• In the current study cocaine did not

  2020-10-22

  

  In the current study, cocaine did not significantly increase negative subjective effects and nepicastat did not increase these responses. This outcome is somewhat surprising given that the most commonly reported effect to date has been to increase the aversive properties of cocaine such as anxiety,

• Like compound substitution on compound contains amino and ca

  2020-10-22

  

  Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226. Th

• The ribosomal synthesis of D

  2020-10-22

  

  The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi

• Several research groups have disclosed potent

  2020-10-22

  

  Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2

• Our recent discovery M P H R

  2020-10-22

  

  Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w

• A variety of fused membered ring chemotypes have arisen

  2020-10-21

  

  A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (PG

• br Conflict of interest statement br Acknowledgements br Int

  2020-10-21

  

  Conflict of interest statement Acknowledgements Introduction Spending their last days on earth having already lost many cognitive functions remains a major fear of elderly people. Although during the last century their lifespans increased, the so-called “old-age diseases” became more and mo

• br Materials and methods br Results br Discussion CHIKV

  2020-10-21

  

  Materials and methods Results Discussion CHIKV is an important arthropod borne virus with substantial impact on global health and cause a major viral disease that requires the development of antiviral drug to combat chikungunya disease. Virus specific proteases have particularly become an a

• br Methods br Results br Discussion MEN

  2020-10-21

  

  Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3

• Because most fusion detection methods

  2020-10-21

  

  Because most fusion detection methods were developed to analyze paired-end reads (and especially Illumina data), they are not suitable for identifying fusion junction-spanning reads in single-end Ion Torrent libraries. Therefore, we developed the FusionDetect algorithm (implemented in the ChildDecod

• It has been reported that PGE increases expression of the

  2020-10-21

  

  It has been reported that PGE2 increases expression of the survivin mRNA (Baratelli et al. 2005) and promotes the stabilization of the survivin protein in some tumor Caspase-9 Fluorometric Assay Kit (Krysan et al. 2003). However, it is unclear whether PGE2 affects the expression of survivin mRNA o

• Epitope analyses of AT AA

  2020-10-21

  

  Epitope analyses of AT1-AA and ET-AA indicate that the 1,2-Dilauroyl-sn-glycerol of both autoantibodies are located at the second extracelluar loop of both receptors. The specific epitopes for both autoantibodies are similar to what was reported previously in a cohort of patients from Brazil [6] an

• Introduction Myclobutanil MCL RS chlorophenyl H triazol ylme

  2020-10-21

  

  Introduction Myclobutanil (MCL), (RS)-2-(4-chlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)hexanenitrile (Fig. 1), is a broad-spectrum systemic triazole fungicide with protective, eradicative, and curative action (University of Hertfordshire, 2018). It is employed to control pests such as powdery mild

• 1295 In this study we have explored a

  2020-10-21

  

  In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta

• Approximately of the etamicastat dose was recovered in urine

  2020-10-21

  

  Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be

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