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Molecular docking simulations were carried out for ligands i
2022-11-04
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic Me
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The co crystal structure of
2022-11-04
The co-crystal structure of ()-blebbistatin ()- bound to myosin II (PDB: ) was used to scout for possible favorable interactions with the residues lining the binding pocket. Looking at A, we hypothesized that -oriented hydrophilic moieties (e.g. hydroxymethyl) on C of the blebbistatin scaffold might
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In addition to drawing attention to
2022-11-04
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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br Material and methods br Results br Discussion
2022-11-04
Material and methods Results Discussion Although we were not able to detect 12/15-LOX mRNA in the lungs of 12/15-LOX knockout mice substantial amounts of 15-HETE could be detected in BALF. In fact, significant synthesis of 15-HETE in 12/15-LOX mice have been already reported [17]. The redun
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Transient transfection with ATR kinase dead D
2022-11-04
Transient transfection with ATR kinase-dead (D2475→A) [30] and ATM kinase-dead (D2870→Ala and N2875→K) [31] constructs was performed using Fugene 6 (Roche Applied Science, Indianapolis). Three microliters of fugene 6+1μg plasmid was used in transfections using 6-well plates at 2×105 cells/well and a
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Tetracyclines constitute one of the
2022-11-03
Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200
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The molecular mechanisms that mediate the plasticity of
2022-11-03
The molecular mechanisms that mediate the plasticity of the NMJ are not well understood. PGC-1α is a master regulator of the NMJ gene expression program 23, 24, and thus AMPK might indirectly regulate the NMJ via its broad influence on the coactivator. Cerveró et al.[6] recently provided more direct
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br MHCI peptide editing N
2022-11-03
MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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br Stress glucocorticoids as risk factor for Alzheimer s Dis
2022-11-03
Stress/glucocorticoids as risk factor for Alzheimer’s Disease: preclinical studies A role for glucocorticoids in shaping the risk for AD is supported by animal studies using rats or mice injected with Aβ oligomers, tau protein or excitotoxins, or transgenic (Tg) mice carrying mutations associated
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br Experimental procedure br Introduction Migraine is a
2022-11-03
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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Acknowledgements The work was supported
2022-11-03
Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medic
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br Funding This work was supported by Arena Pharmaceuticals
2022-11-03
Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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In young animals the HT
2022-11-03
In young animals, the 5-HT2A L-690,330 antagonist ketanserin, at relatively low concentrations, shifted 5-HT concentration-response curves rightward, suggesting a role for 5-HT2A receptors in mediating 5-HT-induced contractions of the ureter. The slopes of the ketanserin Schild plots for the antago
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TCS 2002 A high throughput screening campaign led to the
2022-11-03
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Introduction According to Uganda s Ministry of Health MOH a
2022-11-02
Introduction According to Uganda's Ministry of Health (MOH 2012a:91), intermittent preventive treatment (IPT) to avoid malaria during pregnancy is a free preventive service available to all pregnant women without clinical signs and symptoms of malaria, attending prenatal clinics. However, pregnant
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