Synthesis and binding properties of conjugates between oligodeoxynucleotides and daunorubicin derivatives | Zendy

Anna Garbesi | Zendy

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Synthesis and binding properties of conjugates between oligodeoxynucleotides and daunorubicin derivatives

Author(s) -

Anna Garbesi

Publication year - 1997

Publication title -

nucleic acids research

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 9.008

H-Index - 537

eISSN - 1362-4954

pISSN - 0305-1048

DOI - 10.1093/nar/25.11.2121

Subject(s) - conjugate , intercalation (chemistry) , dna , biology , moiety , oligonucleotide , triple helix , daunorubicin , chromophore , stereochemistry , anthracycline , combinatorial chemistry , anthraquinone , biochemistry , chemistry , photochemistry , genetics , inorganic chemistry , mathematical analysis , mathematics , organic chemistry , cancer , leukemia , breast cancer

Conjugation of an anthracycline to a triplex-forming oligonucleotide (TFO) allows delivery of this drug to a specific DNA site, preserving the intercalation geometry of this class of anticancer agents. Conjugate 11, in which the TFO is linked via a hexamethylene bridge to the O-4 on the D ring of the anthraquinone moiety, affords the most stable triple helix, through intercalation of the planar chromophore between DNA bases and binding of both the TFO and the amino sugar to the major and the minor groove respectively.

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