Conformational Plasticity and Binding Affinity Enhancement Controlled by Linker Derivatization in Macrocycles

V Buffa, C Walz, C Meyners, M Zheng… - Angewandte Chemie …, 2025 - Wiley Online Library
Macrocycles are abundantly used by nature to enable cell‐permeable bioactive molecules.
Synthetic non‐peptidic macrocycles are also increasingly considered as modalities for …

Conformationally Restricted Macrocycles as Improved FKBP51 Inhibitors Enabled by Systematic Linker Derivatization

M Spiske, C Meyners, M Bauder, M Repity… - Angewandte …, 2025 - Wiley Online Library
Macrocycles are increasingly considered as promising modalities to target challenging
intracellular proteins. However, strategies for transitioning from active linear starting points to …

A protein engineering approach toward understanding FKBP51 conformational dynamics and mechanisms of ligand binding

JA Lerma Romero, C Meyners, N Rupp… - Protein Engineering …, 2023 - academic.oup.com
Most proteins are flexible molecules that coexist in an ensemble of several conformations.
Point mutations in the amino acid sequence of a protein can trigger structural changes that …