Macrocyclic FKBP51 Ligands Define a Transient Binding Mode with Enhanced Selectivity

Subtype selectivity represents a challenge in many drug discovery campaigns. A typical example is the FK506 binding protein 51 (FKBP51), which has emerged as an attractive drug target. The most advanced FKBP51 ligands of the SAFit class are highly selective vs. FKBP52 but poorly discriminate against...

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Detalhes bibliográficos
Publicado no:Angew Chem Int Ed Engl
Main Authors: Voll, Andreas M., Meyners, Christian, Taubert, Martha C., Bajaj, Thomas, Heymann, Tim, Merz, Stephanie, Charalampidou, Anna, Kolos, Jürgen, Purder, Patrick L., Geiger, Thomas M., Wessig, Pablo, Gassen, Nils C., Bracher, Andreas, Hausch, Felix
Formato: Artigo
Idioma:Inglês
Publicado em: John Wiley and Sons Inc. 2021
Assuntos:
Research Articles
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8252719/
https://ncbi.nlm.nih.gov/pubmed/33843131
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/anie.202017352
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