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Manumycin A Several studies have found that GPR possesses a
2022-03-09
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 Manumycin A expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (
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Petrat et al could show
2022-03-09
Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c
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br Materials and methods br Results
2022-03-09
Materials and methods Results Discussion Neurotransmitter uptake is one of the most important aspects of synaptic transmission, it fact, the existence of a specific uptake system is one of the requisites that any neuroactive substance has to cover to be considered a neurotransmitter. It has
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The effect of GCK NES mutations
2022-03-09
The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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br Introduction HH GLI signaling
2022-03-09
Introduction HH-GLI signaling is one of the major pathways involved in both normal and neoplastic development [[1], [2], [3], [4]]. Inappropriate activation of this pathway has been linked to cancer, including medulloblastoma, rhabdomyosarcoma, basal cell carcinoma and cancers of the lung, stomac
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br Acknowledgments We apologize for
2022-03-09
Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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The primary or in transit site of
2022-03-09
The primary or in-transit site of metastasis for many cancers, including melanoma, are nearby sentinel lymph nodes (LNs) [6]. As such, sentinel LN biopsy is a common procedure to diagnose and stage melanoma progression [7,8]. Sentinel LNs are often the primary site of metastasis due to tumor cell-st
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To date the crystal structures of HIV IN
2022-03-09
To date, the crystal structures of HIV-1 IN complexed with ligands and related proteins could help us in studying the interactions between the inhibitors and IN. Until now, 114 co-crystal structures of HIV-1 IN with small molecular ligands 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34,
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In an effort to further improve the
2022-03-08
In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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Introduction Hepatitis C virus HCV is a small
2022-03-08
Introduction Hepatitis C virus (HCV) is a small (50–80 nm in size) enveloped RNA virus belonging to the Hepacivirus genus of the Flaviviridae family [1]. The HCV particle consists of a nucleocapsid, which contains the positive single-stranded RNA genome covered by a host cell-derived lipid envelope
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br Conclusion br Disclosure of interest br Acknowledgement
2022-03-08
Conclusion Disclosure of interest Acknowledgement Introduction Vitamin B6 has long been recognized as a cofactor for many enzymes, especially those involved in amino A-54556A metabolism. Apart from its role as coenzyme, recent studies are unveiling a new role of vitamin B6 as a chemopre
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We have shown previously that activation of the TGF Smad
2022-03-08
We have shown previously that activation of the TGFβ/Smad signaling pathway in keratinocytes regulates liothyronine sodium mg cytoskeleton organization via non-genomic and genomic mechanisms and that RhoB gene is a target of Smad proteins [12,13]. Although the role of RhoB in early non-genomic TGFβ
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GPR co localizes with ghrelin in the
2022-03-08
GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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br Material and methods br Results Consistent with
2022-03-08
Material and methods Results Consistent with our previous study, SR-SIM and confocal microscopy showed a large number of IBA1-expressing p450 inhibitors in all parts of the human cochleae (Fig. 1). IBA1, the microglial and macrophage-specific calcium-binding protein, is involved in the membra
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Trypanosomatid GLO enzymes are monomeric and contain a
2022-03-08
Trypanosomatid GLO2 enzymes are monomeric and contain a zinc–iron binuclear metal center (Irsch and Krauth-Siegel, 2004, Silva et al., 2008), similar to all other glyoxalases II. As mentioned, in T. brucei there are two GLO2 genes but only one encodes an enzyme with glyoxalase II activity (Irsch and
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