Institute of Theoretical Chemistry, Jilin University, Changchun 130061, China.
Collaborative Innovation Center of Henan Grain Crops, National Key Laboratory of Wheat and Maize Crop Science, College of Plant Protection, Henan Agricultural University, Zhengzhou 450002, China.
Molecules. 2023 Oct 17;28(20):7140. doi: 10.3390/molecules28207140.
The drug development process suffers from low success rates and requires expensive and time-consuming procedures. The traditional one drug-one target paradigm is often inadequate to treat multifactorial diseases. Multitarget drugs may potentially address problems such as adverse reactions to drugs. With the aim to discover a multitarget potential inhibitor for B-cell lymphoma treatment, herein, we developed a general pipeline combining machine learning, the interpretable model SHapley Additive exPlanation (SHAP), and molecular dynamics simulations to predict active compounds and fragments. Bruton's tyrosine kinase (BTK) and Janus kinase 3 (JAK3) are popular synergistic targets for B-cell lymphoma. We used this pipeline approach to identify prospective potential dual inhibitors from a natural product database and screened three candidate inhibitors with acceptable drug absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties. Ultimately, the compound CNP0266747 with specialized binding conformations that exhibited potential binding free energy against BTK and JAK3 was selected as the optimum choice. Furthermore, we also identified key residues and fingerprint features of this dual-target inhibitor of BTK and JAK3.
药物研发过程成功率低,需要昂贵且耗时的程序。传统的单药单靶标模式往往不足以治疗多因素疾病。多靶标药物可能潜在地解决药物不良反应等问题。为了发现一种用于治疗 B 细胞淋巴瘤的多靶标潜在抑制剂,我们在此开发了一个结合机器学习、可解释模型 SHapley Additive exPlanation (SHAP) 和分子动力学模拟的通用管道,以预测活性化合物和片段。布鲁顿酪氨酸激酶 (BTK) 和 Janus 激酶 3 (JAK3) 是 B 细胞淋巴瘤的热门协同靶标。我们使用该流水线方法从天然产物数据库中识别出有前途的潜在双重抑制剂,并筛选出三种具有可接受的药物吸收、分布、代谢、排泄和毒性 (ADMET) 特性的候选抑制剂。最终,化合物 CNP0266747 被选为最佳选择,该化合物具有针对 BTK 和 JAK3 的特殊结合构象,表现出潜在的结合自由能。此外,我们还鉴定了该 BTK 和 JAK3 双重抑制剂的关键残基和指纹特征。