Discovery, X-ray structure and CPP-conjugation enabled uptake of p53/MDM2 macrocyclic peptide inhibitors

• DOI: 10.1039/d1cb00056j
• Publication Date: 2021-08-26T15:41:09Z
• Authors: Anselm F. L. Schn...; Joerg Kallen; Johannes Ottl; Patrick C. Reid; Sebastien Ripoche; Stephan Ruetz; Therese-Marie Sta...; Samuel Hintermann; Christoph E. Dumelin; Christian P. R. H...; Andreas L. Marzinzik
• Keywords: Chemistry; 0303 health sciences; 03 medical and health sciences

mRNA display leads to the identification of a macrocyclic peptide inhibitor with a unique binding mode to MDM2, a negative regulator of the tumor suppressor p53. Conjugation to a cell-penetrating peptide allows in cellulo evaluation of inhibition.