ADMET, QSAR and Docking studies to predict the activity of tyrosinase-derived medications inhibitors based on computational techniques

基于计算技术,通过ADMET、QSAR和分子对接研究预测酪氨酸酶衍生药物抑制剂的活性

阅读:1

Abstract

The tyrosinase enzyme plays a pivotal role in melanin pigment production; however, heightened tyrosinase activity can lead to undesired pigmentation. Consequently, inhibiting this enzyme's function stands as a critical research avenue for devising effective strategies to mitigate pigmentation issues. This study aimed to forecast the biological activity of chemical compounds capable of inhibiting tyrosinase and elucidate pivotal elements influencing this enzyme's activity. To achieve this goal, we employed computational techniques to construct a model predicting the biological activity of these compounds. Initially, we identified 27 tyrosinase inhibitors from previous studies. Subsequently, after performing ADMET studies, we extracted and pre-processed the significant features of each compound to develop a Stepwise-MLR model. Moreover, with the help of this model, we were able to identify the most influential and novel structural features that directly affect enzyme activity and determine the importance factor of each feature. Furthermore, all derived inhibitors with evaluated inhibition constants were docked to the active site of target tyrosinase to investigate the binding mode of the compounds. Docking analysis indicated T1 as the most stable compound with a binding energy of -8.00 kcal/mol. T1 as the most active compound identified through these computational studies can be applied as a prospective tyrosinase inhibitor. The implications of our findings extend to the development of new therapies for pigmentation disorders, notably within the cosmetic and dermatological sectors.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。