Lee Damhee, Lee Dongsun, Won Kyujeong, Kim Suhyun, Kim Youngjun
Department of Medicinal Bioscience, Nanotechnology Research Center, Konkuk University, Chungju 27478, Republic of Korea.
Life (Basel). 2024 Dec 20;14(12):1686. doi: 10.3390/life14121686.
This study identified several inhibitors of Starch Excess 4 (SEX4), an enzyme in plants' starch decomposition. Our research aims to inhibit starch breakdown by SEX4 with its potential to significantly impact food security, leading to starch accumulation in plants such as potatoes, sweet potatoes, and significant crops like grains and rice. We recognized potential candidates by screening approximately 1840 chemical compounds using the phosphatase assay against NPP. The IC values of the selected candidates were determined through the NPP assay and the amylopectin assay, while K values were confirmed by calculating V, K, and values. Finally, we compared the IC values of Like Sex Four 2 (LSF2) and SEX4 to assess their selectivity. This screening yielded several potential inhibitory compounds, with F05 showing promise in the NPP assay and F09 and G11 in the amylopectin assay, all demonstrating more selectivity for SEX4 than LSF2. Consequently, we identified seven chemicals as promising inhibitor compounds, offering potential for future research and applications. However, further quantitative structure-activity relationship studies and the practical application to test selected compounds on crops will be necessary in future research.
本研究鉴定出了几种淀粉过量4（SEX4）的抑制剂，SEX4是植物淀粉分解过程中的一种酶。我们的研究旨在通过抑制SEX4的淀粉分解作用，因为其有潜力显著影响粮食安全，从而使土豆、红薯等植物以及谷物和水稻等重要作物中积累淀粉。我们通过针对对硝基苯磷酸酯（NPP）的磷酸酶测定法筛选了约1840种化合物，从而识别出潜在的候选物。通过NPP测定法和支链淀粉测定法确定所选候选物的IC值，同时通过计算V、K和 值来确认K值。最后，我们比较了类SEX4蛋白2（LSF2）和SEX4的IC值以评估它们的选择性。该筛选产生了几种潜在的抑制性化合物，F05在NPP测定中显示出前景，F09和G11在支链淀粉测定中显示出前景，所有这些化合物对SEX4的选择性均高于LSF2。因此，我们确定了七种化学物质为有前景的抑制剂化合物，为未来的研究和应用提供了潜力。然而，未来的研究有必要进一步开展定量构效关系研究，并将所选化合物应用于作物进行实际测试。
