• To investigate the role of DPP inhibition in

  2019-10-17

  

  To investigate the role of DPP-4 inhibition in inflammation-induced bone resorption, we evaluated the effect of a DPP-4 inhibitor on LPS-induced osteoclast formation and bone-resorption in vivo. Our results showed that the DPP-4 inhibitor inhibited LPS-induced osteoclast formation and bone resorptio

• The members in apple are similar

  2019-10-17

  

  The 8 members in apple are similar in number to the 7 in Arabidopsis and the 8 in rice, but fewer than the 10 found in mammalian species. GenBank numbers have also been reported for DGK homologues from tomato (AW035995), maize (AY106320), wheat (BT009326), a Populus cross (BU828590), grape (CB981130

• Based on the deduced amino

  2019-10-17

  

  Based on the deduced amino [Ala92]-p16 (84-103) sequence of the catalytic subunit of rG3DH, we could find sequence features that are highly conserved in FAD-harboring dehydrogenase, which include FAD binding motif and sequential cysteine residues in Cysteine-rich region. Several dehydrogenases shar

• Collectively the results presented here provide new insights

  2019-10-17

  

  Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of

• Moreover recent structural studies of

  2019-10-17

  

  Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT

• 9-Phenanthrol clinical Deregulated Wnt signaling either due

  2019-10-17

  

  Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen

• Redundancy of tumor promoting signaling pathways is one of

  2019-10-17

  

  Redundancy of tumor promoting signaling pathways is one of the mechanisms that prevent a lasting effect of targeted therapies, as has been demonstrated by the growing number of alternative pathways that confer resistance to EGFR-targeted therapies [3]. We show here that CSF-1R can, at least partiall

• In the original ELF study patients were considered

  2019-10-17

  

  In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and

• Peptides undergoing only a single hydroxylation

  2019-10-17

  

  Peptides undergoing only a single hydroxylation, i.e. PA-Hyp-KPAPK and PAPK-Hyp-APK, were then used to investigate the kinetics of vCPH co-factor and co-substrate dependences. The values for KMapp for Fe(II) and KM for 2OG for the two peptide substrates were within error (KMapp, Fe(II): 0.9 μM ± 0.1

• Through the process of alternative splicing the IKZF

  2019-10-17

  

  Through the process of alternative splicing, the IKZF1 gene is capable of encoding a large number of Ikaros isoforms (Molnar et al., 1996). Some of these isoforms were shown to have distinct functions (Li et al., 2011, Ronni et al., 2007). Ikaros protein contains four zinc fingers at the N-terminus

• br Experimental Procedures br Acknowledgments br Bisphenol A

  2019-10-17

  

  Experimental Procedures Acknowledgments Bisphenol A (BPA) has been recognized as one of the most potent endocrine disruptors, functioning even at very low doses. Although it is anticipated that CCT251545 analogue receptor (ER) would mediate these effects of low-dose BPA, studies revealed th

• br Conflict of interest statement br Acknowledgement The

  2019-10-17

  

  Conflict of interest statement Acknowledgement The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7/2007-2013) under grant agreement n° 278742 (Eurosarc) Introduction Pseudomyogenic hemangioendothelioma/epithelioid sarcoma-like

• For the current studies we used the selective Epac agonist

  2019-10-17

  

  For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce

• The optimization of the lead compound

  2019-10-17

  

  The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Brefeldin A moiety with other functional groups led to loss of functional activity against EP4 receptor.

• To develop antagonists selective for

  2019-10-16

  

  To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic 449 () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde . 4-Chl

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