Long Y Q, Lee S L, Lin C Y, Enyedy I J, Wang S, Li P, Dickson R B, Roller P P
Laboratory of Medicinal Chemistry, National Cancer Institute, NIH, FCRDC, 376/208, PO Box B, Frederick, MD 21702, USA.
Bioorg Med Chem Lett. 2001 Sep 17;11(18):2515-9. doi: 10.1016/s0960-894x(01)00493-0.
We report here the synthesis of a 14-amino acid long bicyclic peptide, previously isolated from sunflower seeds. This peptide, termed sunflower trypsin inhibitor (SFTI-1), is one of the most potent naturally occurring small-molecule trypsin inhibitors. In addition to inhibiting trypsin, the synthetic SFTI-1 is also a very potent inhibitor, with a K(i) of 0.92nM, of the recently identified epithelial serine protease, termed 'matriptase'.
我们在此报告一种14个氨基酸长的双环肽的合成，该双环肽先前是从向日葵种子中分离出来的。这种肽被称为向日葵胰蛋白酶抑制剂（SFTI-1），是自然界中最有效的小分子胰蛋白酶抑制剂之一。除了抑制胰蛋白酶外，合成的SFTI-1还是一种非常有效的抑制剂，对最近鉴定出的上皮丝氨酸蛋白酶“matriptase”的抑制常数（K(i)）为0.92纳摩尔。
