• In an attempt to further optimize interactions in the

  2021-11-09

  

  In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou

• br Materials and methods br Results In this study

  2021-11-09

  

  Materials and methods Results In this study we re-examined the kinetics of ET transport and tested the ability of various suggested substrates of OCNT1 to inhibit ET uptake. Using a native ET transporter expressed in the human HeLa cell line ET was found to be taken up with a Km of 51 μM and V

• We also demonstrated that inhibition of NAAG hydrolysis to s

  2021-11-09

  

  We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express

• Introduction The brain contains abundant fatty acids which s

  2021-11-09

  

  Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev

• br Materials and methods br Results br

  2021-11-09

  

  Materials and methods Results Discussion Quercetin is a relatively abundant bioactive flavonoid with a wide variety of documented physiological effects, which has gained popularity as a nutritional supplement [40]. There is increasing interest in quercetin's anticancer properties (for recen

• Expression and translocation of GLUT are

  2021-11-09

  

  Expression and translocation of GLUT4 are regulated by various mechanisms including protein kinase C isoforms (PKCs) and mitogen-activated protein kinase (MAPK) signals [22], [23], but the real mechanism that statins alter expression and function of GLUT4 has not been fully identified. It is general

• This work was supported by the

  2021-11-09

  

  This work was supported by the National Natural Science Foundation of China (Grants 81471101 and 81870852), the Natural Science Foundation of Jiangsu Province (Grant BK20181146), the Natural Science Foundation of the Jiangsu Higher Education Institutions of China (Grants 18KJA320007 and 17KJB320018)

• In summary our findings provide the evidence and the

  2021-11-09

  

  In summary, our findings provide the evidence and the mechanistic understanding of the protective effects of GIP receptor agonist, D-Ala2GIP, in the MPTP-induced neurotoxicity in mice. The observed protective effects are potentially due to reduced oxidative stress and attenuation of dopamine loss in

• br Contributions br Acknowledgements This research was suppo

  2021-11-09

  

  Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua

• br Presenilins and Wnt catenin signalling Several

  2021-11-09

  

  Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a

• The PK profile and tissue distribution of which

  2021-11-09

  

  The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an

• The release of FBPase and aldolase from subcellular structur

  2021-11-09

  

  The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle bcl-2 inhibitor was about 6–7 times higher in the

• Recently the spectrin cytoskeleton a

  2021-11-09

  

  Recently, the spectrin cytoskeleton, a deformable actin-associated network, has been identified as a modulator of Yki function, potentially acting both apically and basally in different cell types [75•, 76•, 77•]. Several mechanisms have been proposed, including regulation via Crb/Ex tethering [], t

• Of the many thousands of mutations analyzed in tracheal term

  2021-11-09

  

  Of the many thousands of mutations analyzed in tracheal terminal cells, less than a handful affect tube morphology specifically in the transition zone (Baer et al., 2007, Beitel and Krasnow, 2000, Förster et al., 2010, Ghabrial et al., 2011, Myat et al., 2005, Ruiz et al., 2012, Samakovlis et al., 1

• One of the key epithelium derived factors required to

  2021-11-08

  

  One of the key epithelium-derived factors required to maintain immune tolerance in the intestine is Indian Hedgehog (Ihh). Ihh is secreted exclusively by intestinal epithelial cells, and signals in a paracrine manner to the inhibitory receptor Patched1 (Ptch1) on nisin in the mesenchyme. Binding of

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