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Article Dans Une Revue Journal of Inorganic Biochemistry Année : 2011

Chelate oxorhenium to assemble new integrin antagonists

Résumé

Assembly of independent chemical modules through oxorhenium coordination by a NS$_2$ + S chelation motif was applied to the synthesis of RGD (Arg-Gly-Asp) analogs. Modules were assembled through oxorhenium chelation to give a series of 18 metal complexes in good yields and satisfactory purities. Screening of these oxorhenium coordinates as antagonists of integrins αVβ3, αIIbβ3 and αVβ5 led to the identification of 3 bioactive compounds that exhibit submicromolar affinities for the 3 integrins. Preliminary studies showed that the corresponding oxotechnetium complexes are stable in mice plasma and therefore could be proposed for the molecular imaging of pathologies that overexpress integrins αVβ3 and αVβ5.

Domaines

Chimie

Dates et versions

hal-03634393 , version 1 (07-04-2022)

Identifiants

Citer

Julien Le Gal, Marta Gonera, Marie-Anne Lelait, Denis Servent, Christophe Dugave. Chelate oxorhenium to assemble new integrin antagonists. Journal of Inorganic Biochemistry, 2011, 105 (6), pp.880-886. ⟨10.1016/j.jinorgbio.2011.03.008⟩. ⟨hal-03634393⟩
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