Development of small molecule inhibitors and stabilizers of dimerization of tRNA-guanine transglycosylase to treat Shigellosis

Applicant Professor Dr. Gerhard Klebe

Subject Area Pharmacy

Term from 2016 to 2021

Project identifier Deutsche Forschungsgemeinschaft (DFG) - Project number 324043133

Final Report Year 2020

Final Report Abstract

No abstract available

Sugar Acetonides are a Superior Motif for Addressing the Large, Solvent-Exposed Ribose-33 Pocket of tRNA- Guanine Transglycosylase, Chem. Eur. J. 24 (2018) 9957–9967
L. D. Movsisyan, E. Schäfer, A. Nguyen, F. R. Ehrmann, A. Schwab, T. Rossolini, D. Zimmerli, B. Wagner, H. Daff, A. Heine, G. Klebe, F. Diederich
(See online at https://doi.org/10.1002/chem.201801756)
Swapping Interface Contacts in the Homodimeric tRNA Guanine Transglycosylase: An Option for Functional Regulation, Angew. Chem. Int Ed. Engl., 57 (2018) 10085-10090
F. R. Ehrmann, J. Kalim, T. Pfaffeneder, B. Bernet, C. Hohn, E. Schäfer, T. Botzanowski, S. Cianférani, A. Heine, K. Reuter, F. Diederich, G. Klebe
(See online at https://doi.org/10.1002/anie.201804627)
The Importance of Charge in Perturbing the Aromatic Glue Stabilizing the Protein–Protein Interface of Homodimeric tRNA-Guanine Transglycosylase, ACS Chem. Biol. 15 (2020) 3021–3029
A. Nguyen, D. Nguyen, T. X. P. Nguyen, M. Sebastiani, S. Dörr, O. Hernandez-Alba, F. Debaene, S. Cianférani, A. Heine, G. Klebe, K. Reuter
(See online at https://doi.org/10.1021/acschembio.0c00700)