{"title":"DrugProtAI:一种机器学习驱动的方法,通过特征工程和基于鲁棒分割的集成方法来预测蛋白质的可药物性。","authors":"Ankit Halder, Sabyasachi Samantaray, Sahil Barbade, Aditya Gupta, Sanjeeva Srivastava","doi":"10.1093/bib/bbaf330","DOIUrl":null,"url":null,"abstract":"<p><p>Drug design and development are central to clinical research, yet 90% of drugs fail to reach the clinic, often due to inappropriate selection of drug targets. Conventional methods for target identification lack precision and sensitivity. While various computational tools have been developed to predict the druggability of proteins, they often focus on limited subsets of the human proteome or rely solely on amino acid properties. Our study presents DrugProtAI, a tool developed by implementing a partitioning-based method and trained on the entire human protein set using both sequence- and non-sequence-derived properties. The partitioned method was evaluated using popular machine learning algorithms, of which Random Forest and XGBoost performed the best. A comprehensive analysis of 183 features, encompassing biophysical, sequence-, and non-sequence-derived properties, achieved a median Area Under Precision-Recall Curve (AUC) of 0.87 in target prediction. The model was further tested on a blinded validation set comprising recently approved drug targets. The key predictors were also identified, which we believe will help users in selecting appropriate drug targets. We believe that these insights are poised to significantly advance drug development. This version of the tool provides the probability of druggability for human proteins. The tool is freely accessible at https://drugprotai.pythonanywhere.com/.</p>","PeriodicalId":9209,"journal":{"name":"Briefings in bioinformatics","volume":"26 4","pages":""},"PeriodicalIF":6.8000,"publicationDate":"2025-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12236430/pdf/","citationCount":"0","resultStr":"{\"title\":\"DrugProtAI: A machine learning-driven approach for predicting protein druggability through feature engineering and robust partition-based ensemble methods.\",\"authors\":\"Ankit Halder, Sabyasachi Samantaray, Sahil Barbade, Aditya Gupta, Sanjeeva Srivastava\",\"doi\":\"10.1093/bib/bbaf330\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Drug design and development are central to clinical research, yet 90% of drugs fail to reach the clinic, often due to inappropriate selection of drug targets. Conventional methods for target identification lack precision and sensitivity. While various computational tools have been developed to predict the druggability of proteins, they often focus on limited subsets of the human proteome or rely solely on amino acid properties. Our study presents DrugProtAI, a tool developed by implementing a partitioning-based method and trained on the entire human protein set using both sequence- and non-sequence-derived properties. The partitioned method was evaluated using popular machine learning algorithms, of which Random Forest and XGBoost performed the best. A comprehensive analysis of 183 features, encompassing biophysical, sequence-, and non-sequence-derived properties, achieved a median Area Under Precision-Recall Curve (AUC) of 0.87 in target prediction. The model was further tested on a blinded validation set comprising recently approved drug targets. The key predictors were also identified, which we believe will help users in selecting appropriate drug targets. We believe that these insights are poised to significantly advance drug development. This version of the tool provides the probability of druggability for human proteins. The tool is freely accessible at https://drugprotai.pythonanywhere.com/.</p>\",\"PeriodicalId\":9209,\"journal\":{\"name\":\"Briefings in bioinformatics\",\"volume\":\"26 4\",\"pages\":\"\"},\"PeriodicalIF\":6.8000,\"publicationDate\":\"2025-07-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12236430/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Briefings in bioinformatics\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://doi.org/10.1093/bib/bbaf330\",\"RegionNum\":2,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"BIOCHEMICAL RESEARCH METHODS\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Briefings in bioinformatics","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.1093/bib/bbaf330","RegionNum":2,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"BIOCHEMICAL RESEARCH METHODS","Score":null,"Total":0}
DrugProtAI: A machine learning-driven approach for predicting protein druggability through feature engineering and robust partition-based ensemble methods.
Drug design and development are central to clinical research, yet 90% of drugs fail to reach the clinic, often due to inappropriate selection of drug targets. Conventional methods for target identification lack precision and sensitivity. While various computational tools have been developed to predict the druggability of proteins, they often focus on limited subsets of the human proteome or rely solely on amino acid properties. Our study presents DrugProtAI, a tool developed by implementing a partitioning-based method and trained on the entire human protein set using both sequence- and non-sequence-derived properties. The partitioned method was evaluated using popular machine learning algorithms, of which Random Forest and XGBoost performed the best. A comprehensive analysis of 183 features, encompassing biophysical, sequence-, and non-sequence-derived properties, achieved a median Area Under Precision-Recall Curve (AUC) of 0.87 in target prediction. The model was further tested on a blinded validation set comprising recently approved drug targets. The key predictors were also identified, which we believe will help users in selecting appropriate drug targets. We believe that these insights are poised to significantly advance drug development. This version of the tool provides the probability of druggability for human proteins. The tool is freely accessible at https://drugprotai.pythonanywhere.com/.
期刊介绍:
Briefings in Bioinformatics is an international journal serving as a platform for researchers and educators in the life sciences. It also appeals to mathematicians, statisticians, and computer scientists applying their expertise to biological challenges. The journal focuses on reviews tailored for users of databases and analytical tools in contemporary genetics, molecular and systems biology. It stands out by offering practical assistance and guidance to non-specialists in computerized methodologies. Covering a wide range from introductory concepts to specific protocols and analyses, the papers address bacterial, plant, fungal, animal, and human data.
The journal's detailed subject areas include genetic studies of phenotypes and genotypes, mapping, DNA sequencing, expression profiling, gene expression studies, microarrays, alignment methods, protein profiles and HMMs, lipids, metabolic and signaling pathways, structure determination and function prediction, phylogenetic studies, and education and training.