• It was demonstrated that the

  2019-07-05

  

  It was demonstrated that the addition of 10-fold excess of α-synuclein without modifications (with respect to the molar concentration of tetrameric GAPDH) leads to partial inactivation of GAPDH after 1-h incubation by 20% (Fig. 4, curve 2) in Fucoidan to insignificant decrease of the specific activ

• br Concluding remarks br Introduction Hypertrophic pachymeni

  2019-07-05

  

  Concluding remarks Introduction Hypertrophic pachymeningitis (HP) is a neurologic disorder characterized by diffuse or focal thickening of the intracranial or spinal dura mater, presenting with intracranial hypertension, cranial nerve palsy and spinal cord dysfunction (Kupersmith et al., 2004;

• pak 4 To investigate the mechanism of

  2019-07-05

  

  To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due

• Kinetic isotope effects KIEs inform on bond vibrational chan

  2019-07-05

  

  Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal antibiotics of labeled substrate

• Schizandrin A We have previously reported the characterizati

  2019-07-05

  

  We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot

• Replacement of the saturated propoxy group in compound

  2019-07-05

  

  Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have

• br Transparency document br Acknowledgments

  2019-07-05

  

  Transparency document Acknowledgments This study was funded by ICMR, Govt. of India. Alisha Dhiman acknowledges UGC-DSKPDF, India for post-doctoral fellowship and Monisha Gopalani acknowledges CSIR, India for Senior Research Fellowship. AIRF, JNU is acknowledged for TEM, confocal microscopy an

• Our previous work has demonstrated that two glutamate residu

  2019-07-05

  

  Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi

• Breast cancer is the most common neoplasm in women with

  2019-07-05

  

  Breast cancer is the most common neoplasm in women, with approximately 231,840 new cases of invasive breast cancer, 60,290 additional cases of in situ breast cancer and 40,290 deaths occurring in 2015 in the United States. Meanwhile, about 2350 men will be diagnosed with breast cancer, and 440 men w

• These studies suggested that PV PVH

  2019-07-05

  

  These studies suggested that PV/PVH might promote bone formation activities and/or inhibit bone resorption activities probably due to its anti-inflammation activity; however, the underlying mechanism remained unknown. Furthermore, it is unclear if PVH shows better activity than that of PV; this is i

• Studies of Jelski and Szmitkowski show that differences of

  2019-07-04

  

  Studies of Jelski and Szmitkowski show that differences of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activity between guanidine hydrochloride of many cancers and healthy tissue may be one of the factors intensifying carcinogenesis [7]. Moreover, changes of ADH and ALDH activity

• In this study we reported that over expressed

  2019-07-04

  

  In this study, we reported that over-expressed endogenous central ET-1 exerted anti-allodynic and anti-hyperalgesic effects on SNL-induced NP for the first time. Furthermore, we showed that ETA-R mRNA However, together with the level of ET-1 was increased in the CNS up to 21days after SNL surgery i

• Grapiprant is a selective antagonist for

  2019-07-04

  

  Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap

• The Acat gene was identified by functional complementation

  2019-07-04

  

  The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, atp gamma s 1 and 7, with each site containing a distinct promoter: chromosome 1 contains exon

• In our previous research we have focused on the discovery

  2019-07-04

  

  In our previous research, we have focused on the discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Numbers of biphenyl-aryl urea incorporated with salicylaldoxime including BPS-7 have been developed as potent and selective VEGFR-2 inhibitors (Fig. 3) [12], [13], [14], [15], [16], [1

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