Publikationen 2022
P. Sun, J. Wang, K. S. Khan, W. Yang, W.-L. Ng, N. Ilmenov, M. Zessin, E. F. Bülbül, D. Robaa, F. Erdmann, M. Schmidt, C. Romier, M. Schutkowski, A. S. L. Cheng, W. Sippl. Development of alkylated hydrazides as selective HDAC8 inhibitors with T cell modulatory properties. J Med Chem. 2022 Nov 30. doi:10.1021/acs.jmedchem.2c01132 .
M. Abdelsalam, M. Zessin, M. Schmidt, M. Schutkowski and W. Sippl. N1-(2-Amino-4-fluorophenyl)-N4-(3-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4yl)amino)propoxy)ethoxy)ethoxy)propyl)terephthalamide. Molbank 2022, 2022(4), M1501; https://doi.org/10.3390/M1501
B. Noce, E. Di Bello, C. Zwergel, R. Fioravanti, S. Valente, D. Rotili, A. Masotti, G. Fianco, D. Trisciuoglio, A. Chakrabarti, C. Romier, D. Robaa, W. Sippl, M. Jung, C. Häberli, J. Keiser, and A. Mai. Chemically Different S. mansoni HDAC8 Inhibitors Reduced Viability in Worm Juvenile and Adult Forms. ChemMedChem. 2022 Oct 17. doi:10.1002/cmdc.202200510
B. Turgutalp, P. Bhattarai , T. Ercetin, C. Luise, R. Reis, E. Gurdal, A. Isaak, E. Dinter, H. Sipahi, A. Junker, D. Schepmann, B. Wünsch, W. Sippl, H. O. Gulcan, C. Kizil, M. Yarim. Discovery of Potent Cholinesterase Inhibition-Based Multi-Target Directed Lead Compounds for Synaptoprotection in Alzheimer’s Disease. J Med Chem. 2022 Sep 9. doi:10.1021/acs.jmedchem.2c0100 3
D. Kalbas, M. Meleshin, S. Liebscher, M. Zessin, E.F. Bulbul, J. Melesina, C. Schiene-Fischer, F. Bordusa, W. Sippl, M. Schutkowski. Small changes make the difference for SIRT2: Two different binding modes for 3-arylmercapto-acylated lysine derivatives. Biochemistry, 2022 Aug 16. doi:10.1021/acs.biochem.2c00211
H Ahmed, L Gisler, NH Elghazawy, C Keller, W Sippl, SH Liang, A Haider, S M Ametamey. Development and Validation of [3H] OF-NB1 for Preclinical Assessment of GluN1/2B Candidate Drugs. Pharmaceuticals 15 (8), 960, 2022 https://doi.org/10.3390/ph15080960
A Opitz, LM Seitz, V Krystof, F Baselious, M Holzer, W Sippl, A Hilgeroth. Novel effective small-molecule inhibitors of protein kinases related to tau pathology in Alzheimer's disease. Future Med Chem. 2022 Aug;14(16):1175-1186. doi:10.4155/fmc-2022-0061
S. Darwish, E. Ghazy, T. Heimburg, D. Herp, P. Zeyen, R. Salem-Alintas, J. Ridinger, D. Robaa, K. Schmidtkunz, F. Erdmann, M. Schmidt, C. Romier, M. Jung, I. Oehme, W. Sippl. Design, Synthesis and Biological Characterization of Histone Deacetylase 8 (HDAC8) Proteolysis Targeting Chimera (PROTAC) with Anti-Neuroblastoma Activity. Int. J. Mol. Sci. 2022, 23(14), 7535; https://doi.org/10.3390/ijms23147535
S. Lechner, M. I. P. Malgapo, C. Grätz, R.R. Steinbach, A. Baron, P. Rüther, S. Nadal, C. Stumpf, C. Loos, X. Ku, P. Prokofeva, L. Lautenbacher, T. Heimburg, V. Würf, C. Meng, M. Wilhelm, W. Sippl, K. Kleigrewe, J. K. Pauling, K. Kramer, A.K. Miller, M. W. Pfaffl, M. E. Linder, B. Kuster, G. Médard.
Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target.
