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On the other hand imidazolylcyclopropane derivatives and hav
2021-09-26
On the other hand, imidazolylcyclopropane derivatives and having a 2-substituted benzimidazolyl group showed moderate binding affinities for both the HR and HR. Replacement of 4-chlororbenzylamino group of with a benzimidazolyl group () led to increase the affinity for the HR more than 5-fold ( =
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abiraterone acetate In this current study we not only demons
2021-09-26
In this current study, we not only demonstrated the growth-inhibitory effects of the 2nd generation analog SL-1-39 on the HER2+ breast cancer cells, MDA-MB-453 and SKBR3 (Table 1), but we also demonstrated that the decrease in cell number was associated with an interruption of abiraterone acetate pr
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In addition to these effects on
2021-09-24
In addition to these effects on metabolic function in cardiac cells, this study also demonstrates changes in the expression of hypertrophic genes and proteins subsequent to GPR119 activation. Again this occurred in a distinct pattern dependent on palmitate exposure. Of interest SOCS3 mRNAs were decr
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The rat model was validated with another
2021-09-24
The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L
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br Introduction The amino acid glycine functions as a neurot
2021-09-24
Introduction The amino apexbt kinase inhibitor glycine functions as a neurotransmitter in the vertebrate central nervous system: as an inhibitory neurotransmitter and as a co-agonist of the NMDA-subtype of excitatory glutamatergic receptors (Eulenburg et al., 2005). Under a current hypothesis th
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In order to test the
2021-09-24
In order to test the influence of the initial depolarization, experiments were performed, where the degree of chloride substitution was varied, either by adding n-Ringer to histamine-1 receptor antagonist incubated in a sucrose Ringer or by suspending the cells directly in Ringers identical to the
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br Hydroxyfarnesyl diphosphate was synthesised in three
2021-09-24
12-Hydroxyfarnesyl diphosphate (6) was synthesised in three steps starting from commercially available (E,E)-farnesol (10) (Scheme 5). Chlorination of 10 gave farnesyl chloride (11) in a quantitative yield, which was carried forward without purification. The following step was a selenium dioxide-c
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br Funding The research for this paper is conducted as
2021-09-24
Funding The research for this paper is conducted as part of a PhD thesis at Pasteur Institute of Iran and it was financially supported by Pasteur Institute of Iran and the Iranian Centre for Communicable Diseases. Conflict of interest Acknowledgments Introduction The viral enzyme integr
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The structures of KDM A revealed
2021-09-24
The structures of KDM4A revealed a Cys-His Zn(II) binding site that is close to the substrate binding spot, which bioinformatic analyses indicated was not present in any other histone demethylase subfamily. Therefore, an alternative method to inhibit the KDM4 family (95) would be to use compounds th
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The first wave of cells infiltrating heart shortly after MI
2021-09-23
The first wave of aristocort infiltrating heart shortly after MI is composed mainly of neutrophils, with the highest number on the first day after ischemic episode [101]. These cells are recruited via C-X-C motif chemokine ligand-2 (CXCL-2)- and CXCL-5-mediated chemotaxis. Both chemokines are produ
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Our aim was to gain insight
2021-09-23
Our aim was to gain insight into mechanisms that underlie the contribution of thrombospondin-1 (TSP1) to progression of CKD. TSP1 is the most-studied member of the thrombospondin family of matricellular proteins. Previous studies have demonstrated that pharmacological suppression or genetic depletio
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In order to elucidate the mechanisms behind the observed cha
2021-09-23
In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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In recent years several DPP IV inhibitors have
2021-09-23
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic interleukins with a unique xanthine scaffold developed through high-throu
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br Introduction High dose niacin or
2021-09-23
Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic ARM1 form of niacin modulates plasma lipid profiles including decreasing circulating
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gsk3 inhibitor CF patients can suffer from a
2021-09-23
CF patients can suffer from a multitude of hepatobiliary problems including gall stones, hepatitis, steatosis and cirrhosis. Hepatobiliary problems are common in pediatric CF patients with reported prevalence rates up to 25% [12,13]. Cystic fibrosis related liver disease (CFLD) was thought to develo
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