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New small-size peptides modulators of the exosite of BACE1 obtained from a structure-based design
(Taylor & Francis, 2016-03)
We report here two new small-size peptides acting as modulators of the β-site APP cleaving enzyme 1 (BACE1) exosite. Ac-YPYFDPL-NH2 and Ac-YPYDIPL-NH2 displayed a moderate but significant inhibitory effect on BACE1. These ...
Active and exo-site inhibition of human factor Xa: Structure of des-Gla factor Xa inhibited by NAP5, a potent nematode anticoagulant protein from Ancylostoma caninum
(Elsevier B.V., 2007-08-17)
Hookworms are hematophagous nematodes capable of growth, development and subsistence in living host systems such as humans and other mammals. Approximately one billion, or one in six, people worldwide are infected by ...
Active and exo-site inhibition of human factor Xa: Structure of des-Gla factor Xa inhibited by NAP5, a potent nematode anticoagulant protein from Ancylostoma caninum
(Elsevier B.V., 2007-08-17)
Hookworms are hematophagous nematodes capable of growth, development and subsistence in living host systems such as humans and other mammals. Approximately one billion, or one in six, people worldwide are infected by ...
Intermolecular interactions and characterization of the novel factor Xa exosite involved in macromolecular recognition and inhibition: Crystal structure of human Gla-domainless factor Xa complexed with the anticoagulant protein NAPc2 from the hematophagous nematode Ancylostoma caninum
(Elsevier B.V., 2007-02-16)
NAPc2, an anticoagulant protein from the hematophagous nematode Ancylostoma caninum evaluated in phase-II/IIa clinical trials, inhibits the extrinsic blood coagulation pathway by a two step mechanism, initially interacting ...
Investigation of Thrombin Activity with PAR 1-based Fluorogenic Peptides
(Bentham Science Publ Ltd, 2013-10-01)
Thrombin, a highly specific protease of blood coagulation, has two exosites that modulate its specificity. We designed two sets of synthetic substrate FRET peptides with 25- or 11-amino acids (aa) each, based on the PAR 1 ...
Structural and functional insights into the anti-BACE1 Fab fragment that recognizes the BACE1 exosite
(Taylor & Francis, 2014-09)
A molecular modeling study giving structural, functional, and mutagenesis insights into the anti-BACE1 Fab fragment that recognizes the BACE1 exosite is reported. Our results allow extending experimental data resulting ...
Structural and thermodynamic characteristics of the exosite binding pocket on the human BACE1: A molecular modeling approach
(American Chemical Society, 2010-09-23)
We report a molecular modeling study aimed to locate and provide the full structural characteristics of the exosite binding site of the BACE1. A three-step procedure was followed. In the first stage, we performed blind ...
Regulation of thrombin activity with ultrasmall nanoparticles: effects of surface chemistry
(American Chemical Society, 2020-06-26)
Nanomaterials displaying well-tailored sizes and surface chemistries can provide novel ways with which to modulate the structure and function of enzymes. Recently, we showed that gold nanoparticles (AuNPs) in the ultrasmall ...