Aptamers: An Emerging Class of Therapeutics

Author:

Nimjee Shahid M.12,Rusconi Christopher P.23,Sullenger Bruce A.12

Affiliation:

1. 1 University Program of Genetics, Duke University Medical Center, Durham, North Carolina 27710;

2. 2 Department of Surgery, Division of Experimental Surgery, Duke University Medical Center, Durham, North Carolina 27710;

3. 3 Regado Biosciences, Inc., Research Triangle Park, North Carolina 27709;

Abstract

Numerous nucleic acid ligands, also termed decoys or aptamers, have been developed during the past 15 years that can inhibit the activity of many pathogenic proteins. Two of them, Macugen and E2F decoy, are in phase III clinical trials. Several properties of aptamers make them an attractive class of therapeutic compounds. Their affinity and specificity for a given protein make it possible to isolate a ligand to virtually any target, and adjusting their bioavailability expands their clinical utility. The ability to develop aptamers that retain activity in multiple organisms facilitates preclinical development. Antidote control of aptamer activity enables safe, tightly controlled therapeutics. Aptamers may prove useful in the treatment of a wide variety of human maladies, including infectious diseases, cancer, and cardiovascular disease. We review the observations that facilitated the development of this emerging class of therapeutics, summarize progress to date, and speculate on the eventual utility of such agents in the clinic.

Publisher

Annual Reviews

Subject

General Biochemistry, Genetics and Molecular Biology,General Medicine

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