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hydroxydopamine OHDA is a selective
2023-10-08
6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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While the direct effects of ARI lead to
2023-10-08
While the direct effects of 5-ARI lead to a dramatic OTX-015 in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal laboratory range [
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Loss of expression or functional activity of cell
2023-10-08
Loss of expression or functional activity of cell adhesion is intricately related to advanced stages of tumour progression and invasiveness. Martin-Belmonte and Perez-Moreno recently mentioned that the deregulation of adhesion can alter tumourgenesis in the early stage. We have shown for the first t
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It has also been reported that defects
2023-10-08
It has also been reported that defects in ATM or ATR signalling are synthetically lethal with PARP inhibition (Turner et al., 2008, Peasland et al., 2011, Yap et al., 2011, Michels et al., 2014), suggesting that combined inhibition of PARP and ATM or ATR may be an effective therapeutic strategy. In
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In order to further explore whether
2023-10-08
In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 BIBR 953 sale is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD activity. A large b
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br HMGB proteins and chromatin structure The
2023-10-08
HMGB proteins and chromatin structure The multifaceted roles played by HMGB (formerly called HMG-1 and -2) proteins in modulating chromatin structure, gene transcriptional activity and cellular phenotype have been covered in a number of recent reviews and readers are referred to these for in-dept
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Erteberel mg Several combination studies have been performed
2023-10-08
Several combination studies have been performed using animal models of mucormycosis, principally involving R. arrhizus. In two investigations using diabetic and/or neutropenic mice, a combination of a polyene with an echinocandin was shown to improve survival compared with monotherapies [25], [34].
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Angiogenesis refers to the formation of
2023-10-08
Angiogenesis refers to the formation of new blood vessels from pre-existing vasculature [1]. Physiological angiogenesis is necessary for key processes such as wound healing, tissue regeneration and repair. In pathological conditions, including cardiovascular diseases, diabetes, cancer, and other pat
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br Concluding remarks Enhanced membrane
2023-10-08
Concluding remarks Enhanced membrane binding upon calcium stimulation in GW9662 suggests a pre-requisite step that involves a conformational change in LOX. This might facilitate it to tether to the membrane and regulate enzyme activity. The calcium binding loops and the putative active site entr
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br Acknowledgements Dr Paul J Gasser is supported
2023-10-07
Acknowledgements Dr. Paul J. Gasser is supported by the National Institutes of Health (grant number R01DA032895), and the Charles E. Kubly Mental Health Research Center. Dr. Christopher A. Lowry is supported by the National Institutes of Health (grant number R21 MH116263), the Department of the N
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Fluconazole br Material and methods br Results br
2023-10-07
Material and methods Results Discussion GRK2 activity has increasingly been shown to contribute to the progression of numerous diseases and organ dysfunction [5], [6]. For instance, a large body of work over the last two decades has identified GRK2 as a major regulator of cardiac dysfunctio
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The activation of the A BR subtype
2023-10-07
The activation of the A2BR subtype triggers different intracellular metabolic pathways, often linked to the activation of adenylyl cyclase and increased levels of intracellular cAMP (Lynge et al., 2003, Bernareggi et al., 2015). The nAChR-channel xanthine oxidase mediated by the cAMP/PKA pathway wa
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In the late s Solvay Pharmaceuticals discontinued the
2023-10-07
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Tacrine an aminoacridine derivative Fig A
2023-10-07
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Since the localization of LO depends
2023-10-07
Since the localization of 5-LO depends on phosphorylation, we also analyzed the phosphorylation profile of 5-LO-WT and all isoforms by Western blot using specific 9292 against the phosphorylation sites S271 and S523. Whereas phosphorylation at S271 activates the 5-LO, inhibits nuclear export and le
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