From Serendipity to Rationality: Expanding Druggability by Molecular Glue Discovery

From Serendipity to Rationality: Expanding Druggability by Molecular Glue Discovery

Journal of Medicinal Chemistry

doi:10.1021/acs.jmedchem.6c01252

https://doi.org/10.1021/acs.jmedchem.6c01252

David E. Heppner, CongBao Kang, Weijun Xu

14 May 2026

Heppner, D. E., Kang, C., & Xu, W. (2026). From Serendipity to Rationality: Expanding Druggability by Molecular Glue Discovery. Journal of Medicinal Chemistry, 69(9), 9776–9779. https://doi.org/10.1021/acs.jmedchem.6c01252

Molecular glues represent an emerging class of small molecules that modulate protein function by stabilizing or inducing protein-protein interactions. Unlike conventional small molecules, molecular glues are applicable to diverse targets including those previously considered undruggable due to the formation of unique protein complexes, most commonly ternary complexes formed by the target of interest, the designed molecular glue, and an effective protein linked with an important pathway. Recent advances in molecular glue development have greatly expanded our understanding of the mechanism of action and provide insights into rational development of this emerging class of promising agents.

Publisher Copyright

This research is supported by core funding from: Experimental Drug Development Centre (EDDC)
Grant Reference no. : Core

This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/doi:10.1021/acs.jmedchem.6c01252.

https://oar.a-star.edu.sg/communities-collections/articles/23424

0022-2623
1520-4804

Experimental Drug Development Centre