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Dipeptidyl-peptidase IV (DPP IV/CD26)-activated prodrugs: A successful strategy for improving water solubility and oral bioavailability

AutorVelázquez, Sonsoles ; Castro, Sonia de ; Diez-Torrubia, Alberto ; Balzarini, Jan; Camarasa Rius, María José
Palabras clavestability
water solubility
oral bioavailability
hydroxy-containing drugs
Amine-containing drugs
CD26 prodrugs
dipeptidyl peptidase IV
Fecha de publicación2015
EditorBentham Science Publishers
CitaciónCurrent Medicinal Chemistry 22 (8) : 1041-1054 (2015)
ResumenIn the search of novel enzyme-based prodrug approaches to improve pharmacological properties of therapeutic drugs such as solubility and bioavailability, dipeptidyl-peptidase IV (DPP IV, also termed as CD26) enzyme activity provides a previously unexplored successful prodrug strategy. This review covers key aspects of the enzyme useful for the design of CD26-directed prodrugs. The proof-of-concept of this prodrug technology is provided for amine-containing agents by directly linking appropriate di- (or oligo)peptide moieties to a free amino group of a non-peptidic drug through an amide bond which is specifically hydrolized by DPP IV/CD26. Special emphasis is also made in discussing the design and synthesis of more elaborated tripartite prodrug systems, for further extension of the strategy to hydroxy-containing drugs. The application of this technology to improve water solubility and oral bioavailability of prominent examples of antiviral nucleosides is highlighted.
Identificadoresissn: 0929-8673
e-issn: 1875-533X
Aparece en las colecciones: (IQM) Artículos
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