An anticancer conjugate, which comprises a fusion protein comprising domain (a), which is the functional fragment of a sequence of soluble human TRAIL (hTRAIL) protein beginning with an amino acid at a position not lower than hTRAIL95 or a sequence having at least 70% identity with said functional fragment, domain (b) which is the sequence of an effector peptide having proapoptotic, antiangiogenic, antiproliferative or pore forming activity, and conjugation domain (d) for attachment of a chemical compound selected from the group consisting of the sequences Cys Ala Ala Ala Cys Ala Ala Cys and Cys Ala Ala Cys Ala Ala Ala Cys, and a molecule of a chemical compound Z having antiblastic activity, which is attached to said conjugation domain (d) of said fusion protein directly or via a conjugation linker L.
一种抗癌结合物,包括融合蛋白,该融合蛋白包括以下部分:(a)功能性片段,该片段是以不低于hTRAIL95位置的氨基酸开始的可溶性人类TRAIL(hTRAIL)蛋白序列的片段,或者具有与该功能性片段至少70%同源性的序列;(b)是具有促凋亡、抗血管生成、抗增殖或形成孔活性的效应肽序列;以及(d)用于连接来自以下序列的化学化合物的结合结构域,该序列包括Cys Ala Ala Ala Cys Ala Ala Cys和Cys Ala Ala Cys Ala Ala Ala Cys,以及具有抗肿瘤活性的化学化合物Z的分子,该分子附着在所述融合蛋白的结合结构域(d)上,直接或通过结合连接物L连接。
Synthesis of Amaminol B
作者:Mathias Christmann、Wiebke Jacobs
DOI:10.1055/s-2007-1000935
日期:2008.1
The synthesis of the cytotoxic marine natural product amaminol B is described. Key steps include an organocatalytic intramolecular Diels-Alder reaction, an HWE olefination and a diastereoselective ketone reduction.
本文介绍了具有细胞毒性的海洋天然产物氨基醇 B 的合成过程。关键步骤包括有机催化分子内 Diels-Alder 反应、HWE 烯化反应和非对映选择性酮还原反应。
Amaminols A and B, new bicyclic amino alcohols from an unidentified tunicate of the family Polyclinidae
作者:Noriko U. Sata、Nobuhiro Fusetani
DOI:10.1016/s0040-4039(99)02098-5
日期:2000.1
Two new cytotoxic amino alcohols, amaminols A and B, have been isolated from an unidentified tunicate of the family Polyclinidae. Their structures including stereochemistry were elucidated by spectroscopic and chemical methods. Both compounds were cytotoxic against P388 murine leukemia cells.