• Brain derived neurotrophic factor BDNF is the most abundant

  2022-03-30

  

  Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of

• Herein we describe the design and optimization

  2022-03-30

  

  Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during

• br Conclusions br Conflicts of interest br Funding The resea

  2022-03-30

  

  Conclusions Conflicts of interest Funding The research work was partially supported by National Science Center (Contract Grant Number: UMO-2015/19/B/NZ1/00332). Introduction Frusectose-1, 6-bisphosphatase (FBPase) has long been recognized as a potential therapeutic target for the treatm

• To discriminate the peripheral and central involvement of FA

  2022-03-30

  

  To discriminate the peripheral and central involvement of FAAH in paracetamol action, we proposed a pharmacological strategy challenging the analgesic action of paracetamol observed in an inflammatory context with either a peripherally-restricted FAAH inhibitor (URB937, Clapper et al., 2010, Moreno-

• RO4956371 Here we show in contrast to previous work that sev

  2022-03-30

  

  Here we show, in contrast to previous work, that several phenotypes associated with Orb6 inactivation, including increased cell width, are independent of Gef1. We further find that Orb6 positively regulates exocytosis, also independently of Gef1. To identify novel targets of Orb6, we performed quant

• Here we report the kinetics of inhibition of

  2022-03-30

  

  Here, we report the kinetics of inhibition of the MYST HAT family member KAT8 by MG149, and a calculation of the inhibitory constant Ki of MG149 for KAT8. The inhibition of HATs by MG149 could be correlated to inhibition of histone acetylation in murine PCLS upon MG149 treatment, as determined by a

• Compared to the other histamine receptor

  2022-03-30

  

  Compared to the other vomitoxin receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005) and B

• Importantly the regulation of the Hippo pathway by metabolic

  2022-03-30

  

  Importantly, the regulation of the Hippo pathway by metabolic networks, such as by glycolysis39, 40, hexosamine biosynthesis41, 42, and mevalonate synthesis43, 44, as well as by nutrient-sensing pathways including AMP-activated protein kinase (AMPK) 40, 45, 46 and mTOR 47, 48, 49, 50, was recently d

• The Hedgehog signaling pathway HH pathway hereafter

  2022-03-30

  

  The Hedgehog signaling pathway (HH pathway hereafter) is vital for development and tissue homeostasis. [4] In recent years, studying the role of the HH pathway in carcinogenesis and cancer stemness has highlighted the HH inhibitors as putative cancer therapeutics [5]. However, clinical application o

• Importantly recent in vivo results demonstrated

  2022-03-30

  

  Importantly, recent in vivo results demonstrated that combining an HDACi and a IKK inhibitor significantly reduced ovarian tumor growth compared with either inhibitor alone [26]. The slowest tumor growth in the HDACi/IKK inhibition combination group was associated with the lowest CXCL8 tumor and pla

• In the present referred patients

  2022-03-30

  

  In the present referred patients with hemochromatosis and HFE p.C282Y homozygosity, eight of the ten patients with HCV infection were men. In another US cohort of ten patients with HFE p.C282Y homozygosity, chronic HCV infection, and stage 3 or 4 fibrosis, all were men [30]. In the present post-scre

• Recently anti tumor or antiviral strategies using RNAi for

  2022-03-30

  

  Recently, anti-tumor or antiviral strategies using RNAi for both gene silencing and innate-receptor activation were designed; one mechanism of these strategies is activating the intracellular retinoic acid–inducible gene I protein (RIG-I). 5′-Triphosphate RNA (3p-small interfering RNA [siRNA]) is th

• The endocytic inhibitors MDC and

  2022-03-30

  

  The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat

• Routine administration of exogenous GC is pertinent

  2022-03-29

  

  Routine administration of exogenous GC is pertinent during late gestation, particularly in women who are at risk of delivering a preterm infant, aiming at ensuring proper neonatal outcome and survival (Kamath-Rayne et al., 2012). Unfortunately, despite its beneficial roles in foetal survival, variou

• For some agonists these stable GPR responses were resistant

  2022-03-29

  

  For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer

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