• Introduction Cysteinyl leukotrienes CysLTs LTC LTD and

  2020-05-05

  

  Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic d-amphetamine and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3], [4] and montelu

• potassium hydrochloride br Results and Discussion br Conclus

  2020-05-05

  

  Results and Discussion Conclusion What we have shown here is that highly specific antagonist can be a very useful tool, can mimic gene KO experiments or even further dissect receptor function. We just took ETA antagonist as an example and found that ETA mediates physiological closure of DA whi

• br Expression and Tissue Functions of

  2020-05-05

  

  Expression and Tissue Functions of DDRs The DDRs are widely expressed in different tissues, both during development and in adult organisms. DDR1 mRNA is found in many tissues in mice and humans, with high levels in brain, lung, kidney, spleen, and placenta (Di Marco et al., 1993, Johnson et al.,

• br Conclusions br Acknowledgment br Introduction The role

  2020-05-05

  

  Conclusions Acknowledgment Introduction The role of cholesterol metabolism during multiple sclerosis (MS) is debated and the underlying physiopathology largely unknown. Dyslipidaemia is associated with worsening inflammatory activity and MS disease progression [1], [2], [3]. In the mouse mo

• br Authors contribution br Disclosure statement br Acknowled

  2020-05-05

  

  Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)

• br Conclusions br Acknowledgements This work was supported b

  2020-05-05

  

  Conclusions Acknowledgements This work was supported by funding from the Natural Sciences and Engineering Research Council of Canada (RGPIN-2017-06346 to JB), National Institute of Child Health and Human Development (5R01HD083930-02 to JB), and the National Institute of Biomedical Imaging and

• br Materials and methods br Results br Discussion We initial

  2020-05-05

  

  Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen

• br Conclusions br Introduction Today just as

  2020-05-05

  

  Conclusions Introduction Today – just as for the past 50 years – the most commonly used repellent in the world is DEET (Fradin, 1998; Pickett et al., 2008). The active ingredient, N,N-Diethyl-m-toluamide, is an oily synthetic substance applied topically to the skin in order to alter the host f

• br Chk and Chk mediated signaling act

  2020-05-05

  

  Chk 1 and Chk 2 mediated signaling act as a barrier to tumorigenesis It was hypothesized recently that early events during tumorigenesis, such as the overexpression of oncogenes, lead to a DNA-damage response which, in turn halts tumor progression [44], [45], [46]. The DNA-damage response is prop

• One step in pyrimidine biosynthesis is conversion of

  2020-04-30

  

  One step in pyrimidine biosynthesis is conversion of l-dihydroorotate (DHO) to orotate (ORO), under action of the enzyme dihydroorotate dehydrogenase (DHODH, EC 1.3.99.11), which contains a flavine (FMN) as redox cofactor [1]. In this transformation, electrons resulting from DHO oxidation are transf

• Our previous high throughput screening HTS

  2020-04-30

  

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

• Interestingly anti inflammatory actions for sPLA V were also

  2020-04-30

  

  Interestingly, anti-inflammatory actions for sPLA2-V were also described in mice a few years ago in a model of autoimmune complex mediated arthritis [148]. A novel mechanism was delineated, whereby sPLA2-V promotes phagocytosis of immune complexes by macrophages to ameliorate inflammation in autoimm

• In bone PGE exerts both

  2020-04-30

  

  In bone, PGE2 exerts both anabolic and catabolic effects [6], [7], [8], [9]. Administration of PGE2 to mice lacking each of the four prostanoid receptors identified EP4 as the primary mediator of PGE2-induced bone formation [10]. While the role of EP1 in osteoblastic differentiation and bone metabol

• br Clinical potential of ET receptor biased ligands Is there

  2020-04-30

  

  Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21

• Moreover considering that several polyphenols and flavonoids

  2020-04-30

  

  Moreover, considering that trpv1 antagonist several polyphenols and flavonoids (i.e. chalcones, flavanones, resveratrol derivatives, ellagic acid) are reported to inhibit tyrosinase and elastase (Pillaiyar et al., 2017; Xing et al., 2016; Wittenauer et al., 2015), the relations between enzyme inhib

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