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One important discovery of our study is the identification o
2021-12-15
One important discovery of our study is the identification of a pharmacological mechanism for the macrolide antibiotic erythromycin (EM) in promoting joint health. EM is a commonly used antibiotic that directly binds bacterial ribosomes to inhibit protein synthesis [66]. Although EM-like macrolide A
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Enhancer of zeste homolog EZH which functions
2021-12-14
Enhancer of zeste homolog 2 (EZH2), which functions as a methyltransferase, is a critical subunit of polycomb repressive complex 2 (PRC2), which has been demonstrated to be involved in the development of the MI-773 [23]. Aberrant expression of EZH2 has been found to be associated with a variety of
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br Financial support This study was supported by Grant PH
2021-12-14
Financial support This study was supported by Grant PH-102-PP-11, PH-103-PP-11 from the National Health Research Institutes, Taiwan. Conflict of interest Please refer to the accompanying ICMJE disclosure forms for further details. Authors’ contributions Acknowledgements Introduction
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br GSK Glycogen synthase kinase GSK
2021-12-14
GSK-3 Glycogen synthase kinase-3 (GSK-3) is a ubiquitous serine/threonine kinase that is involved in multiple signaling pathways that are crucial for cellular metabolism and proliferation (Doble and Woodgett, 2003, Frame and Cohen, 2001, Grimes and Jope, 2001, Woodgett, 1990). GSK-3 is known to d
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In three independent groups identified GPR A HM
2021-12-14
In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niac
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PTMs have been shown to influence transporter kinetics both
2021-12-14
PTMs have been shown to influence transporter kinetics, both directly and indirectly (Xu & You, 2017). They do not just regulate the innate structure-function relationship driven by a transporter's global architecture, but rather are also able to regulate this relationship down to the resolution of
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Among the various delivery strategies in the
2021-12-14
Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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br Vesicular glutamate transporters VGLUTs br Conclusions Du
2021-12-14
Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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br Discussion In the present study we have demonstrated the
2021-12-14
Discussion In the present study, we have demonstrated the effect of a high-fat diet upon wild-type and glut3 pregestational female phenotype and shown that it leads to obesity due to an increase in white adipose tissue contributing to the overall fat mass. Despite this observed obesity along with
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Structurally the termini of FGF are critical for
2021-12-14
Structurally, the termini of FGF21 are critical for effective signaling. Progressive amino XL413 hydrochloride receptor truncation at either end of the protein sequentially impairs FGF21 bioactivity, but via different mechanisms. Shortening at the N-terminus weakens its ability to activate the FGFR
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In conclusion a novel series of GPR
2021-12-14
In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen d-cycloserine had a remarkable effect on the GPR40 agonistic activi
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br Concluding Remarks One of the remarkable features of
2021-12-13
Concluding Remarks One of the remarkable features of Hippo signaling is its sensitivity to the cytoskeleton and mechanical forces. Progress has been made recently in identifying molecular mechanisms by which the cytoskeleton can influence Hippo signaling, but among the many outstanding questions
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Interestingly the rabbit cornea exhibited a
2021-12-13
Interestingly, the rabbit cornea exhibited a more than two-fold higher level of total GST activity compared with that of the porcine cornea, whereas their levels of GSTO1‐1 and GSTP1‐1 activity were similar (Fig. 4). Because members of the GST Alpha, Mu, Pi and Omega 3-Deazaadenosine receptor prima
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Lipid sensing GPCRs as therapeutic
2021-12-13
Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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In recent years several DPP IV inhibitors have
2021-12-13
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic Dihydrodaidzein with a unique xanthine scaffold developed through high-th
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