• br STAR Methods br Acknowledgments We are grateful

  2020-09-15

  

  STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac

• Further modifications on the position of compound

  2020-09-15

  

  Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po

• Furan analogs and N methylpyrrole analogs had completely dif

  2020-09-15

  

  Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 PF-5274857 mg affinity and an increased antagonist activity, while the corresponding chemical modi

• A wealth of studies support the key role of

  2020-09-15

  

  A wealth of studies support the key role of high NO in promoting higher blood flow and thus greater O2 delivery to working tissues in healthy Tibetans and thus partly compensate hypoxia induced low arterial O2 content [7,9,27]. We observed high eNOS mRNA, protein and enzyme activity in Ladakhi women

• Our study revealed elevated basal Akt phosphorylation in

  2020-09-15

  

  Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti

• br Conflicts of interest br Financial support NZ is

  2020-09-14

  

  Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818

• Currently much effort has been made to design and synthesize

  2020-09-14

  

  Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a

• Tailoring pharmacological treatment to the genetic backgroun

  2020-09-14

  

  Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72

• Beta-Lapachone Saururus chinensis Lour Baill Saururaceae

  2020-09-14

  

  Saururus chinensis (Lour.) Baill. (Saururaceae), a perennial herb, is widely cultivated in China and southern Korea. It has been traditionally used as folk medicine for the treatment of inflammation, jaundice and gonorrhea [8]. Previous chemical studies of S. chinensis have revealed the presence of

• Although PQQ has nutritional importance and pharmacological

  2020-09-14

  

  Although PQQ has nutritional importance and pharmacological effects in higher organisms, including humans [15], until recently, there was no clear evidence for the use of PQQ as a co-factor in a eukaryotic enzyme. This review presents a novel eukaryotic PQQ-dependent quinohemoprotein recently discov

• br Materials and methods br Results

  2020-09-14

  

  Materials and methods Results The BUN and creatinine levels in the saline-treated CRF group were found to be significantly higher than those in the sham-operated control rats treated with either montelukast or saline (pHeparin tissues, were found to be significantly higher in the saline-treate

• Testosterone is inactivated through hydroxylation and conjug

  2020-09-14

  

  Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in

• Midazolam oral clearance is used

  2020-09-14

  

  Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo

• br Transparency document br Acknowledgments This work was su

  2020-09-14

  

  Transparency document Acknowledgments This work was supported by the Ministry of Education, Youth and Sports of the Czech Republic (the National Program of Sustainability I, Grants LO1204 and LO1304), by the Czech Science Foundation (15-17282Y) and by Palacký University Olomouc (IGA_PrF_2017_0

• The identification of CRF receptor subtypes has led

  2020-09-14

  

  The identification of CRF DDD107498 synthesis subtypes has led to a number of studies addressing its functional properties. This paper examines the evidence for CRF1 and CRF2 mediation of fear and anxiety. Recent reviews discussing specific CRF receptor functions associated with other conditions in

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