In vivo uses of aptamers selected against cell surface biomarkers for therapy and molecular imaging

Nucleic acid Aptamers are ligands that are selected by a process of molecular evolution to bind with high affinities and specificities to a specific target. Recently, an increasing number of aptamers have been selected against biomarkers expressed at the surface of human cells or infectious pathogens. This class of targets, mostly proteins, is associated with several pathologies including cancer, inflammation and infection diseases. Several of these cell surface specific aptamers were tested in vivo as drugs or as targeting agents for nanocarriers, siRNA or contrast agents. Strikingly, they were used to develop a wide variety of new treatments or new approaches for molecular imaging and they were also able to improve current therapies such as chemotherapy, radiotherapy or immunotherapy. This review presents these different applications and the different studies conducted in vivo with this class of aptamers, predominantly in pre-clinical models.

Graphical abstractFigure optionsDownload full-size imageDownload high-quality image (165 K)Download as PowerPoint slideHighlights► We review the in vivo use of aptamers selected against cell surface biomarkers. ► They were evaluated in different pathologies, mostly in pre-clinical models. ► Aptamers have been used directly as neutralizing or agonistic drugs. ► Aptamers have been used as addressing agents of nanoparticles or siRNA. ► Aptamers have been used for therapy, in vivo imaging or theranostic.