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An alternative to the agonist or antagonist
2024-02-02
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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The first rationally designed dual mPGES LO inhibitor
2024-02-02
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic NG,NG-dimethyl-L-Arginine hydrochloride mg - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substitut
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The consensus amino acid recognition sequence
2024-02-02
The consensus amino 6 ohda synthesis recognition sequence for p38α substrates is (Ser/Thr)Pro (Cuadrado and Nebreda, 2010), typically assisted by upstream docking motifs (Remenyi et al, 2005, Sharrocks et al, 2000). P450c17 has 32 Ser and 25 Thr residues, of which only Thr 341 and Ser 427 are immed
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Herein we disclose novel dihydropyrano
2024-02-02
Herein, we disclose novel 2,4-dihydropyrano[2,3-c]pyrazoles that inhibit human ATX (hATX). Our results demonstrate and further support previous findings showing that a desired biological action can be achieved without targeting the catalytic site of the enzyme. Moreover, this study validated hen egg
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Among steroid saponins ginsenosides are the active
2024-02-02
Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid
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br Experimental br Acknowledgment This paper was financially
2024-02-02
Experimental Acknowledgment This paper was financially supported by the Project Funded by China Postdoctoral Science Foundation (2017T100186), Natural Science Foundation of Liaoning Province (20170540858), General Scientific Research Projects of Department of Education of Liaoning Province (20
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Thiazole heterocycles constitute an interesting class of mol
2024-02-02
Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.
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Introduction Antimicrobial resistance is a growing health th
2024-02-02
Introduction Antimicrobial resistance is a growing health threat worldwide that has been associated with incorrect prescription and overuse of 22 9 [1]. Considering that physicians play a central role in antibiotic usage, a better understanding of their prescribing behaviours and their knowledge o
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N terminally extended antigenic peptide
2024-02-01
N-terminally extended antigenic peptide precursors that survive cytosolic degradation and enter the ER, need to be further processed by ERAP1 and/or ERAP2, in order to acquire the right length required for MHCI binding. ERAP1 (ERAAP in mouse) is an IFN-γ-inducible, metalloaminopeptidase that trims N
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gaba receptors The number of times an animal reared was the
2024-02-01
The number of times an animal reared was the only emotional behavior that was significantly higher in the young mice than in the middle-aged group. This may be explained by diminished curiosity or augmented ambulation with aging (Lalonde and Strazielle, 2008). A recent study showed that middle-aged
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For hippocampal asymmetry two SNPs rs
2024-02-01
For hippocampal asymmetry, two SNPs (rs1476679 and rs4147929) showed significant interaction with diagnosis. They have an inverse effect on asymmetry, which is consistent with their different roles as preventative or risk loci in AD. rs1476679 is intronic in the ZCWPW1 gene, is a histone modificatio
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The application of diuretics induce an
2024-02-01
The application of diuretics induce an increased rate of water exiting brain cells encouraging the formation of increased intracellular polyphosphoric acid. In the absence of the diuretic water is retained in cells converting polyphosphoric SCH772984 to monophosphoric acid. The latter change decrea
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Aberrant lipid levels are associated
2024-02-01
Aberrant lipid levels are associated with various disorders, including vascular diseases and diabetes. Furthermore, important events support the idea that lipids, especially cholesterol and its derivatives, have a fundamental role in the physiopathology of AD. The eif2a is rich in cholesterol, and
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br Potential and established risk factor for Alzheimer s
2024-02-01
Potential and established risk factor for Alzheimer’s Disease The only way to overcome the above mentioned limitations is the identification of risk factors, which, taken together, can reliable predict the development of AD. Age and ApoE4 are established non-modifiable risk factors for AD. The ri
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We now present a series of
2024-02-01
We now present a series of findings obtained in heterologous expression systems, brain slices, and living animals that suggest that any interaction between mGlu7 and α1-adrenergic receptors exists, is specific, and is physiologically and behaviourally relevant. Materials and methods Norepinephri
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