| RRC ID |
42755
|
| 著者 |
Sasaki S, Bando T, Minoshima M, Shimizu T, Shinohara K, Takaoka T, Sugiyama H.
|
| タイトル |
Sequence-specific alkylation of double-strand human telomere repeat sequence by pyrrole-imidazole polyamides with indole linkers.
|
| ジャーナル |
J Am Chem Soc
|
| Abstract |
We designed and synthesized pyrrole (Py)-imidazole (Im) hairpin polyamide 1-(chloromethyl)-5-hydroxy-1,2-dihydro-3H-benz[e]indole (seco-CBI) conjugates 1 and 2, which target both strands of the double-stranded region of the human telomere repeat sequences, 5'-d(TTAGGG)(n)-3'/5'-d(CCCTAA)(n)-3'. High-resolution denaturing polyacrylamide gel electrophoresis demonstrated that conjugates 1 and 2 alkylated DNA at the 3' A of 5'-ACCCTA-3' and 5'-AGGGTTA-3', respectively. Cytotoxicities of conjugates 1 and 2 were evaluated using 39 human cancer cell lines; averages of log IC(50) values for conjugates 1 and 2 were -6.96 (110 nM) and -7.24 (57.5 nM), respectively. Conjugates 1 and 2 have potential as antitumor drugs capable of targeting telomere repeat sequence.
|
| 巻・号 |
128(37)
|
| ページ |
12162-8
|
| 公開日 |
2006-9-20
|
| DOI |
10.1021/ja0626584
|
| PMID |
16967966
|
| MeSH |
Alkylation
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Base Sequence
Cell Line, Tumor
Electrophoresis, Polyacrylamide Gel
Humans
Indoles / chemical synthesis
Indoles / chemistry*
Indoles / pharmacology*
Molecular Sequence Data
Neoplasms / genetics
Neoplasms / metabolism
Pyrroles / chemical synthesis
Pyrroles / chemistry*
Pyrroles / pharmacology*
Repetitive Sequences, Nucleic Acid
Substrate Specificity
Telomere / chemistry
Telomere / genetics
Telomere / metabolism*
|
| IF |
14.612
|
| 引用数 |
28
|
|
WOS 分野
|
CHEMISTRY, MULTIDISCIPLINARY
|
| リソース情報 |
| ヒト・動物細胞 |
MRC-5
NHSF46(RCB0162) |
