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Updated: Mar 6, 2026

Probing High-density Functional Protein Microarrays to Detect Protein-protein Interactions
Published on: August 2, 2015
Discovery of Clinical Candidate IAG933, a Potent YAP-TEAD PPI Disrupter
Markus Vögtle1, Holger Sellner1, Emilie Chapeau1
1Novartis BioMedical Research, 4002 Basel, Switzerland.
Abstract:
The interaction of transcriptional enhanced associate domain (TEAD) and transcriptional coactivator yes-associated protein (YAP) mediates oncogenic functions downstream of the Hippo pathway. In this report, we outline our efforts to find a potent inhibitor of this protein-protein interaction with suitable properties for clinical evaluation. We detail the medicinal chemistry program that led to the discovery of IAG933, an inhibitor with a balanced ADME profile, enabling its evaluation as a potential treatment option in clinical settings.
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