Antisense research and applications.

Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

Antisense research and applications.

Antisense Research and Applications. Crooke ST, Lebleu B, eds. Boca Raton, FL, CRC Press, 579 p., 1993.. Unique Identifier : AIDSLINE ICDB/95615469
Anonymous; No affiliation given

Abstract: It has only recently become accepted that oligonucleotides might have therapeutic utility. Although new to human therapeutics, small, diffusible, untranslated RNA transcripts, termed antisense RNAs, that pair to specific target RNAs at regions of complementarity, occur universally among prokaryotes and eukaryotes, serving to control target RNA function and expression. The antisense oligonucleotides finding therapeutic application are for the most part chemically modified and rendered resistant to nucleases; they also operate by sequence-specific binding to preselected cellular nucleic acids as their target. This book contains chapters by 56 international collaborating authors who survey the whole field of antisense research and its potential applications. The 32 chapters are grouped into nine sections: an introduction to the history and context of antisense drug discovery; a consideration of nucleic acid structure and function in relation to antisense drugs, including discussion of the 5' cap and the use of ribozymes; antisense RNAs occurring naturally; medicinal chemistry of oligonucleotides; first generation analogs, including methylphosphonates, phosphorothioates, alpha-oligonucleotides, P-chiral analogs, and other reactive derivatives; newer analogs, including those involving heterocyclic base modification, peptide nucleic acids, 2'-O-alkyl derivatives and various designer approaches; mechanisms of action of current synthetic oligonucleotides, which includes a discussion of higher order structures of HIV-1 RNAs as sites of drug action; pharmacokinetics and toxicology, largely of the major first generation drugs; and activities of current antisense drugs, which includes two chapters on antiviral action, one on their application in inflammation research and therapeutics, and one on inhibition of proto-oncogene expression in leukemic cells, which appears the CANCERLIT data base with the accession number ICDB/95615470. There is a subject index.

Keywords: Antineoplastic Agents/CHEMISTRY/PHARMACOKINETICS/*THERAPEUTIC USE Antiviral Agents/CHEMISTRY/PHARMACOKINETICS/*THERAPEUTIC USE Drug Design Human Oligonucleotides, Antisense/CHEMISTRY/PHARMACOKINETICS/ *THERAPEUTIC USE MONOGRAPH
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M9570947

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