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Oltipraz has been shown to inhibit the growth of
2022-02-08

Oltipraz has been shown to inhibit the growth of HCC VEGFR Tyrosine Kinase Inhibitor II and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver
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AGK7 Substrate affinity and specificity can
2022-02-08

Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of AGK7 bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of short lin
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br Intracellular trafficking with concurrent signaling
2022-02-08

Intracellular trafficking with concurrent signaling of NPRA Our recent studies have shown internalization and concurrent signaling of NPRA in subcellular compartments; this had not been previously demonstrated [26,42]. Preparation of the enhanced GFP (eGFP)-tagged NPRA (eGFP-NPRA) construct has g
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br Role of dynamin in NPRA
2022-02-08

Role of dynamin in NPRA endocytosis In recent studies using 125I-ANP binding assay and confocal microscopy, we have examined the role of dynamin in the internalization and trafficking of NPRA in a stably transfected HEK-293 KU60019 [69]. Our findings indicated that ANP treatment of high-density N
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R547 There is abundant literature about different functional
2022-02-08

There is abundant literature about different functional aspects of the cannabinoid system (Badal et al., 2017, Balenga et al., 2011, Henderson-Redmond et al., 2016, Nair et al., 2015); however, not a great deal is known about the mechanism by which ethanol impacts its function in connection to the i
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Although it is currently unknown
2022-02-08

Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the Dioscin receptor splice variant ERbeta2 identified in human and primate, but not other species (Sierens, e
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br Conclusions br Acknowledgements The authors thank Matt JM
2022-02-08

Conclusions Acknowledgements The authors thank Matt JM Wood and colleagues (AstraZeneca, UK) for permission to use logD and protein binding data presented in Sup. Table S2. Introduction The number of people suffering from type 2 diabetes mellitus (T2DM) has escalated worldwide as a consequ
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br Introduction Major depressive disorder MDD
2022-02-07

Introduction Major depressive disorder (MDD) is a disease with poorly recognized etiology. Currently used antidepressant drugs, which mainly affect synaptic neurotransmitter levels, show full clinical efficacy in only one third of patients (Rush, 2007). Thus it is now generally accepted that the
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In addition we assessed the viability of
2022-02-07

In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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br Acknowledgments We apologize to the researchers who were
2022-02-07

Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Christine Heiner (Department of Surgery, University of Pittsburgh) for her critical reading of the manuscript. This work was supported by grants from the US National Institutes of Health (R0
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Despite the importance of intratumor phenotypic heterogeneit
2022-02-05

Despite the importance of intratumor phenotypic heterogeneity for tumor progression and therapy resistance (Marusyk et al., 2012, Marusyk and Polyak, 2010), our understanding of regulators of this process and our ability to modulate them are very limited. Recent advances in genomic sequencing and si
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Acetylation of histones by histone acetyltransferases stimul
2022-02-05

Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing Chidamide structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Recent studies
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In the same research group
2022-02-05

In 2017, the same research group released a free internet accessible database (HemeOxDB, http://www.researchdsf.unict.it/hemeoxdb), to make it easier the analysis of the literature and, consequently, the design of potent and selective HO-1 inhibitors. The database reported the entire set of HO-1 and
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To solve the atomic structures of several
2022-02-05

To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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Additionally increased GLO gene expression
2022-02-04

Additionally, increased GLO1 gene expression, protein expression, and activity have been reported in a variety of cancers, including breast,22, 23, 24 pancreatic, melanoma, and prostate.27, 28, 29 Vince and Daluge proposed that inhibitors of GLO1 could serve as anti-tumor agents, by increasing conce
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