Lorenzo Meneghelli , Stephanie Davidson , Anthony Gineste , Lamia El Guermah , Sabrina Kellouche-Gaillard , Franck Carreiras , Ludovic Carlier , Simon Nadal , Maud Larregola , Julien Pytkowicz , Chiara Zanato
{"title":"Design and synthesis of a clickable cell-permeable pseudopeptide Pin1 inhibitor with antiproliferative effects on human multiple myeloma cell line†","authors":"Lorenzo Meneghelli , Stephanie Davidson , Anthony Gineste , Lamia El Guermah , Sabrina Kellouche-Gaillard , Franck Carreiras , Ludovic Carlier , Simon Nadal , Maud Larregola , Julien Pytkowicz , Chiara Zanato","doi":"10.1039/d4cc05968a","DOIUrl":null,"url":null,"abstract":"<div><div>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 , demonstrated effective cell permeability, inhibitory activity, and an antiproliferative effect on a multiple myeloma cell line.</div></div>","PeriodicalId":67,"journal":{"name":"Chemical Communications","volume":"61 31","pages":"Pages 5774-5777"},"PeriodicalIF":4.2000,"publicationDate":"2025-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemical Communications","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/org/science/article/pii/S1359734525005580","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
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 , demonstrated effective cell permeability, inhibitory activity, and an antiproliferative effect on a multiple myeloma cell line.
期刊介绍:
ChemComm (Chemical Communications) is renowned as the fastest publisher of articles providing information on new avenues of research, drawn from all the world''s major areas of chemical research.