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Updated: Sep 10, 2025

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
Published on: July 25, 2020
TargetPair: A Single Cell-omics Resource of Clinical Trials-derived Therapeutical Target Combinations for Cancer
Kaicheng Zhou1, Xingxiu Li1, Yuan Yang1
1School of Pharmaceutical Sciences, Shanghai Engineering Research Center of Immunotherapeutics, Fudan University, Shanghai 201203, China.
Abstract:
The complexity of the tumor microenvironment (TME) makes cancer therapy challenging. Multi-targeting strategies often exhibit superior clinical benefits and dominate ongoing cancer clinical trials. However, existing multi-targeting strategies largely rely on empirical approaches. The rational design of target pairs (TPs) for multi-target cancer therapy development is a high priority but remains a significant challenge, which may benefit from single-cell omics technologies to decode the TME. However, there has been no thorough survey of clinically relevant cancer TPs and their characterization at the single-cell level. Here, we established the TargetPair database to address this gap by manually annotating TPs from drug combinations and multi-targeting drugs whose anti-tumor efficacy has been evaluated, and calculating their omics features at the single-cell level. The TargetPair database provides (1) 60 approved, 1,580 clinical-stage, and 7,424 experimental-stage TPs manually annotated from 3,470 clinical trials and 1,396 publications, and (2) the omics features of TPs (co-expression, distribution, expressed cell fractions, pathways, and single-cell gene networks) from manually curated scRNA-seq datasets derived from 55 pieces of literature (including 3,022,556 single cells, 13 cell types, 16 cancer types, and 588 patients). It can be freely accessed at https://www.targetpair.aiddlab.com via several search and browsing modes.
Insights
Developing rational multi-target cancer therapies is crucial. The new TargetPair database systematically catalogs clinically relevant target pairs and their single-cell omics features, aiding in rational drug design for improved cancer treatment.
Area of Science:
- Oncology
- Bioinformatics
- Computational Biology
Background:
- The tumor microenvironment (TME) presents significant challenges for cancer therapy.
- Multi-targeting strategies show clinical promise but often rely on empirical methods.
- Rational design of target pairs (TPs) for multi-target therapy is a priority.
Purpose of the Study:
- To address the lack of comprehensive data on clinically relevant cancer TPs and their single-cell characterization.
- To establish a manually annotated database of TPs with associated omics features.
- To facilitate the rational design of multi-target cancer therapies.
Main Methods:
- Manual annotation of TPs from drug combinations and multi-targeting drugs with evaluated anti-tumor efficacy.
- Calculation of single-cell omics features for TPs, including co-expression, distribution, and cell fractions.
- Curating single-cell RNA sequencing (scRNA-seq) datasets from 55 publications.
Main Results:
- The TargetPair database contains 60 approved, 1,580 clinical-stage, and 7,424 experimental-stage TPs.
- TPs were annotated from 3,470 clinical trials and 1,396 publications.
- Omics features were derived from 3,022,556 single cells across 13 cell types, 16 cancer types, and 588 patients.
Conclusions:
- The TargetPair database provides a valuable resource for understanding TPs at the single-cell level.
- This resource can aid in the rational design of novel multi-target cancer therapies.
- The database is freely accessible online for research purposes.
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