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

Institutions

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

Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

PROTAC-DB 3.0: an updated database of PROTACs with extended pharmacokinetic parameters

Huiyong Sun, Gaoqi Weng, Tingjun Hou, Yafeng Deng et al.
79 citations
Nucleic Acids Research
Protein Degradation and Inhibitors
18.47
article

PROTAC-DB 3.0: an updated database of PROTACs with extended pharmacokinetic parameters

Huiyong Sun, Gaoqi Weng, Tingjun Hou, Yafeng Deng, Huating Wang, Shimeng Li, Meijing Fang, Jingxuan Ge, Chang- Yu Hsieh, Dan Li
article en
79 citations

Abstract

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/.

Nucleic Acids ResearchVol. 53(D1)
China Pharmaceutical University (CN), Zhejiang University (CN)
National Natural Science Foundation of China, National Key Research and Development Program of China, Natural Science Foundation of Zhejiang Province
Openalex Percentile: Top 0%
Protein Degradation and Inhibitors
18.47
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.