期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 21, 页码 9645-9667出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00551
关键词
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Oligonucleotide-based therapeutics have made rapid progress in the clinic for treatment of a variety of disease indications. Unmodified oligonucleotides are polyanionic macromolecules with poor drug-like properties. Over the past two decades, medicinal chemists have identified a number of chemical modification and conjugation strategies which can improve the nuclease stability, RNA-binding affinity, and pharmacokinetic properties of oligonucleotides for therapeutic applications. In this perspective, we present a summary of the most commonly used nucleobase, sugar and backbone modification, and conjugation strategies used in oligonucleotide medicinal chemistry.
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