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Recently unimolecular multi functional peptides
2021-10-15
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with γ-Secretase inhibitor IX and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose con
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Newt GHS R a proteins
2021-10-15
Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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According to the aforementioned preclinical
2021-10-15
According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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Next we were interested in replacing
2021-10-14
Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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Thus from this preliminary study a working model of
2021-10-14
Thus from this preliminary study, a working model of HIV-1 integrase was developed from which a selective inhibitor of the strand-transfer reaction displaying whole-cell activity and negligible cytotoxicity was produced. Compound 9 provides a promising scaffold for further elaboration, and current i
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In the present study we investigated the
2021-10-14
In the present study, we investigated the mechanisms underlying the ability of 5-FU to modify histone acetylation. Our results suggested that 5-FU induces global histone de-acetylation in CRC by promoting the degradation of p300 and CBP, two important homologous HATs catalyzing acetylation at multip
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br Introduction Lysine acetylation is an important post tran
2021-10-14
Introduction Lysine acetylation is an important post-translational modification that is found on numerous cellular proteins, including both histone and non-histone proteins [1], [2]. Dynamic acetylation and deacetylation is regulated by enzymes called histone acetyltransferases (HATs) as writers
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br Materials and methods br Results Estimations
2021-10-14
Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of racecadotril concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that the fract
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signal transducer and activator of transcription 6 fragment
2021-10-14
Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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We found statistically significant association between p
2021-10-14
We found statistically significant association between p95-HER2 levels and hormone receptor status, Ki-67 EZLink Sulfo-NHS-Biotin Kit and metastatic regions (p = 0.004, 0.05) and the median OS was 27.66 months versus 24.02 months for p95-HER2 positive and p95-HER2 negative BC patients respectivel
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Interestingly the virulence of HBV may adaptively
2021-10-14
Interestingly, the virulence of HBV may adaptively evolve, thus affecting the macroscopic propagation of hepatitis B. Higher virulence in vivo may result in a higher transmission rate and mortality. By assuming that the transmission rate is a monotonically increasing function of virulence, , we pro
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In summary we obtained and type of linaclotide by protein
2021-10-14
In summary, we obtained - and -type of linaclotide by protein chemical synthesis and acquired the X-ray crystal structure of linaclotide for the first time through racemic crystallization technique. The structure of linaclotide forms a compact spatial structure containing three- turns through three
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br Mutagenesis and Receptor Modeling Studies br
2021-10-14
Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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We hypothesized that modulating redox stress by altering end
2021-10-14
We hypothesized that modulating redox stress by altering endogenous antioxidant content (overexpression of catalase) and/or via dietary intervention will improve energy metabolism, adipose tissue function, and overall glucose and lipid homeostasis. To better understand the interplay between redox re
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No other lacZ mutant showed a marked difference in mutation
2021-10-14
No other lacZ mutant showed a marked difference in mutation rate between fpg and fpg backgrounds (that is, rates were comparable between HS101 and CSH1191, HS102 and CSH1192, etc.). The number of reversion mutants was much higher in HS1194 than in any other fpg strain. The inclusion of the pTRC99a p
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