ArticleACS medicinal chemistry letters2026
Design of PKC-Targeting Benzolactams as Gli Inhibitors.
Article in ACS medicinal chemistry letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Dysregulated Hedgehog signaling, driven by oncogenic Gli transcription factors, plays a central role in many cancers and other Gli-dependent diseases. Inhibition of Gli through Smoothened-independent mechanisms represents a promising strategy to overcome resistance to clinical Hedgehog pathway inhibitors. Herein we report the synthesis and structure-activity relationship analysis of benzolactam analogues derived from TPPB, a potent inhibitor of Gli signaling that suppresses Gli activity via a protein kinase C (PKC)-mediated mechanism. Strategic chemical modifications were introduced across positions of the benzolactam core to assess their effects on biological activity using Gli-reporter cell-based assays. Our findings identified key structural features required for PKC-mediated Gli inhibition, and computational modeling revealed novel interactions between the PKC C1 domain and benzolactam analogues with nanomolar potency. Together, these studies provide a framework for designing therapeutics targeting Gli-driven diseases resistant to current treatments.
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