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Various compounds have been designed to inhibit aldose reduc
2023-10-12

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic Gentamycin Sulfate moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to
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The second evidence comes from the results obtained by patch
2023-10-12

The second evidence comes from the results obtained by patch-clamp recordings carried out at the endplate region of isolated mouse FDB fibers, where adenosine and the P1R agonist NECA significantly affected the NPo, the open frequency and the time constant τ of the adult nAChR channels. It is genera
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br Methods br Results From a
2023-10-12

Methods Results From a study population of 7069 patients, a total of 149 falls were reported during the study NT157 for an incidence rate (IR) of 5.2 falls per 1000 patient-days (PD), 95% confidence interval (CI) 4.4/1000 PD–6.1/1000 PD. The incidence rate ratio (IRR) for patients in the ACE u
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br Co http www apexbt com media
2023-10-12

Conclusions This paper is the first meta-analysis about the association between SRD5A2 V89L polymorphism and hypospadias risk. The results of this meta-analysis have revealed that V89L polymorphism definitely increases the risk of hypospadias, and the C allele is a genetic risk factor for hypospa
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We have previously shown that
2023-10-12

We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific Bialaphos sodium salt blockade or activation (Rojas-Corrales et al., 2000).
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Derivatives of M that possess either
2023-10-12

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these N-acetyl D-galactosamine mg to maintain 5-HTR antagonist properties as (+)-M100
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The identification of novel kinase
2023-10-11

The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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The phylogenetic relationship demonstrates that both bovine
2023-10-11

The phylogenetic relationship demonstrates that both bovine and porcine 12/15-LO is more related to the human enzyme than the rabbit enzyme, despite the fact that the rabbit reticulocyte enzyme is a 15-lipoxygenase. The rabbit is one single species that expresses a 12/15 LO with 15-LO activity while
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Introduction Lipoxygenases LOXs are key enzymes that catalyz
2023-10-11

Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic 98059 (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (Claesson, 2009).
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br Experimental protocols br Results and discussion
2023-10-11

Experimental protocols Results and discussion Conclusion 15-LOX-1 is an important mammalian lipoxygenase which plays an important role in the biosynthesis of leukotrienes, lipoxins and other signalling molecules. These signalling molecules play a regulatory role in several respiratory disea
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In this review we will present the traditional
2023-10-11

In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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However most of these SBVS studies
2023-10-11

However, most of these SBVS studies were focused on the target(s) for which crystal structures were available or have a similar template in PDB for comparative modeling. Besides, these were limited to SBVS only which relies on the rigid binding pocket, therefore, it may result in high false positive
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Thymoquinone TQ is the major active compound derived from
2023-10-11

Thymoquinone (TQ) is the major active myc pathway derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et al.,
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Cyclophosphamide receptor Gene regulation of MMPs is influen
2023-10-11

Gene regulation of MMPs is influenced by the transcription factor activating factor-1 (AP-1). AP-1 complexes are heterodimers of proteins of the two proto-oncogene families (jun and fos) and have Cyclophosphamide receptor in the promoter region of MMPs, as well as in genes mediating inflammatory re
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Most human diseases e g cancer
2023-10-11

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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