Synthesis of new poly-acridine and binding mode with DNA.
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Accession number;02A0304362
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| Title;Synthesis of new poly-acridine and binding mode with DNA. |
| Author;
TAKENAKA SHIGEORI
(Kyushu Univ., Grad. Sch.)
UEYAMA HIROYUKI
(Kyushu Univ., Grad. Sch.)
WAKI MICHINORI
(Kyushu Univ., Grad. Sch.)
TAKAGI MAKOTO
(Kyushu Univ., Grad. Sch.)
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Journal Title;Abstracts. Symposium on Biofunctional Chemistry
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Journal Code:L0836A
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ISSN:
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VOL.16th;NO.;PAGE.12-13(2001)
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| Figure&Table&Reference; |
| Pub. Country;Japan |
| Language;Japanese |
| Abstract;Bis-, tris-, tetrakis-, and pentakis-acridinyl(Acr) peptides 2-5 were synthesized from Fomc-Lys(Acr)-OH and Fmoc- Lys(Boc)-OH with the peptide synthesizer. The molar absorptivity of these peptides saturated with an increase in the number of the acridinyl unit in the peptide, suggesting intramolecular stacking of the acridinyl units. It was found from Scatchard analysis by means of spectrophotometry that all the peptides can bind to double stranded DNA with very high affinity even under high salt conditions (0.4M NaCl). Tetrakis-acridinyl peptides 4 binds to double stranded DNA with a very large affinity constant, which is 103-times larger than that of 1. Spectrophotometric and hydrodynamic studies suggested that all of the acridinyl parts of 4 contribute to the intercalating interaction for the DNA binding. Moreover, the logarithmic binding constant of 2-4 increased in proportion to the number of the acridinyl unit in the peptide. This result suggested effective poly-intercalation of all the acridinyl units into double stranded DNA. (author abst.) |
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