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br Disclosure statement br Acknowledgment
2019-09-10
Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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br Introduction Hydrogen sulfide H S and nitric
2019-09-10
Introduction Hydrogen sulfide (H2S) and nitric oxide (NO) are important gasotransmitters in the cardiovascular system and instrumental to the fine control of vascular tone [1] and cellular function [2]. NO is synthesized from l-arginine by calmodulin-dependent endothelial nitric oxide synthase (e
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It is particularly notable that CYP D appears to
2019-09-10
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 ICI 118,551 hydrochloride in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time
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br Results br Discussion Our UbV library was originally desi
2019-09-10
Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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br Results and discussion br Conclusion In the current
2019-09-10
Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I
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br Conflict of interest br Acknowledgments This work was
2019-09-09
Conflict of interest Acknowledgments This work was supported in part by grants from the , Spain (INCITE08PXIB203092PR). VGM was supported by a FPU pre-doctoral scholarship from the , Spain. MLR was supported in part by a crowdfunding campaign (PRECIPITA), coordinated by the Spanish Foundation
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Apparently no study has been undertaken on alterations in
2019-09-09
Apparently, no study has been undertaken on alterations in cholinesterase activity and its correlation with neurological disorders in clinical case of trypanosomosis in buffaloes. Therefore, the present study was undertaken to evaluate the alterations in cholinesterase activity in clinical cases of
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α-Cyperone mass br Acknowledgements br Introduction Endothel
2019-09-09
Acknowledgements Introduction Endothelial α-Cyperone mass constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile role
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br Perspective and conclusion Collagen
2019-09-09
Perspective and conclusion Collagen Toolkits II and III have been used to determine the IKK-16 and for DDR1 and DDR2, and the main binding site is the GVM-GFO motif [103,108]. The co-crystal structure of the DS domain of human DDR2 bound to a synthetic collagen-like peptide containing the GVM-GFO
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AMG-458 Proof of concept studies with disulfiram suggest
2019-09-09
Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d
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br Experimental Procedures br Acknowledgments The authors wi
2019-09-09
Experimental Procedures Acknowledgments The authors wish to thank P. Costet (University of Bordeaux) and Véronique Guyonnet-Duperat (FR TransBioMed, Plateforme de Vectorologie, University of Bordeaux) and Prof. Nils-Göran Larsson and Dr. Bettina Bertalan (Max Planck Institute for Biology of Ag
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br Application of the screening system for
2019-09-09
Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human BAY 80-6946 because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or a pro
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In our preliminary evaluation of this series we were
2019-09-09
In our preliminary evaluation of this series, we were surprised to discover that Doripenem and was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is compared wit
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Functional studies revealed that these
2019-09-09
Functional studies revealed that these ESR1 mutations lead to constitutive activity of the ER, meaning that the receptor is active in absence of estrogen, conferring resistance against several endocrine agents. Recent studies reported that the occurrence of ESR1 mutations is rare in ER+ primary brea
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In recent years there has been
2019-09-07
In recent years there has been a dramatic increase in identification and optimization of potent CRTh2 antagonists which may not only inhibit the recruitment and activation of Th2 cells but also accelerate apoptosis and clearance of these cells from inflamed tissue, thereby promoting the resolution o
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