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The acetylcholinesterase AChE inhibitor tacrine THA exerts n
2023-03-02
The acetylcholinesterase (AChE) inhibitor, tacrine (THA), exerts neuroprotective effects in time- and does-dependent manners against glutamate neurotoxicity (Takada-Takatori et al., 2006a, 2006b) and amyloid-β protein toxicity in PC12, a pheochromocytoma line (Wang et al., 2002; Xiao et al., 2000).
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We showed that activation of the ATM ATR pathway
2023-03-02
We showed that activation of the ATM/ATR pathway leads to over-replication through suppression of CDK1 activity, consistent with previous findings that suppression of CDK1 activity is involved in the polyploidization of megakaryocyte and trophoblast cells [36], [37], [38], [39]. Suppression of CDK1
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br Conclusion br Acknowledgments The authors
2023-03-02
Conclusion Acknowledgments The authors extend their appreciation to Kayyali Chair for Pharmaceutical Industry, Department of Pharmaceutics, College of Pharmacy, King Saud University for funding this work through the research project Number (G-2016-2). Introduction L-ornithine is a natural
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br Androgen interference with the action of arachidonic
2023-03-01
Androgen interference with the action of arachidonic hydrocort metabolites’ actions; the other side of the coin Arachidonic acid, being a polyunsaturated fatty acid present in the phospholipids of the membrane of cells, is highly abundant within the organism. It is mainly involved in cellular si
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br Conclusions In sum enhanced
2023-03-01
Conclusions In sum, enhanced incentive motivation in obesity-prone rats is mediated by NAc CP-AMPARs. These neurobehavioral differences may render obesity-susceptible populations more sensitive to the motivational influence of food cues, producing more intense, focused, “wanting” that may limit
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br Experimental Procedures br Acknowledgments We thank the m
2023-03-01
Experimental Procedures Acknowledgments We thank the members of the Qing laboratory for helpful suggestions and Biotree Biotech Co., Ltd. (Shanghai, China) for metabolomics analysis and data interpretation. This study was supported by the National Key Research and Development Program of China
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AdK as an important upstream regulator of adenosine based ho
2023-03-01
AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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The CK catalyzes the reversible conversion of creatine
2023-03-01
The CK catalyzes the reversible conversion of creatine into creatine phosphate using ATP and thereby releasing ADP. The CK isoenzymes, specifically localized in places where there is a demand and production of energy, are linked to a creatine/creatine phosphate shuttle (Wallimann et al., 1998). This
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In the late s Solvay Pharmaceuticals discontinued
2023-03-01
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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br Acknowledgment br Introduction Vascular smooth muscle cel
2023-03-01
Acknowledgment Introduction Vascular smooth muscle cells (VSMC) exhibit the capacity to switch between a differentiated (contractile) and a dedifferentiated (synthetic) phenotype [1]. Synthetic VSMC express a lower amount of contractile proteins such as Smooth muscle 22α (sm22α) and α-Smooth m
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A combination of factors might however account for
2023-03-01
A combination of factors might, however, account for the low rate of success of drug development for neuropsychiatric disorders. First, in most neuropsychiatric disorders, the symptomatology is heterogeneous and the neurobiology remains poorly understood, making therapeutic targets difficult to ide
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The structure of LO is divided
2023-03-01
The structure of 5-LO is divided in two domains, the catalytic C-terminal domain and the N-terminal regulatory C2-like domain (C2ld) [59,60]. The C2ld spans the Cy3 TSA 1-114 and is responsible for translocation and binding of calcium and membranes [61–63]. The catalytic domain is primarily an α-he
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These results from the present study are
2023-03-01
These results from the present study are summarized in Table 1. Eight drugs (doxorubicin, epirubicin, daunorubicin, idarubicin, irinotecan, imatinib, sunitinib and gefitinib) inhibited 5-HT-induced 5-HT3A and 5-HT3AB currents; three (irinotecan, topotecan and mitoxantrone) showed different responses
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IC values were obtained for an
2023-03-01
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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Receptors containing an x y
2023-02-27
Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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