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Targeted protein degradation reveals BET bromodomains as the cellular target of Hedgehog pathway inhibitor-1

Publié dansNature communications, vol. 14, no. 1, 3893
Date de publication2023-07-01
Date de mise en ligne2023-07-01
Résumé

Target deconvolution of small molecule hits from phenotypic screens presents a major challenge. Many screens have been conducted to find inhibitors for the Hedgehog signaling pathway – a developmental pathway with many implications in health and disease – yielding many hits but only few identified cellular targets. We here present a strategy for target identification based on Proteolysis-Targeting Chimeras (PROTACs), combined with label-free quantitative proteomics. We develop a PROTAC based on Hedgehog Pathway Inhibitor-1 (HPI-1), a phenotypic screen hit with unknown cellular target. Using this Hedgehog Pathway PROTAC (HPP) we identify and validate BET bromodomains as the cellular targets of HPI-1. Furthermore, we find that HPP-9 is a long-acting Hedgehog pathway inhibitor through prolonged BET bromodomain degradation. Collectively, we provide a powerful PROTAC-based approach for target deconvolution, that answers the longstanding question of the cellular target of HPI-1 and yields a PROTAC that acts on the Hedgehog pathway.

eng
Mots-clés
  • Protein Domains
  • Proteolysis
  • Antineoplastic Agents
  • Hedhegog Proteins
  • Proteolysis Targeting Chimera
Citation (format ISO)
BAGKA, Meropi et al. Targeted protein degradation reveals BET bromodomains as the cellular target of Hedgehog pathway inhibitor-1. In: Nature communications, 2023, vol. 14, n° 1, p. 3893. doi: 10.1038/s41467-023-39657-1
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Identifiants
ISSN du journal2041-1723
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Informations techniques

Création24/01/2024 14:00:49
Première validation03/05/2024 08:53:32
Heure de mise à jour03/05/2024 08:53:32
Changement de statut03/05/2024 08:53:32
Dernière indexation03/05/2024 08:53:52
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