Design and synthesis of a clickable cell-permeable pseudopeptide Pin1 inhibitor with antiproliferative effects on human multiple myeloma cell line
The synthesis of a library of minimal-backbone, cell-permeable, clickable pseudopeptide Pin1 ligands with potential applications in drug development and biochemical studies is reported. The ligands' affinity constants were evaluated using NMR. The lead compound 4b, demonstrated effective cell permeability, inhibitory activity, and an antiproliferative effect on a multiple myeloma cell line.
Authors
- Sabrina Kellouche-Gaillard
- Ludovic Carlier (ORCID: https://orcid.org/0000-0002-9036-6561)
- Franck Carreiras (ORCID: https://orcid.org/0000-0001-8765-7280)
- Chiara Zanato (ORCID: https://orcid.org/0000-0002-9132-5120)
- Maud Larregola (ORCID: https://orcid.org/0000-0002-9196-3552)
- Julien Pytkowicz (ORCID: https://orcid.org/0000-0002-8545-3046)
- Lorenzo Meneghelli
- Simon Nadal (ORCID: https://orcid.org/0000-0002-0748-0284)
- Stephanie Davidson (ORCID: https://orcid.org/0000-0003-1177-1559)
- Anthony Gineste
- Lamia El Guermah
Institutions
- Centre National de la Recherche Scientifique (FR)
- Université Paris-Saclay (FR)
- École Normale Supérieure - PSL (FR)
- Sorbonne Université (FR)
- CY Cergy Paris Université (FR)
- Chimie Physique et Chimie du Vivant (FR)
Publication Details
- Journal
- Chemical Communications
- Published
- 2025-01-01
- DOI
- https://doi.org/10.1039/d4cc05968a
- Primary Topic
- Peptidase Inhibition and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Agence Nationale de la Recherche