Synthetic modification of protein surfaces to mediate induced-proximity pharmacology.

Molecular glues and bifunctional small molecules, such as targeted protein degraders, induce protein proximity to mediate gain-of-function pharmacology. Emerging technologies that synthetically manipulate protein surfaces to create neoproteins, and the development of covalent chemical probes for intra- and inter-protein surface labeling are described. Ligand-directed protein surface modification strategies have the potential to enhance the induced-proximity pharmacology toolkit and expand the druggable proteome, and this Opinion considers the opportunities and challenges that lie ahead. This journal is © The Royal Society of Chemistry.

Citation

Lyn H Jones. Synthetic modification of protein surfaces to mediate induced-proximity pharmacology. RSC medicinal chemistry. 2024 Aug 09

PMID: 39185450

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