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Among prostaglandins PG PGD remained
2021-10-26
Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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The third generation cephalosporin antibiotics
2021-10-26
The third-generation cephalosporin CL 316243 disodium salt australia can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability
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Consistent with recent independent studies we confirm that t
2021-10-26
Consistent with recent independent studies, we confirm that the GCG-induced increase in oxygen consumption is only partially blunted in Fgf21−/− mice [32], implicating additional GCGR-dependent mechanisms contributing to the acute GCG-dependent enhancement of energy expenditure. Notably, glucagon ad
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Although in in vitro analyses GANT sensitized Daoy cells
2021-10-26
Although in in vitro analyses GANT61 sensitized Daoy Donitriptan hydrochloride to RITA treatment, this was not fully reflected in the in vivo xenograft studies in nude mice, as the combinatorial treatment elicited a comparable reduction of tumor growth. However, the dual drug administration reduced
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Two excellent GSMs with clear pharmacological
2021-10-26
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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MM-102 In this study according to the critical pharmacophore
2021-10-25
In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested
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br Introduction br Results br Discussion br
2021-10-25
Introduction Results Discussion Experimental Acknowledgment Introduction Endocannabinoids, N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) have been found in most mammalian tissues and they stimulate cannabinoid CB1 and CB2 receptor activity thereby modulating se
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In human cancers it has been
2021-10-25
In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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br The hedgehog signalling pathway The canonical Hh pathway
2021-10-25
The hedgehog signalling pathway The canonical Hh pathway is a conserved, highly complex signalling cascade, with many players and intricate regulation. However, it can be simplified into four fundamental components: i) the ligand Hh, ii) the receptor Patched (Patch [PTCH1]), iii) the signal trans
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br Mechanism of HH pathway
2021-10-25
Mechanism of HH pathway activation in NSCLC Despite the role of the HH pathway in basal cell carcinoma and medulloblastoma, it has been postulated that epithelial tumors do not demonstrate cell autonomous HH ligand activity. The main evidence comes from the study by Yauch et al showing no correla
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phosphodiesterase inhibitors These to date remain the only t
2021-10-25
These to date remain the only two reports of mutations in GC-C found in humans. Perhaps this once again emphasized the critical requirement of the presence of an optimally functional GC-C in the intestine, since neither its loss, nor its hyperactivity, can be tolerated in humans without severe conse
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Our study expands our current knowledge of Ras like small
2021-10-25
Our study expands our current knowledge of Ras-like small GTPase molecules involved in TLR-mediated responses in macrophages. We found that steady-state levels of Rap2a mRNA and protein undergo alterations after stimuli with TLR agonists. Although statistically significant, the effect of LPS-induced
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Several studies have found that GPR possesses a distinct
2021-10-25
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected influenza a virus expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141
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siRNA construction and transfection For small
2021-10-25
siRNA construction and transfection. For small interfering RNA (siRNA) experiments, we used Stealth™ select RNAi oligonucleotides targeted against GPR120 (Gibco/Invitrogen). The target sequence of siGPR120 used were; sense 5′-AAGUGGGUGCGAUUGACUUGGUCCA-3′ and antisense 5′-UGGACCAAGUCAAUCGCACCCACUU-3′
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ICH induced striatal lesion produced a reduction of EAAT exp
2021-10-25
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino tranylcypromine transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain isch
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