Linker Modification Enables Control of Key Functional Group Orientation in Macrocycles

Macrocycles are promising drug modalities that can enable unique ways of conformational preorganization, but how even minor modifications to a macrocyclic scaffold influence the conformational preorganization remains poorly understood. Here, we show how macrocyclization and further derivatization of...

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Autor principal:	Christian Brudy (19468152) (author)
Altres autors:	Enrico Ruijsenaars (13889916) (author), Christian Meyners (7354283) (author), Wisely O. Sugiarto (22669618) (author), Hanaa Achaq (22669621) (author), Moritz Spiske (19468155) (author), Vanessa Buffa (14614045) (author), Margherita Springer (14614048) (author), Maximilian Repity (22669624) (author), Arjen Weller (13763995) (author), Undine Haferkamp (10266529) (author), Ole Pless (4864297) (author), Patricia Muschong (22669627) (author), Dominik Miltner (22669630) (author), Mario Mezler (5523578) (author), Mathias V. Schmidt (14614051) (author), Sereina Riniker (1450804) (author), Felix Hausch (383326) (author)
Publicat:	2025
Matèries:	Biophysics Biochemistry Medicine Molecular Biology Neuroscience Pharmacology Biotechnology Space Science Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified resolution cocrystal structures molecular dynamics simulations macrocyclic scaffold influence human stress response good brain permeability exposed methyl group even minor modifications enable unique ways enable desired properties binding protein 51 small linker variations key carbonyl group promising drug modalities improve binding affinity improve affinity linker region key regulator vivo profile using high plasma stability nonmethylated analog improved solubility highly ligand highly atom fkbp51 ), efficient manner conformational preorganization advantageous position 10 ×
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Linker Modification Enables Control of Key Functional Group Orientation in Macrocycles

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