Ligandomics: a paradigm shift in biological drug discovery

Wei Li, Iok Hou Pang, Mario Thiego F. Pacheco, Hong Tian

Research output: Contribution to journalReview articlepeer-review

13 Scopus citations


As productivity of pharmaceutical research and development (R&D) for small-molecule drugs declines, the trend in drug discovery strategies is shifting towards biologics, which predominantly target secreted or cell surface proteins. Receptors and ligands are the most-valuable drug targets. In contrast to conventional approaches of discovering one ligand at a time, the emerging technology of ligandomics can systematically map disease-selective cellular ligands in the absence of molecular probes. Biologics targeting these ligands with disease selectivity have the advantages of high efficacy, minimal adverse effects, wide therapeutic indices, and low safety-related attrition rates. Therefore, ligandomics represents a paradigm shift to address the bottleneck of target discovery for biologics development.

Original languageEnglish
Pages (from-to)636-643
Number of pages8
JournalDrug Discovery Today
Issue number3
StatePublished - Mar 2018


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