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Improving Antisense Oligonucleotide Binding to Human Serum Albumin: Dramatic Effect of Ibuprofen Conjugation
Author(s) -
Manoharan Muthiah,
Inamati Gopal B.,
Lesnik Elena A.,
Sioufi Namir B.,
Freier Susan M.
Publication year - 2002
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/1439-7633(20021202)3:12<1257::aid-cbic1257>3.0.co;2-2
Subject(s) - oligonucleotide , ibuprofen , albumin , chemistry , human albumin , serum albumin , plasma protein binding , human serum albumin , biochemistry , combinatorial chemistry , dna , biology , pharmacology
The next generation: The effect of ibuprofen conjugation to hydrophilic second‐generation antisense oligonucleotides on the binding affinity for serum albumin has been evaluated. The conjugation (see structure) offers a chemical solution for improving the pharmacokinetic distribution of 2′‐ O ‐methoxyethyl phosphodiester (PO) derivatives (RNA analogues). These compounds could provide an alternative solution to the nonspecific toxic side effects displayed by first‐generation 2′‐deoxyphosphorothioate (PS) antisense oligonucleotides.