Cruz Patricia G, Daranas Antonio Hernández, Fernández José J, Norte Manuel
Instituto Universitario de Bio-OrgAnica Antonio GonzAlez, Universidad de La Laguna, Astrofísico Francisco SAnchez 2, 38206 La Laguna, Tenerife, Spain.
Org Lett. 2007 Aug 2;9(16):3045-8. doi: 10.1021/ol071099i. Epub 2007 Jul 14.
A new protein phosphatase inhibitor, 19-epi-okadaic acid, was isolated from the marine dinoflagellate Prorocentrum belizeanum. Its structure and conformation in solution has been determined, and important differences were found when compared with the lead compound okadaic acid. The new metabolite showed nanomolar activities, and its selectivity for PP2A versus PP1 surpasses that shown by okadaic acid 10-fold, making it one of the most selective inhibitors of this class.
一种新的蛋白磷酸酶抑制剂，19-表冈田酸，是从海洋双鞭毛藻伯利兹原甲藻中分离出来的。已确定其在溶液中的结构和构象，与先导化合物冈田酸相比发现了重要差异。这种新的代谢产物显示出纳摩尔活性，其对PP2A相对于PP1的选择性比冈田酸高出10倍，使其成为这类中最具选择性的抑制剂之一。
