• The activation of GPR FFA signaling

  2021-10-09

  

  The activation of GPR40/FFA1 signaling triggers the PLC/PIP2 signaling pathway and results in Ca2+ release from the endoplasmic reticulum (ER). Increased Ca2+ levels may lead to activation of different protein kinases, such as Ca2+/calmodulin-dependent protein kinase type IV, Akt, extracellular sign

• br Acknowledgements We thank Dr

  2021-10-09

  

  Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery

• Computational approaches such as docking and classical molec

  2021-10-09

  

  Computational approaches such as docking and classical molecular dynamics (MD) are now commonly used to study the structure and dynamics of proteins as well as associated protein-ligand interactions [12]. A fundamental requirement of MD in order to accurately determine the behavior of a protein over

• br Conflict of interest br Funding br Introduction Heme is

  2021-10-09

  

  Conflict of interest Funding Introduction Heme is an essential molecule for cellular metabolism involving oxygen and electron transfer [1]. However, free heme is a potent pro-oxidant that catalyzes the generation of reactive oxygen species (ROS) leading to cellular damage [2]. Heme oxygenas

• In conclusion while class I HDAC inhibitors isoform

  2021-10-09

  

  In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides

• Of special interest is that riociguat

  2021-10-09

  

  Of special interest is that riociguat and NO donors decreased the phosphorylation of many proteins in human platelets. This aspect is presently under further investigation but a few comments can be made already here. Of the extensive spectrum and diversity of human protein kinases and protein phosph

• We observed that the Toc G domain

  2021-10-09

  

  We observed that the Toc159G domain recognizes the N-terminal portion of the transit peptide of pSSU with a dissociation constant of 70 μM (Fig. 2; Table 1), while a tenfold higher KD was obtained for the phosphorylated C-terminal region. In turn, the homodimer of Toc34G recognizes the phosphorylate

• Glutathione transferases GST have been discovered

  2021-10-09

  

  Glutathione transferases (GST) have been discovered in many tissues including the cornea of humans and several other mammals (Awasthi et al., 1980, Bilgihan et al., 2003; Gondhowiardjo and van Haeringen, 1993; Saneto et al., 1982, Sastry et al., 1995, Singh et al., 1985, Watkins et al., 1991). To da

• Approximately mammalian genes encoding family A or

  2021-10-09

  

  Approximately 250 mammalian genes encoding family A (or rhodopsin-like) GPCRs have been cloned (Lee et al., 2001a). As yet, the total number of cloned GPCRs reported in the literature including the secretin and metabotropic glutamate-like families of GPCRs falls short of the projected 616 GPCR-encod

• Initial evidence that cell contact mediated transmission

  2021-10-09

  

  Initial evidence that cell-contact-mediated transmission of HIV-1 is relevant for the generation of latently infected ml7 was suggested in the context of transmission from dendritic cells to resting CD4+ T cells (Evans et al., 2013, Kumar et al., 2015). As dendritic cells probe for antigens, they c

• We also explored various nitrogen

  2021-10-09

  

  We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff

• In contrast to UDG SMUG

  2021-10-09

  

  In contrast to UDG, SMUG1 exhibits dramatically lower product yield in its excision of U, and this is not dependent on sequence context. Though we cannot rule out that a small amount of the product is derived from a duplex contaminant, our extensive purification techniques limit the amount of conta

• As a part of our continuing efforts towards discovery of

  2021-10-09

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• We report on four affected children

  2021-10-09

  

  We report on four affected children from two unrelated consanguineous SGC 0946 with moderate to severe ID associated with epilepsy and variable neuropsychiatric features. Using whole-exome sequencing, we identified homozygous missense variants in SLC45A1 (OMIM: 605763), which codes for a neuronal gl

• During the tests in vitro SHP showed

  2021-10-09

  

  During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g

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