PROTAC-DB 3.0: an updated database of PROTACs with extended pharmacokinetic parameters
Proteolysis-targeting chimera (PROTAC) is an emerging therapeutic technology that leverages the ubiquitin-proteasome system to target protein degradation. Due to its event-driven mechanistic characteristics, PROTAC has the potential to regulate traditionally non-druggable targets. Recently, AI-aided drug design has accelerated the development of PROTAC drugs. However, the rational design of PROTACs remains a considerable challenge. Here, we present an updated online database, PROTAC-DB 3.0. In this third version, we have expanded the database to include 6111 PROTACs (87% increase compared to the 2.0 version). Additionally, the database now contains 569 warheads (small molecules targeting the protein), 2753 linkers, and 107 E3 ligands (small molecules recruiting E3 ligases). The number of target-PROTAC-E3 ternary complex structures has also increased to 959. Recognizing the importance of druggability in PROTAC design, we have incorporated pharmacokinetic data to PROTAC-DB 3.0. To enhance user experience, we have added features for sorting based on molecular similarity and literature publication date. PROTAC-DB 3.0 is accessible at http://cadd.zju.edu.cn/protacdb/.
Authors
- Huiyong Sun (ORCID: https://orcid.org/0000-0002-7107-7481)
- Gaoqi Weng (ORCID: https://orcid.org/0000-0001-8476-7548)
- Tingjun Hou (ORCID: https://orcid.org/0000-0001-7227-2580)
- Yafeng Deng (ORCID: https://orcid.org/0000-0003-2416-6913)
- Huating Wang (ORCID: https://orcid.org/0000-0001-5474-2905)
- Shimeng Li (ORCID: https://orcid.org/0000-0003-4004-1707)
- Meijing Fang (ORCID: https://orcid.org/0009-0009-4509-9212)
- Jingxuan Ge (ORCID: https://orcid.org/0009-0006-9835-5660)
- Chang- Yu Hsieh
- Dan Li
Institutions
- China Pharmaceutical University (CN)
- Zhejiang University (CN)
Publication Details
- Journal
- Nucleic Acids Research
- Published
- 2024-09-03
- DOI
- https://doi.org/10.1093/nar/gkae768
- Citations
- 79
- Primary Topic
- Protein Degradation and Inhibitors
- Type
- article
- Field-Weighted Citation Impact
- 18.47
Funders
- National Natural Science Foundation of China
- National Key Research and Development Program of China
- Natural Science Foundation of Zhejiang Province