title: Aptamers as Therapeutics.
abstract: Aptamers are single-stranded nucleic acid molecules that bind to and inhibit proteins and are commonly produced by systematic evolution of ligands by exponential enrichment (SELEX). Aptamers undergo extensive pharmacological revision, which alters affinity, specificity, and therapeutic half-life, tailoring each drug for a specific clinical need. The first therapeutic aptamer was described 25 years ago. Thus far, one aptamer has been approved for clinical use, and numerous others are in preclinical or clinical development. This review presents a short history of aptamers and SELEX, describes their pharmacological development and optimization, and reviews potential treatment of diseases including visual disorders, thrombosis, and cancer.
authors.affiliation: Department of Neurological Surgery, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210; email: shahid.nimjee@osumc.edu.
authors.forename: Shahid M
authors.initials: SM
authors.lastname: Nimjee
authors.affiliation: Department of Surgery, Duke University Medical Center, Durham, North Carolina 27705; email: rebekah.white@duke.edu.
authors.forename: Rebekah R
authors.initials: RR
authors.lastname: White
authors.affiliation: Department of Medicine, University of Cincinnati Medical Center, Cincinnati, Ohio 45267; email: beckerrc@ucmail.uc.edu.
authors.forename: Richard C
authors.initials: RC
authors.lastname: Becker
authors.affiliation: Department of Surgery, Duke University Medical Center, Durham, North Carolina 27705; email: rebekah.white@duke.edu.|Duke Translational Research Institute, Duke University Medical Center, Durham, North Carolina 27705; email: bruce.sullenger@duke.edu.
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Sullenger
mesh_terms: D000818:Animals; D052157:Aptamers, Nucleotide / Q000008:administration & dosage* / Q000235:genetics* / Q000378:metabolism; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D016032:Randomized Controlled Trials as Topic / Q000379:methods; D052156:SELEX Aptamer Technique / Q000379:methods* / Q000639:trends; D014786:Vision Disorders / Q000188:drug therapy / Q000378:metabolism
chemical_list: D052157:Aptamers, Nucleotide; C495058:pegaptanib
keywords: SELEX; antidote; aptamer; pharmacology; therapeutics