| Synthesis of N-acetyl-D-galactosamine and folic acid conjugated ribozymes. | |
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MedLine Citation:
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PMID: 12236789 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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To evaluate potential improvement in tissue specific targeting and cellular uptake of therapeutic ribozymes, we have developed three new phosphoramidite reagents. These reagents can be used in automated solid-phase synthesis to produce oligonucleotide conjugates containing N-acetyl-D-galactosamine (targeting hepatocytes) and folic acid (targeting tumor). N-Acetyl-D-galactosamine was attached through a linker to both 2'-amino-2'-deoxyuridine and D-threoninol scaffolds, and these conjugates were converted to phosphoramidite building blocks. Incorporation of a D-threoninol-based monomer into ribozymes provided multiply labeled ribozyme conjugates. Attachment of the fully protected pteroic acid to the D-threoninol-6-aminocaproyl-L-glutamic acid construct afforded the folic acid conjugate, which was converted into the phosphoramidite and incorporated onto the 5'-end of the ribozyme. |
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Authors:
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Jasenka Matulic-Adamic; Vladimir Serebryany; Peter Haeberli; Victor R Mokler; Leonid Beigelman |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Bioconjugate chemistry Volume: 13 ISSN: 1043-1802 ISO Abbreviation: Bioconjug. Chem. Publication Date: 2002 Sep-Oct |
Date Detail:
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Created Date: 2002-09-18 Completed Date: 2003-06-16 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9010319 Medline TA: Bioconjug Chem Country: United States |
Other Details:
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Languages: eng Pagination: 1071-8 Citation Subset: IM |
Affiliation:
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Department of Chemistry & Biochemistry, Ribozyme Pharmaceuticals, Inc., 2950 Wilderness Place, Boulder, Colorado 80301, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Acetylgalactosamine
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chemistry Antineoplastic Agents / chemical synthesis Cross-Linking Reagents / chemistry Drug Delivery Systems / methods* Folic Acid / chemistry Oligonucleotides / chemical synthesis Organophosphorus Compounds / chemistry RNA, Catalytic / administration & dosage*, chemistry |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Cross-Linking Reagents; 0/Oligonucleotides; 0/Organophosphorus Compounds; 0/RNA, Catalytic; 0/phosphoramidite; 31022-50-1/Acetylgalactosamine; 59-30-3/Folic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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