Department of Animal Food Technology, Faculty of Food Science and Biotechnology, University of Life Sciences in Lublin, Skromna 8, 20-704 Lublin, Poland.
Curr Issues Mol Biol. 2021 Sep 27;43(3):1335-1349. doi: 10.3390/cimb43030095.
Peptidyl peptidase IV (DPP-IV) is a pharmacotherapeutic target in type 2 diabetes, and inhibitors of this enzyme are an important class of drugs for the treatment of type 2 diabetes. In the present study, peptides (<7 kDa) isolated from dry-cured pork loins after pepsin and pancreatin hydrolysis were identified by mass spectrometry and tested as potential inhibitors of DPP-IV by the in silico method. Two peptides, namely WTIAVPGPPHS from myomesin (water-soluble fraction, A = 0.9091) and FKRPPL from troponin (salt-soluble fraction, A = 0.8333), were selected as the most promising inhibitors of DPP-IV. Both peptides were subjected to ADMET analysis. Fragments of these peptides showed promising drug-likeness properties as well as favorable absorption, distribution, metabolism, excretion, and toxicity functions, suggesting that they are novel leads in the development of DPP-IV inhibitors from food.
肽基肽酶 IV（DPP-IV）是 2 型糖尿病的药物治疗靶点，该酶的抑制剂是治疗 2 型糖尿病的一类重要药物。本研究采用胃蛋白酶和胰蛋白酶水解干腌猪里脊肉，通过质谱鉴定得到<7 kDa 的肽段，并用计算机方法筛选这些肽段作为 DPP-IV 的潜在抑制剂。两种肽段，即肌联蛋白（水溶性部分，A = 0.9091）中的 WTIAVPGPPHS 和肌钙蛋白（盐溶性部分，A = 0.8333）中的 FKRPPL，被选为最有希望的 DPP-IV 抑制剂。对这两种肽段进行了 ADMET 分析。这些肽段的片段显示出有希望的类药性特征，以及良好的吸收、分布、代谢、排泄和毒性功能，表明它们是开发 DPP-IV 抑制剂的新型食品先导物。
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