Michael Salcius, Antonin Tutter, Marianne Fouché, Halil Koc, Dan King, Anxhela Dhembi, Andrei Golosov, Wolfgang Jahnke, Chrystèle Henry, Dayana Argoti, Weiping Jia, Liliana Pedro, Lauren Connor, Philippe Piechon, Francesca Fabbiani, Regis Denay, Emine Sager, Juergen Kuehnoel, Marie-Anne Lozach, Fabio Lima, Angela Vitrey, Shu-Yu Chen, Gregory Michaud and Hans-Joerg Roth
RSC Chem. Biol., 2025,6, 788-799
Abstract
Protein array screening revealed a macrocyclic glue that recruits MAPRE1 to FKBP12. The corresponding ternary complex was characterized and the compound-dependent inhibition of a native MAPRE1 interaction was demonstrated in a cellular assay.
Robin C. E. Deutscher, Christian Meyners, Maximilian L. Repity, Wisely Oki Sugiarto, Jürgen M. Kolos, Edvaldo V. S. Maciel, Tim Heymann, Thomas M. Geiger, Stefan Knapp, Frederik Lermyte and Felix Hausch
Chem. Sci., 2025,16, 4256-4263
From themed collection:
2025 Chemical Science HOT Article Collection
Abstract
We discovered a fully synthetic non-degradative molecular glue for the ternary complex between FKBP12 and the FRB domain of mTOR by screening a library of FKBP12 ligands. Solving the ternary complex structure allowed significant potency enhancement.
Wei Zhang, Xinwei Lu and Jicun Ren
Analyst, 2025,150, 2029-2038
Abstract
Drug-mediated protein–protein interaction and drug–protein interaction form the basis of drug development and pharmacological research.
Jason Yun, Yimeng Huang, Austin D. C. Miller, Brandon L. Chang, Logan Baldini, Kaamini M. Dhanabalan, Eugene Li, Honghao Li and Arnab Mukherjee
Chem. Sci., 2024,15, 11108-11121
Abstract
Biochemically destabilized aquaporin allows for small-molecule modulation of genetically encoded MRI signals, enabling the detection of transcriptional activity in deep tissues in a background-free, drug-gated, and chemically multiplexed manner.
Isabella A. Riha, Miguel A. Campos, Xiaokang Jin, Fiona Y. Wang, Chenlu Zhang, Sara F. Dunne, Benjamin F. Cravatt and Xiaoyu Zhang
RSC Med. Chem., 2025,16, 892-906
From themed collection:
Induced-Proximity Pharmacology
Abstract
An HTRF assay was developed to measure the DCAF16–SPIN4 interaction and was subsequently employed to screen for DCAF16 recruiters. A hit compound, 2G07, was identified and further optimized into a PROTAC for the targeted degradation of FKBP12.