• PKA signalling in the nucleus was thought to be due

  2021-03-24

  

  PKA signalling in the nucleus was thought to be due to the translocation of the catalytic subunit upon activation from the SP 141 to the nucleus via diffusion [72]. However, a new understanding has emerged, as both the regulatory and catalytic subunits have been identified in the nucleus and functio

• br Materials and methods br Results and discussion br Conclu

  2021-03-24

  

  Materials and methods Results and discussion Conclusions Data about the ability of non-conventional ligands to operate class-A GPCRs have been accumulating. Specifically, increasing evidence indicates that oxysterols, oxidized derivatives of cholesterol, are involved in many activities that

• Quinacrine hydrochloride hydrate sale In another study Nutli

  2021-03-24

  

  In another study, Nutlin-3a-mediated p53 activation induced strong negative impact on NF-κB signaling in LPS-stimulated neutrophils and macrophages [34]. Nutlin-3a limited cellular immune response to LPS, partly by attenuating DNA binding activity of NF-κB and impairing transcription of its target c

• br Results and discussion br Conclusion We have constructed

  2021-03-24

  

  Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz

• br Authors contributions br Acknowledgements br Introduction

  2021-03-24

  

  Authors’ contributions Acknowledgements Introduction Retinoic Luciferase Reporter Assay Kit receptor is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic aci

• The three dimensional crystal structure of Ca

  2021-03-24

  

  The three-dimensional crystal structure of Ca2+ loaded CaM reveals a dumbbell-shaped molecule with two roughly globular lobes, the N- and C-terminal lobes linked by a long solvent-exposed helix, which has been shown by NMR to be non-helical in its central part and flexible in solution [13]. Each glo

• p Kip is a critical component of the

  2021-03-24

  

  p27Kip1 is a critical component of the cell cycle machinery [15]. As an inhibitor of cyclin E-Cdk2, p27Kip1 plays a pivotal role in controlling cell proliferation, S-phase entry, and G1-phase exit during development and tumorigenesis [16]. p27Kip1 is predominantly regulated via posttranslational mod

• CK comprises a family of serine threonine protein

  2021-03-23

  

  CK1 comprises a family of serine/threonine protein kinases, that includes different CK1 isoforms namely α, β, δ, ε and γ their various splice variants [56]. It was reported that the pharmacological inhibitor IC261 shows an order of magnitude of higher selectivity for CK1δ or CK1ε isoforms (IC50 of 1

• never ET expression occurs in many carcinomas including thos

  2021-03-23

  

  ET-1 expression occurs in many carcinomas, including those arising in the kidney [38], prostate [7], ovary [5] endometrium [39], melanocyte [40], and central nervous system [41], [42], among others [43]. The endothelin axis expression in RCC appears to be dependent upon the tumor subtype [38]. In se

• Considering these reports and with

  2021-03-23

  

  Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b

• Compounds and possessed relatively low clogP values and

  2021-03-23

  

  Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.

• Nitrid oxide NO and its

  2021-03-23

  

  Nitrid oxide (NO) and its potential endogenous production as an endothelium-derived factor was the first gaseous molecule accepted to be a signaling mediator in the organism [4,5]. NO plays a key role in physiological regulation of the 5 aminolevulinic acid receptor and exerts physiological functio

• prostaglandin e CYP A and CYP D are among

  2021-03-23

  

  CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i

• Recent studies have also uncovered

  2021-03-23

  

  Recent studies have also uncovered additional roles for E2 enzymes and E2~Ub conjugates in modulating the activity of deubiquitinating enzymes (DUBs), such as OTUB1 (Juang et al., 2012, Wiener et al., 2013, Wiener et al., 2012). Interestingly, OTUB1 has also been shown to associate and modulate the

• Main Text Post translational modifications by ubiquitin Ub

  2021-03-23

  

  Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p

15735 records 683/1049 page Previous Next First page 上5页 681682683684685 下5页 Last page