Aptamers as inhibitors of target proteins.
BACKGROUND
Aptamers as inhibitors of proteins in therapeutic applications offer great advantages over their antibody counterparts and the promise to be developed into the next generation therapeutic agents. However, the control of aptamer intellectual property (IP) by two major players has made aptamers an area difficult to operate and often off-putting for academic and commercial organisations. Yet, their great potential is keeping aptamers at the research forefront, with one aptamer in the clinic and various at different stages of clinical trials.


OBJECTIVE
To provide a comprehensive review of the aptamer IP landscape and the issues associated with aptamer therapeutics against protein targets.


METHODS
Extensive review of the scientific and patent literature.


CONCLUSIONS
Following our experience in developing, patenting and commercialising our aptamers against MUC1 and an extensive review of the literature, we have identified a variety of issues pertaining to the development of aptamers against protein targets for therapeutic applications, their patenting and granting of patents, the original IP holders and their policy, as well as the current market and traits. Despite a slow start, aptamers have been developed against various therapeutic proteins and offer the promise of providing a novel generation of therapeutic entities with a variety of applications.
Missailidis
S
S
The Open University, Department of Chemistry and Analytical Sciences, Walton Hall, Milton Keynes, MK7 6AA, UK. s.missailidis@open.ac.uk
Hardy
A
A
D000954:Antigens, Surface; D052157:Aptamers, Nucleotide / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D043425:Glutamate Carboxypeptidase II / Q000037:antagonists & inhibitors; D006801:Humans; D010330:Patents as Topic; D010982:Platelet-Derived Growth Factor / Q000037:antagonists & inhibitors; D011506:Proteins / Q000037:antagonists & inhibitors*; D052156:SELEX Aptamer Technique; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors
D000954:Antigens, Surface; D052157:Aptamers, Nucleotide; D010982:Platelet-Derived Growth Factor; D011506:Proteins; D042461:Vascular Endothelial Growth Factor A; C473848:FOLH1 protein, human; D043425:Glutamate Carboxypeptidase II