Corey D R, Phillips M A
Department of Pharmacology, University of Texas Southwestern Medical Center at Dallas.
Proc Natl Acad Sci U S A. 1994 May 10;91(10):4106-9. doi: 10.1073/pnas.91.10.4106.
A recent report [Atassi, M. Z. and Manshouri, T. (1993) Proc. Natl. Acad. Sci. USA 90, 8282-8286] described the design and synthesis of two 29-amino acid cyclic peptides that were reported to hydrolyze both ester and amide bonds with chymotrypsin-like or trypsin-like specificity. We have synthesized the trypsin-mimic peptide (TrPepz) and detect no activity toward either ester or peptide substrates. The same result was independently obtained by Wells et al. [Wells, J. A., Fairbrother, W. J., Otlewski, J., Laskowski, M., Jr., & Burnier, J. (1994) Proc. Natl. Acad. Sci. USA 91, 4110-4114.] Additionally, we found that Atassi and Manshouri failed to obtain accurate kinetic constants for trypsin- and chymotrypsin-catalyzed ester hydrolysis because the high concentrations of trypsin and chymotrypsin that they report using would have prevented evaluation of initial rates. These findings are incompatible with the claims, reported by Atassi and Manshouri, that TrPepz has trypsin-like activity.
最近的一份报告[阿塔西，M. Z. 和曼苏里，T.（1993年）《美国国家科学院院刊》90，8282 - 8286]描述了两种29个氨基酸的环肽的设计与合成，据报道这两种环肽能以类似胰凝乳蛋白酶或类似胰蛋白酶的特异性水解酯键和酰胺键。我们合成了类胰蛋白酶肽（TrPepz），但未检测到其对酯底物或肽底物有任何活性。韦尔斯等人[韦尔斯，J. A.，费尔布拉泽，W. J.，奥特列夫斯基，J.，拉斯科夫斯基，M.，Jr.，& 伯尼尔，J.（1994年）《美国国家科学院院刊》91，4110 - 4114]独立得到了相同的结果。此外，我们发现阿塔西和曼苏里未能获得胰蛋白酶和胰凝乳蛋白酶催化酯水解的准确动力学常数，因为他们报告中使用的高浓度胰蛋白酶和胰凝乳蛋白酶会阻碍对初始速率的评估。这些发现与阿塔西和曼苏里所声称的TrPepz具有类胰蛋白酶活性不相符。
