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Vortioxetine is a multimodal antidepressant that
2024-09-26
Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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Here the so called alkali assay is
2024-09-25
Here the so-called alkali assay [18] is proposed as a method to be applied directly on the purified recombinant enzyme sharing the same structural and functional features of the wild-type enzyme [19], [20], [21] using its physiological substrate androstenedione. The assay that was already successful
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Thiolutin As with most G protein coupled receptors
2024-09-25
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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Despite the absence of disulfide
2024-09-25
Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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The habit of prescribing antibiotics just in
2024-09-25
The habit of prescribing BS-181 HCl “just-in-case” there is an infection is based on the misguided perception that antibiotics are “safe” drugs and therefore pose little risk to patients. Surgeons need to dispel this myth. In the outpatient setting, antibiotic-associated ADEs account for 19% of all
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From a clinical utility standpoint this study showed that AR
2024-09-25
From a clinical utility standpoint, this study showed that AR can be useful in the GATA3-positive tumor of unknown origin setting. Epidemiologically, in this setting, the top 2 diagnoses in the differential diagnosis are metastatic carcinoma of breast origin or urothelial origin [18]. Seven out of 1
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Treatment of RAW cells with
2024-09-25
Treatment of RAW264.7 Quinidine with AP(+)-exosomes caused an increase in their phagocytic activity. In the presence of amastatin, phagocytic activity was not completely suppressed, suggesting that at least two components were responsible for the activity; one of which is aminopeptidase(s). When th
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Romidepsin br Development of lorlatinib from
2024-09-25
Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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Although several studies indicate that ALDH protects the hea
2024-09-25
Although several studies indicate that ALDH2 protects the heart from injury and maladaptive remodeling (reviewed in [11], [12], [13]), accumulating evidence indicates that deficiency of the enzyme could be protective as well. For example, mice expressing the defective Aldh2*2 mutation show lower ald
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The excellent potencies selectivities and improved PK associ
2024-09-25
The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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br Conclusion br Conflict of interest br Acknowledgments We
2024-09-25
Conclusion Conflict of interest Acknowledgments We thank Nancy Kerkvliet for helpful advice. The research in the lab of CE and THS is supported by the Deutsche Forschungsgemeinschaft (grants ES103/7-1 and 9-1, HA7346/2-1). We apologize to all authors whose work could not be cited due to lim
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In conclusion we have shown that mGlu receptors negatively
2024-09-25
In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, vx 765 tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of noradrenergic transmis
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br A Rs which were cloned and
2024-09-25
A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including KU-57788 involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R agonists produce
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br Occurrence of Inosine in
2024-09-25
Occurrence of Inosine in RNA Inosine is widespread among various types of RNAs including transfer RNA (tRNA), ribosomal RNA (rRNA), messenger RNA (mRNA), long noncoding RNA (lncRNA), and microRNA (miRNA). Within these RNAs, inosine can appear in different locations as well. Table 1 lists examples
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Epithelial mesenchymal transition EMT is the process by whic
2024-09-25
Epithelial-mesenchymal transition (EMT) is the process by which epithelial cells are trans-differentiated into motile mesenchymal cells. During EMT, epithelial cells reorganize their cortical BMS265246 cytoskeleton, lose their junctions and apical-basal polarity, change cell shape, and reprogram ge
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