A BIOACTIVE FULLERENE PEPTIDE

被引:120
作者
TONIOLO, C
BIANCO, A
MAGGINI, M
SCORRANO, G
PRATO, M
MARASTONI, M
TOMATIS, R
SPISANI, S
PALU, G
BLAIR, ED
机构
[1] UNIV PADUA,CNR,CTR MECCANISMI REAZIONI ORGAN,DIPARTIMENTO CHIM ORGAN,I-35131 PADUA,ITALY
[2] UNIV TRIESTE,DIPARTIMENTO SCI FARMACEUT,I-34127 TRIESTE,ITALY
[3] UNIV FERRARA,DIPARTIMENTO SCI FARMACEUT,I-44100 FERRARA,ITALY
[4] UNIV FERRARA,DIPARTMENTO BIOCHIM & BIOL MOLEC,I-44100 FERRARA,ITALY
[5] UNIV PADUA,IST MICROBIOL,I-35100 PADUA,ITALY
[6] WELLCOME RES LABS,DEPT MOLEC SCI,BECKENHAM BR3 3BS,KENT,ENGLAND
关键词
D O I
10.1021/jm00052a015
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The highly hydrophobic C-60 (buckminsterfullerene) was water solubilized by covalently linking the synthon 1,2-dihydro-1,2-methanofullerene [60]-61-carboxylic acid to the alpha-amino group of the hydrophilic 4-8 sequence of peptide T, known to display potent human monocyte chemotaxis. The resulting compound, characterized by a variety of analytical techniques, including a UV spectrum in aqueous solution, exhibits remarkable chemotactic potency, comparable to that of the parent pentapeptide. Furthermore, this fullerene-peptide conjugate inhibits, albeit weakly, HIV-1 protease.
引用
收藏
页码:4558 / 4562
页数:5
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