Functionalisation of aptamers for the development of effective cancer therapeutics

Makwana, Vaidehi; Khan, Huma; Courtenay-Luck, Nigel and Missailidis, Sotiris (2008). Functionalisation of aptamers for the development of effective cancer therapeutics. Anticancer Research, 28(5C) pp. 3394–3395.

URL: http://ar.iiarjournals.org/content/28/5C

Abstract

Aptamers, short oligonucleotide therapeutic, diagnostic and imaging agents, possess great affinity and selectivity for their targets. However, they are limited in terms of application due to their rapid renal clearance and degradation from nucleases in the blood. Thus, it is often necessary to incorporate appropriate modifications for achieving their full potential. Aptamer labelling with appropriate fluorescent moieties or radioisotopes can confer diagnostic and imaging potential, respectively. Various chemical modifications, such as PEGylation, can improve their pharmacokinetic properties and retain aptamers longer in circulation, making them suitable for therapeutic applications. We now present a range of chemical modifications on our tumour-targeting aptamers that have allowed us to develop them as diagnostic or therapeutic agents.

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