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A computational and experimental study to develop E-selectin targeted peptides for molecular imaging applications.
Fernandes, Ana Carina; Liu, Mengjiao; Sorbo, Teresa; Appold, Lia Christina; Ilbert, Marianne; Ferracci, Géraldine; Kiessling, Fabian; F Branco, Ricardo J; Lammers, Twan; Iranzo, Olga.
Afiliación
  • Fernandes AC; Instituto de Tecnologia Química e Biológica António Xavier, Universidade Nova de Lisboa, Av. da República, 2780-157 Oeiras, Portugal.
  • Liu M; Aix Marseille Univ, CNRS, Cent Marseille, ISM2, Marseille, France.
  • Sorbo T; Institute for Experimental Molecular Imaging, University Clinic & Helmholtz Institute for Biomedical Engineering, RWTH Aachen University, Aachen, Germany.
  • Appold LC; Aix Marseille Univ, CNRS, Cent Marseille, ISM2, Marseille, France.
  • Ilbert M; Institute for Experimental Molecular Imaging, University Clinic & Helmholtz Institute for Biomedical Engineering, RWTH Aachen University, Aachen, Germany.
  • Ferracci G; Bioénergétique et Ingénierie des Protéines, Institut de Microbiologie de la Méditerranée, Aix Marseille Université, CNRS, UMR 7281, 13009 Marseille, France.
  • Kiessling F; Aix-Marseille Université, CNRS, INP - UMR7051, 13015 Marseille, France.
  • F Branco RJ; Institute for Experimental Molecular Imaging, University Clinic & Helmholtz Institute for Biomedical Engineering, RWTH Aachen University, Aachen, Germany.
  • Lammers T; UCIBIO, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal.
  • Iranzo O; Institute for Experimental Molecular Imaging, University Clinic & Helmholtz Institute for Biomedical Engineering, RWTH Aachen University, Aachen, Germany.
Future Med Chem ; 10(23): 2695-2711, 2018 Dec.
Article en En | MEDLINE | ID: mdl-30520324
Aim: E-selectin is overexpressed on angiogenic and inflamed endothelium. Molecules binding to E-selectin with high affinity and specificity enable its use as a molecular imaging biomarker. Material & methods: The interactions of four different peptides (i.e., Ac-P1 [Acetyl-IELLQAR-CONH2], H2N-P2 [H2N-DITWDQLWDLMK-CONH2], H2N-P3A5 [H2N-YRNWAGRW-CONH2], and Ac-P4 [Acetyl-YRNWDGRW-CONH2]) with E-selectin were analyzed by computational methodologies, surface plasmon resonance and in vitro using activated human umbilical vein endothelial cells. Poly(butyl cyanoacrylate) microbubbles were functionalized with the best candidates and evaluated as molecular ultrasound probes in cultured cells and explanted carotid arteries. Results: H2N-P3A5 and Ac-P4 peptides bound stronger to E-selectin than Ac-P1 and H2N-P2, but with lower specificity. H2N-P2 bound with higher specificity and affinity than Ac-P1. Conclusion: H2N-P2 is a good candidate for designing E-selectin-targeted molecular imaging agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Future Med Chem Año: 2018 Tipo del documento: Article País de afiliación: Portugal Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Future Med Chem Año: 2018 Tipo del documento: Article País de afiliación: Portugal Pais de publicación: Reino Unido