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The cellular mechanism underlying the CGS mediated inhibitio
2022-11-16
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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Additionally regulation of GPCR heteromerization by specific
2022-11-16
Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribu
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The role of DHT in early teleost
2022-11-16
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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The benzimidazole group seems to be
2022-11-16
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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We used the lead compound C to
2022-11-14
We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system. E
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br Conflict of interest statement
2022-11-14
Conflict of interest statement Acknowledgments Introduction Cellular responses to genotoxic stress in eukaryotic cells are coordinated by members of the phosphoinositide kinase related protein kinase (PIKK) family. Two members of this family, Ataxia–Telangiectasia mutated (ATM) and ATM and
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The apoptosis promoting Bcl family includes BH
2022-11-14
The apoptosis-promoting Bcl-2 family includes BH3-only proteins (e.g., Bim, Bid and Bad) and multiple-domain proteins (e.g., Bax and Bak). At the time of apoptosis stimulation (e.g., DNA damage), only the BH3-only protein is activated, directly or indirectly promoting Bax/Bak oligomerization, changi
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Mechanistically it was soon realized that in undead cells Dr
2022-11-14
Mechanistically, it was soon realized that in undead cells, Dronc promotes the activation of Jun-N-terminal kinase (JNK) signaling as the major inducer of AiP [25], [28] (Fig. 2B,C). However, it has been unknown for a long time how active Dronc promotes JNK signaling. Recently, it was reported that
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br Experimental and computation Standard samples of artemisi
2022-11-14
Experimental and computation Standard samples of artemisinin (1) and artemether (2) were purchased from China National Institutes for Food and Drug Control. Their ECD spectra, at a concentration of 1.0–5.0mg/mL in ethanol, were recorded in a quartz cuvette of 1mm optical path length using a Jasco
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br Materials and methods br Results br
2022-11-11
Materials and methods Results Discussion Endophilin A1 is a membrane-binding protein that is mainly distributed in the central nervous system (Giachino et al., 1997), localizes in the dendritic shafts and spines of mature neurons (Yang et al., 2015), and relates to the function and morpholo
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ONC201 Consideration of the rate of product formation
2022-11-11
Consideration of the rate of product formation at different substrate concentrations and estimation of Michaelis-Menten parameters gives some insight into the possible mechanisms underlying the observed decreases in enzyme activity. Estimates based on two-substrate concentrations lack precision and
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Both AD and dyslipidemias are global public health problems
2022-11-11
Both AD and dyslipidemias are global public health problems, and an increase in their incidence over the next decades is expected. Among many triggering elements, the increase in life expectancy is one of the main risk factors associated with the increase in the incidence of AD. Meanwhile, dyslipide
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Activation of AhR is also known to upregulate
2022-11-10
Activation of AhR is also known to upregulate the expression of AhRR (AhR repressor), an inhibitor protein of AhR [29]. However, the exact mechanism by which AhRR represses AhR signaling is not well understood. The initial study by Mimura and colleagues suggested that AhRR is capable of directly com
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Deferiprone As described in the introductory section the
2022-11-09
As described in the introductory section, the rotifer nervous system would be capable to transmit Deferiprone in throughout its neural pathways. In addition, Clément and Amsellem (1989) and Kotikova et al. (2001) suggested acetylcholine to be important for the functioning of rotifer muscles and thei
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Molecular docking is widely used to predict the interaction
2022-11-09
Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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