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Ligand selectivity may directly be
2022-02-26
Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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The repurposing of well characterized and well tolerated
2022-02-26
The repurposing of well-characterized and well-tolerated drugs in order to treat illnesses for which they were not originally intended has emerged as an attractive alternative to a long and costly process of drug development. Repositioning antihistaminergic ligands seems a promising idea given that
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Mammals have three known Gli proteins Gli and
2022-02-25
Mammals have three known Gli proteins: Gli-1, -2 and -3. Gli-1 does not undergo proteosomal degradation and hence, remains untruncated and always acts as a transcription promoter. Gli-1 is an important target gene for Gli-2. Full-length Gli-2 accumulates when Smo is activated because activated Smo p
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br Conflict of interest br Acknowledgment This work
2022-02-25
Conflict of interest Acknowledgment This work was supported by National Program on Key Basic Research Project of China (No. 2013CB127305); The National Natural Science Foundation of China (No. 314020785); Hubei Provincial Creative Team Project of Agricultural Science and Technology (No. 2007-6
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br Regulation of gonadotropins by GnRH GnRH is released
2022-02-25
Regulation of gonadotropins by GnRH GnRH is released from the hypothalamus, and its release pattern is known to be pulsatile. That is, the pulse frequency and amplitude of GnRH release vary physiologically during reproductive cycles in females, and differentially stimulate the production and rele
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Then the seven complexes GLOI indomethacin GLOI zomepirac GL
2022-02-25
Then the seven complexes (GLOI-indomethacin, GLOI-zomepirac, GLOI-fenoprofen, and GLOI-ketoprofen, GLOI-tolmetin GLOI-curcumin, and GLOI-bisdemethoxycurcumin) were energy-minimized to remove unfavorable steric strain relative to the force field adopted. Further MD simulations were carried out based
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Histamine functions as a key neurotransmitter
2022-02-25
Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, hmg-coa reductase is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling
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Consistent with recent independent studies we
2022-02-25
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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In conclusion we show to our knowledge for the first
2022-02-25
In conclusion, we show, to our knowledge for the first-time, compelling evidence for functional OTR and GHSR crosstalk, which is likely via the formation of a novel OTR/GHSR heterocomplex with important downstream signalling consequences. This OTR/GHSR interaction is poised to play an important phys
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The most ubiquitous serine threonine phosphatases such
2022-02-25
The most ubiquitous serine/threonine phosphatases, such as PP1, PP2A, and PP2B are known to contribute to the majority of phosphatase activity in the heart [4]. Dysregulation of these and other PPs have been found in numerous CVDs, including heart failure (HF), and may play a critical role in reduc
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Thus from this preliminary study a working model of
2022-02-24
Thus from this preliminary study, a working model of HIV-1 integrase was developed from which a selective inhibitor of the strand-transfer reaction displaying whole-cell activity and negligible cytotoxicity was produced. Compound 9 provides a promising scaffold for further elaboration, and current i
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The lysine K specific demethylase KDM family is comprised
2022-02-24
The lysine (K)-specific demethylase 4 (KDM4) family is comprised of 4 isoforms, KDM4A to -D, also known as JMJD2A to -D. KDM4A, B, and C encode proteins consisting of a JmjC, a JmjN, two PHD, and two Tudor domains. KDM4D is unique within the KDM4 family in that it has neither PHD nor Tudor domains,
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Glycine released from astrocytes as well as
2022-02-24
Glycine released from astrocytes as well as neurons is also known as a co-agonist of NMDAR (Roux and Supplisson, 2000). Neuronal glycine in mouse hippocampus might be released from glutamatergic terminals (Muller et al., 2013) that express functional 90 receptors (Rodriguez et al., 1997). Glycine re
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Histamine functions as a key neurotransmitter in multiple ci
2022-02-24
Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, histamine is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway
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The observed tendency for higher plasma lactate levels
2022-02-24
The observed tendency for higher plasma lactate levels in the aerated thermal exposure suggests increased reliance on PD325901 metabolism to maintain function. This finding is supported by a recent study that observed an increased ṀO2 in European perch (Perca fluviatilis) exposed to a hyperoxic rat
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