Toniolo C, Bianco A, Maggini M, Scorrano G, Prato M, Marastoni M, Tomatis R, Spisani S, Palú G, Blair E D
Dipartimento di Chimica Organica, Universitá di Padova, Italy.
J Med Chem. 1994 Dec 23;37(26):4558-62. doi: 10.1021/jm00052a015.
The highly hydrophobic C60 (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.
通过将合成子1,2 - 二氢 - 1,2 - 亚甲基富勒烯[60] - 61 - 羧酸与已知具有强大人单核细胞趋化性的亲水性肽T的4 - 8序列的α - 氨基共价连接，使高度疏水的C60（巴基球富勒烯）实现了水溶性。通过包括水溶液中的紫外光谱在内的多种分析技术对所得化合物进行表征，其表现出显著的趋化效力，与母体五肽相当。此外，这种富勒烯 - 肽缀合物虽然抑制作用较弱，但能抑制HIV - 1蛋白酶。
