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The ADME profile of AAT was very promising
2020-12-07
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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br Substrate characterization of candidate peptide reporters
2020-12-07
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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Enolase as a plasminogen receptor and activator localized on
2020-12-07
Enolase, as a plasminogen receptor and activator localized on the surface of several helminths, can interact with the host fibrinolytic system (Yang et al., 2010, Du et al., 2009, de la Torre-Escudero et al., 2010). The enzyme is also one of excretory/secretory (ES) products in some helminths, such
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The isomeric phenyloxazole not only
2020-12-07
The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand AN-2728 receptor (as seen in compound pairs – and –) decrea
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br Experimental procedures br Acknowledgments br Introductio
2020-12-07
Experimental procedures Acknowledgments Introduction Receptor tyrosine kinases (RTKs) control many fundamental cellular processes, such as cell proliferation, differentiation, migration, and metabolism (Lemmon and Schlessinger, 2010). RTK activity is normally tightly controlled, and dysregu
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br Experimental Procedures br Author Contributions br Acknow
2020-12-07
Experimental Procedures Author Contributions Acknowledgments We acknowledge Géraldine Le Goff and Mathieu Canales for blood sampling, Cécile Gameiro and Jean-Pierre Aubry for flow cytometry technical assistance, Giuseppe Pantaleo for support, and Britta Engelhardt, Gisella Puga-Young, Nicol
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Across the scaffold the platform anchors the N terminus
2020-12-07
Across the scaffold, the platform anchors the N terminus of the elongated cullin structure of APC2 [21]. This connects to the flexible cullin–RING catalytic core consisting of the C-terminal region of APC2 and the associated APC11 11, 12, 21. The flexibility and positions of the catalytic core are c
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In the SUMOylation pathway SCE as an E enzyme
2020-12-07
In the SUMOylation pathway, SCE1 as an E2 enzyme has an important role in mediating the conjugation of SUMO to target proteins. The accumulated SUMO conjugates in plants are associated with abiotic stress responses (Castro et al, 2012). We performed a drought stress analysis on WT plants, induced by
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A previous study suggested that DARs and octopamine
2020-12-07
A previous study suggested that DARs and octopamine/tyramine receptors (OARs/TARs) have close pharmacological properties (Beggs et al., 2011). Their relationships were also supported by phylogenetic analyses (Balfanz et al., 2005, Hauser et al., 2008, Wu et al., 2014), indicating that some of DAR an
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PP242 During these processes meiotic recombination
2020-12-07
During these processes, meiotic recombination plays a critical role by physically associating homologs and ensures accurate chromosome segregation. In addition, meiotic recombination redistributes genetic material between homologs, resulting in haplotype diversity among progeny, impacting ecological
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In contrast to the methylation that is catalyzed exclusively
2020-12-07
In contrast to the methylation that is catalyzed exclusively by DNMTs, there have been suggested several pathways that could induce demethylation (Watt & Molloy, 1988). However, the existence and influencing of enzymes that promote active demethylation remains elusive. Studies aiming to gain more in
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br Introduction In mammals there
2020-12-07
Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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Considering all these facts in
2020-12-04
Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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In a cell based functional assay the
2020-12-04
In a cell-based functional assay, the antagonist properties of were assessed by measuring inhibition of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells. produced a concentration-dependent inhibition of CRF (1nM)-induced cAMP production with an IC
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Papain Inhibitor receptor br Advantages of modified proteins
2020-12-04
Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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