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Elastase belongs to chymotrypsin family of proteases and it
2021-03-24
Elastase belongs to chymotrypsin family of proteases and it is responsible for the breakdown of elastin and other proteins, such as collagen and fibronectin, which are fundamental for the ECM elastic properties (Imokawa and Ishida, 2015). Misregulations of this enzyme are involved in skin ageing pro
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br Experimental Procedures br Acknowledgments We thank R Bri
2021-03-24
Experimental Procedures Acknowledgments We thank R. Brink for providing HEL2x, M. Tanaka for CD169DTR mice, R. Lathe for making Cyp7b1+/− mice available, and M. Barnes and A. Reboldi for comments on the manuscript. T.Y. is an Irvington Institute Postdoctoral Fellow at the Cancer Research Insti
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In the context of E ligase
2021-03-24
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 BMS
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Some family I DNA ligases can use dATP
2021-03-24
Some family I DNA ligases can use dATP as nucleotide cofactor. For instance, human Phusion high-fidelity DNA polymerase I uses dATP with a catalytic efficiency that is only 36-fold lower in comparison to ATP [9]. EhDNAlig is unable to use dATP as a nucleotide cofactor, indicating a more constrained
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Our finding that activating DDR
2021-03-24
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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Cystatins are potent inhibitors of
2021-03-24
Cystatins are potent inhibitors of cysteine proteases from the C1A family. These inhibitors primarily reduce the activities of cathepsin L-like proteases, although high concentration of barley cystatin hampers the degradation of storage proteins caused by cathepsin F-like protein (HvPap-1) (Cambra e
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Elevated production of cysLTs in asthma
2021-03-24
Elevated production of cysLTs in Ginsenoside Rd and rhinitis in general and aspirin-sensitive disease in particular10, 11, 26, 27 has been implicated in causing epithelial cell activation and excessive mucus secretion, which characterize these diseases.2, 28 It is of particular interest, therefore,
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br Acknowledgement This work was supported by grant
2021-03-23
Acknowledgement This work was supported by grant form EU (FP7 grant agreement no.: 266033 SPonge Enzyme End Cell for Innovative AppLication-SPECIAL). Introduction Prolyl 4-hydroxylases (P4Hs) have central roles in the synthesis of collagens and the regulation of oxygen homeostasis [1]. The po
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There is a large interindividual
2021-03-23
There is a large interindividual difference in intestinal cholesterol ARCA EGFP mRNA of cholesterol that is mainly due to genetic variation [15], [19]. Single nucleotide variation (SNV) in NPC1L1 and, ABCG5 and ABCG8 key modulators of cholesterol influx and efflux into intestinal mucosal cells, res
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Data from immunohistochemical detection of CIC revealed
2021-03-23
Data from immunohistochemical detection of CIC-3 revealed that the immunostaining of CIC-3 can be present both in hepatocarcinoma and its matched normal controls though; CIC-3 was, on the whole, significantly elevated in hepatocarcinoma relative to its paired normal control. In consideration of the
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br Introduction Rhabdomyosarcoma RMS is a
2021-03-23
Introduction Rhabdomyosarcoma (RMS) is a myogenic tumor that accounts for approximately 50% of all pediatric soft tissue sarcomas. Diagnostic criteria for RMS nicotinic receptor on the validation of proteins of the skeletal muscle lineage, such as Desmin, MyoD or Myogenin [1]. RMS cells are persi
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p and p which are downstream of pAkt and
2021-03-23
p21 and p16, which are downstream of pAkt and pERK1/2, are tumor suppressors which induce cell senescence and KT182 australia arrest [[56], [57], [58]]. Inhibitors of pAkt or pERK1/2 can activate p21 and p16 and promote cell senescence and cell cycle arrest [11,12,[59], [60], [61]]. It is well known
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Further modifications on the position of compound led
2021-03-23
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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On the other hand although the
2021-03-23
On the other hand, although the cardiovascular effects of Epac have been investigated more intensely in recent years [31], there are hardly any studies that suggest or discard a participation of Epac in endothelium-dependent cAMP-induced relaxation. Only our previous results in rat tankyrase inhibit
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br Materials and methods br Results and discussion br
2021-03-23
Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan
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