Author

David E. Heppner

2 papers indexed here

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Open access Oct 2026

Deciphering the Structure−Activity Relationships Underpinning the Linkerology of Bivalent EGFR Inhibitors

Linking small molecules that bind adjacent sites on a target is a promising strategy for developing compounds with tight binding affinities. ATP-allosteric bivalent inhibitors (AABIs) of the epidermal growth factor receptor (EGFR) have provided new insights into efficient linker design where large potency gains can b...

Kishan B. Patel, I. A. Akinwumi, Tess M. Weber et al. · Journal of Medicinal Chemist... · 0 citations

Open access Sep 2026

Thinking Outside the Binding Site: A Self-Encapsulating Kinase Inhibitor Remodels Its Pocket to Achieve Selectivity.

Rendering kinase inhibitors selective is a strict requirement in drug development and remains a persistent challenge. To identify new routes to engineer selectivity, we have discovered a first-in-class p38δ-isoform selective inhibitor reflecting 12 000-fold selectivity improvement over currently available compounds and...

Nico J. Seidler, Monica R. MacDonald, Athina A. Moschopoulou et al. · Angewandte Chemie · 0 citations