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NLX a k a F or befiradol exhibits
2023-12-14
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in pergolide to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has
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In brief serotonin can interact
2023-12-14
In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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Introduction hydroxytryptamine HT is found throughout the bo
2023-12-14
Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary I-BET-762 (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current classifica
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Adenosine receptors activate a number of signalling pathways
2023-12-14
Adenosine receptors activate a number of signalling pathways involved in tissue survival including several mitogen-activated protein kinases (Fredholm et al., 2001). The common feature of all adenosine receptors is the positive coupling to ERK1/2, whilst A2B and A3 receptors can also activate the st
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br Actin at presynapses br Conclusion Thanks to the
2023-12-14
Actin at presynapses Conclusion Thanks to the recent discovery of rings, hotspots and trails, axonal vistusertib is back in the spotlight. These are exiting times for neuronal cell biologists armed with constantly improving labeling and imaging techniques to observe, quantify and perturb thes
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jsh Both subcutaneous s c and mucosal administration of s ht
2023-12-14
Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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br Acknowledgments This work was supported
2023-12-14
Acknowledgments This work was supported by the R&D Program of the Institutional Research Program of KRICT (SI1701-02), and by the Next generation carbon upcycling project of Ministry of Science and ICT. JSC is kindly grateful to the National Research Council of Science and Technology (NST) for fi
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ACh induced changes in respiratory frequency could be
2023-12-14
ACh-induced changes in respiratory frequency could be of interest. They may reveal an important mechanism of respiratory modulation at the caudal NTS level. ACh-induced increases in respiratory frequency within this region have been also reported by Furuya et al. (2014). Changes in respiratory timin
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br Conclusion br Conflicts of
2023-12-14
Conclusion Conflicts of interest Introduction RNA interference is a specific post-transcriptional gene silencing mechanism within a cell via the transfection of microRNAs (miRNA), exogenous small interfering RNAs (siRNA) or small hairpin RNAs (shRNA) [1–3]. Transfection of shRNA can be done
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Autotaxin has been linked to chemoresistance through its abi
2023-12-14
Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer dapivirine australia [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-express
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The molecular mechanisms involved in the pathogenesis
2023-12-14
The molecular mechanisms involved in the pathogenesis of cholestatic pruritus remain unknown [45], [46]. Indeed, there has been an enormous effort at understanding the etiology of PBC-related pruritus, including work at the cellular and molecular level, but such efforts have not been translated into
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Several approved and or experimental drugs together with nat
2023-12-13
Several approved and/or experimental drugs, together with natural compounds, have been reported to induce autophagy in different cancer types [70], [71], [72] (Table 1). In the next paragraphs, we will review more in detail a group of these agents selected in relation to their promising future outco
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PF also a dual Aurora A and Aurora B inhibitor
2023-12-13
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly hydralazine hydrochloride for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule t
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Ryoichi et al modified potent clinical candidate VX with cya
2023-12-13
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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The tumor suppressor function of LOX in normal prostate
2023-12-13
The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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