comparison between data
2024-08-15

Finally, the comparison between data obtained by antioxidant assays in in vitro cultured cells [11], [12] and in liposomes has disclosed the possibility to choose more confidently “the better phenolipid” of a series of fatty acids esters antioxidant derivatives. Looking at the physical parameters th
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In summary present evidence suggests that antimicrobial ther
2024-08-15

In summary, present evidence suggests that antimicrobial therapy for intra-abdominal sepsis can be shortened in patients exhibiting a clinical response to treatment. Hence, clinicians should use the resolution of clinical signs of infection as a guide to determine when during the 4–7-day window anti
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In order to postulate its binding mode in
2024-08-15

In order to postulate its binding mode in APN, luciferin mg 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupied by
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We recently identified a G A dependent epigenetic mechanism
2024-08-15

We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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Recently two distinct small molecule
2024-08-15

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer VX-765 with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the growth a
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br Acknowledgements Dr Paul J Gasser is
2024-08-15

Acknowledgements Dr. Paul J. Gasser is supported by the National Institutes of Health (grant number R01DA032895), and the Charles E. Kubly Mental Health Research Center. Dr. Christopher A. Lowry is supported by the National Institutes of Health (grant number R21 MH116263), the Department of the N
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Canrenone The introduction of a pyrazole moiety into
2024-08-14

The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,
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br Increased blood ATX and LPA in liver fibrosis Although
2024-08-14

Increased blood ATX and LPA in liver fibrosis Although previous in vitro findings have suggested a link between LPA and liver fibrosis in vivo, whether LPA plays a primary role in the pathogenesis of liver fibrosis has remained uncertain. No phenotypic changes in livers of LPA receptor-deficient
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V ATPase is a complex
2024-08-14

V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial ubiquitin conjugating enzyme of rats has been reported to contain V-ATPase which is distributed at the apical pole of t
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exemplifies three of the compounds investigated in
2024-08-14

exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC DLPC as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products. As BL
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The allosteric site of class C receptors is generally locate
2024-08-14

The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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Analysis of ASK crystal structures as well
2024-08-14

Analysis of ASK1 crystal structures as well as an investigation of how AICAR 4 might bind were undertaken to understand opportunities for engaging Gln756. To this end a docking model derived from PDB 3VW622 was used to predict the binding mode of amide 4 in the ASK1 active site as shown in Fig. 4.
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Apelin is a peptide hormone and
2024-08-14

Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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Recent retrospective cohort studies have supported
2024-08-14

Recent retrospective cohort studies have supported these preclinical findings in animals indicating the correlation of AR activation with the induction of LY2109761 carcinogenesis. First, men with prostate cancer who underwent androgen deprivation therapy were shown to have a significantly lower ri
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