ET-PROTACs: modeling ternary complex interactions using cross-modal learning and ternary attention for accurate PROTAC-induced degradation prediction.

Journal: Briefings in bioinformatics
PMID:

Abstract

MOTIVATION: Accurately predicting the degradation capabilities of proteolysis-targeting chimeras (PROTACs) for given target proteins and E3 ligases is important for PROTAC design. The distinctive ternary structure of PROTACs presents a challenge to traditional drug-target interaction prediction methods, necessitating more innovative approaches. While current state-of-the-art (SOTA) methods using graph neural networks (GNNs) can discern the molecular structure of PROTACs and proteins, thus enabling the efficient prediction of PROTACs' degradation capabilities, they rely heavily on limited crystal structure data of the POI-PROTAC-E3 ternary complex. This reliance underutilizes rich PROTAC experimental data and neglects intricate interaction relationships within ternary complexes.

Authors

  • Lijun Cai
    College of Information Science and Engineering, Hunan University, Changsha, Hunan, 410082, China.
  • Guanyu Yue
    College of Computer Science and Electronic Engineering, Hunan University, Changsha, Hunan 410082, China.
  • Yifan Chen
    Adam Smith Business School, University of Glasgow, Scotland, United Kingdom.
  • Li Wang
    College of Marine Electrical Engineering, Dalian Maritime University, Dalian, China.
  • Xiaojun Yao
    Centre for Artificial Intelligence Driven Drug Discovery, Faculty of Applied Sciences, Macao Polytechnic University, Macao, 999078, PR China.
  • Quan Zou
  • Xiangzheng Fu
  • Dongsheng Cao
    School of Pharmaceutical Sciences, Central South University, Changsha, China. oriental-cds@163.com.