NatChemBiol 28th April 2022. https://doi.org/10.1038/s41589-022-01015-5
M. Zessin, M. Meleshin, L. Praetorius, W. Sippl, C. Bařinka, M. Schutkowski
Uncovering robust delactoylase and depyruvoylase activities of HDAC isoforms
ACS Chem Biol. 2022 May 31. doi:10.1021/acschembio.1c00863
D. Herp, J. Ridinger, D. Robaa, S. A. Shinsky, K. Schmidtkunz, T. Z. Yesiloglu, T. Bayer, R. Steimbach, C.J. Herbst-Gervasoni , A. Merz, C.Romier, P. Seher, N. Gunkel, A. Miller, D.W. Christianson, I. Oehme, W. Sippl, M. Jung.
First fluorescent acetylspermidine deacetylation assay for HDAC10 identifies selective inhibitors with cellular target engagement.
ChemBioChem, 2022 May 24. doi:10.1002/cbic.202200180
S. Zähringer, T. Rumpf, J. Melesina, A.E. Lang, K. Aktories, W. Sippl, M. Jung, G.K. Wagner
Defined stereoisomers of 2′′-amino NAD+ and their activity against human sirtuins and a bacterial (ADP-ribosyl) transferase
Bioorg Med Chem, 3 June 2022, 116875. https://doi.org/10.1016/j.bmc.2022.116875
H. Ahmed, A. Haider, N. Elghazawy, L. Gisler C. Keller, W. Sippl, S. Liang, A., S. Ametamey.
[3H]OF-NB1 and [18F]OF-NB1: novel radioligands for the preclinical assessment of GluN1/2B targeting ligands. Nuclear Medicine and Biology 108-109:S95-S96, 2022.
E. F. Bülbül, J. Melesina, H. S. Ibrahim, M. Abdelsalam, A. Vecchio, D. Robaa, M. Zessin, M. Schutkowski, and W. Sippl.
Docking, Binding Free Energy Calculations and in vitro Characterization of Pyrazine Linked 2-Aminobenzamides as new Class I Histone Deacetylase (HDAC) Inhibitors.
Molecules. 2022 Apr 14;27(8):2526. doi:10.3390/molecules27082526 .
N. Cheshmazar, S.Hemmati, M. Hamzeh-Mivehroud, B. Sokouti, M. Zessin, M. Schutkowski, W. Sippl, H. Nozad Charoudeh, S. Dastmalchi.
Development of new inhibitors of HDAC 1-3 enzymes aided by in silico design strategies.
J Chem Inf Model. 2022 Apr 25. doi:10.1021/acs.jcim.1c01557
E. Ghazy, M. Abdelsalam, D. Robaa, R.J. Pierce, W. Sippl.
Histone deacetylase (HDAC) inhibitors for the treatment of Schistosomiasis.
Pharmaceuticals 15(1), 80, 2022. https://doi.org/10.3390/ph15010080
H. Ibrahim, M. Abdelsalam, Y. Zeyn, M. Zessin, E F. Bülbül, A. M. Mustafa, M. A. Fischer, P. Zeyen, A. Vecchio, P. Sun, F. Erdmann, M. Schmidt, D. Robaa, C. Romier, M. Schutkowski, O. H. Krämer, and W. Sippl.
Synthesis and structure-activity relationship studies of pyrazine linked 2-aminobenzamides as new class I selective histone deacetylase (HDAC) inhibitors and their biological characterization in leukemic cellsInt.
J. Mol. Sci. 23(1), 369, 2022. https://doi.org/10.3390/ijms23010369
A. Vogelmann, M. Schiedel, N. Wössner, A. Merz, D. Herp, S. Hammelmann, A. Colcerasa, J. Y. Hong, G. Komaniecki, M. Sum, E. Metzger, E. Neuwirt, L. Zhang, O. Einsle, O. Groß, R. Schüle, H. Lin, W. Sippl and M. Jung.
Development of a NanoBRET assay to validate inhibitors of Sirt2-mediated lysine deacetylation and defatty-acylation that block prostate cancer cell migration. RSC Chem Biol. 2022 Mar 1;3(4):468-485. doi:10.1039/d1cb00244a.
H. R. Vaca, A. Toscaninni, A. M. Celentano, M. Cuesta, A. Nusblat, N. Macchiaroli, G. Oliverira, M. C. Elissondo, A.T. Hauser, W. Sippl, M. Jung, F. Camicia and M. C. Rosenzvit.
Identification and characterization of sirtuin enzymes in cestodes and evaluation of sirtuin inhibitors as new cestocidal molecules
Int J Parasitol. 2022 Feb 9:S0020-7519(22)00015-7. doi:10.1016/j.ijpara.2021.12.002.