• Our previous high throughput screening HTS campaign using

  2021-04-17

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based Mifepristone assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22],

• Collectively the results presented here provide new insights

  2021-04-17

  

  Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of

• The total reduced glutathione content

  2021-04-17

  

  The total reduced glutathione content was determined in both c-di-AMP to examine whether retinol was decreasing glutathione concentrations and thus decreasing the conjugation of NAPQI. Total hepatic (3.9±0.3 vs 4.9±1.0 μmol/g, retinol vs untreated, respectively) and renal (0.4±0.1 vs 0.2±0.1 μmol/g

• In some cases more than one CYP enzyme may be

  2021-04-17

  

  In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple CGP 42112 (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape to determine the k

• Immunomodulation effects of certain oxysterols were previous

  2021-04-17

  

  Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychol

• SIRT is a representative member of Sirtuins which is a

  2021-04-17

  

  SIRT1 is a representative member of Sirtuins, which is a family of highly conserved NAD+-dependent class III histone deacetylases. SIRT1 deacetylates plentiful nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016; Gu et al., 2016; Tu et al., 2018) to p

• The quaternary structure of many of

  2021-04-17

  

  The quaternary structure of many of the family B members (i.e., secretin, glucagon, glucagon-like peptide and SC 144 receptor receptors) have been actively studied and it has been demonstrated that they can form homodimers/oligomers (Gao et al., 2009; Ng & Chow, 2015; Ng, Lee, & Chow, 2013). Hariku

• Air trapping at the small

  2021-04-17

  

  Air-trapping at the small airways is related to severe MK1775 (Bjermer, 2014), and acute exacerbation (Mahut et al., 2010). Although asthma patients are generally treated with inhaled corticosteroid (ICS) or with ICS and long-acting β2 agonist (LABA), the efficacy of such treatment depends on drug p

• BAY 87-2243 While several C terminal peptides have

  2021-04-17

  

  While several C-terminal peptides have been reported to have modest (astressin) or substantial (astressin2-B, antisauvagine-30) subtype selectivity for the CRF2 receptor (), [125I]YP20 is the first reported small analog of the C-terminus of CRF exhibiting subtype selectivity for the CRF1 receptor vs

• Tacrine amino tetrahydroacridine I Fig was

  2021-04-16

  

  Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor

• br Introduction Oral contraceptives OCs are the most

  2021-04-16

  

  Introduction Oral contraceptives (OCs) are the most commonly used medication for contraception all over the world and are also used in the treatment of menstrual disturbances and hyperandrogenism in women with polycystic ovary syndrome [1]. The impact of OC steroids on cardiovascular pathophysiol

• MK-2206 receptor br Materials and methods br Results br Disc

  2021-04-16

  

  Materials and methods Results Discussion COX-2-mediated production of PGE2 is involved in cell growth and metastasis of many cancers. Previous studies indicated that COX-2 was overexpressed in many cancer tissues and that PGE2 increased cancer cell growth, a process that could be suppressed

• The expression of DDR receptor

  2021-04-16

  

  The expression of DDR2 receptor has regulated by numerous types of factors depending upon the cell type. During the osteogenic differentiation, the transcription factorATF4 combined with CCAAT/enhancer binding site in the DDR2 promoter, which is responsible for induction of DDR2 transcription [24].

• br Inhibiting APC C during Interphase and prior to

  2021-04-16

  

  Inhibiting APC/C during Interphase and prior to Anaphase Because ubiquitylation by APC/C triggers cell division, it is essential that APC/C is restrained until cells are prepared for its substrates to be degraded. In addition to regulation by phosphorylation, an additional layer of control comes

• In plants SUMOylation has been shown to modulate plant hormo

  2021-04-16

  

  In plants, SUMOylation has been shown to modulate plant hormone signaling (Lois et al., 2003, Miura et al., 2009, Conti et al., 2014), root stem cell maintenance (Xu et al., 2013), and responses to abiotic and biotic stress (Lois, 2010). Many of the plant biological processes regulated by SUMOylatio

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