• Our structures also provide new

  2021-08-04

  

  Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta

• The in vitro cytotoxicity of the prodrugs was

  2021-08-04

  

  The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately

• Compression The L vertebral body was tested

  2021-08-04

  

  Compression: The L4 vertebral body was tested in compression with loads applied along the craniocaudal axis using an Instron 8800 device at a rate of 3mm/min. Load displacement data were captured using Bluehill software. The ultimate load, yield load, stiffness, ultimate stress, yield stress and You

• Two GPCR subtypes of interest in the myocardium are

  2021-08-04

  

  Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy

• br Results br Discussion The

  2021-08-04

  

  Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i

• br Methods br Results br Discussion Preclinical

  2021-08-04

  

  Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the 77 4 with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did not significantly al

• However one major challenge will be to understand how

  2021-08-04

  

  However, one major challenge will be to understand how the diverse actions of D2Rs in multipartite, dopamine-sensitive circuits are coordinated to produce specific behaviors across species. It is possible that emerging techniques for imaging neuronal activity in different neuronal population in beha

• br Methods for assessing TLS While

  2021-08-04

  

  Methods for assessing TLS While the precise quantification of restricted DNA synthesis events is possible (e.g. unscheduled DNA synthesis (UDS) reveals NER), so far, it is impossible to identify TLS stretches of only a few nucleotides within the background of bulk DNA replication of normal DNA. N

• In many studies spatial and temporal expression

  2021-08-04

  

  In many studies, spatial and temporal expression and subcellular localizations of the DNMTs are examined in greater detail. These studies are evaluated and discussed in the remaining part of the article. DNMT1 protein expression was characterized in the genital ridge of the primitive mouse gonad at

• Although there was little to no expression change observed

  2021-08-04

  

  Although there was little to no expression change observed by TELI of the recA and ruvA genes upon CAA exposure, other specific repair pathways were induced by both CAA and SO and include the SOS-inducible gene sulA, the DNA repair gene ykfG, the mismatch repair gene mutS, the recombination and repa

• In the present study Asian swamp

  2021-08-03

  

  In the present study, Asian swamp eel CXCR1a (MaCXCR1a), MaCXCR1b, MaCXCR2, MaCXCR3a, MaCXCR3b, and MaCXCR4 were identified from the Asian swamp eel genome. To explore the features and functions of these CXCRs, we focused on the identification and molecular characterization of MaCXCRs, and L-161,982

• Acidic substituents showed moderate biochemical activity but

  2021-08-03

  

  Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic glucagon receptor antagonist were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of

• CHAPS br Material and methods br

  2021-08-03

  

  Material and methods Results Diagrammatic representations showing the bilateral injection sites in the BNST of all animals used in the present study are presented in Fig. 1. Discussion The present results provide the first evidence that both CRF1 and CRF2 receptors in the BSNT are involved

• The small molecule d mannuronic

  2021-08-03

  

  The small molecule β-d-mannuronic p0035 (M2000), patented (DE-102016113018.4), has been tested as an anti-inflammatory and a novel immunosuppressive agent in various experimental models such as animal models of immune complex glomerulonephritis, nephrotic syndrome, multiple sclerosis and rheumatoid

• br Acknowledgments We thank the

  2021-08-03

  

  Acknowledgments We thank the Lapaha Community and Nobles (His Serene Highness Prince Kalaniuvalu Fotofili, Her Serene Highness Princess Marcella Taumoepeau Tupou Kalaniuvalu Fotofili and Her Royal Highness Mele Siu'ilikutapu Kalaniuvalu Fotofili) and the Ministry of Internal Affairs (Government o

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