Tailored SirReal-type inhibitors enhance SIRT2 inhibition through ligand stabilization and disruption of NAD+ co-factor binding

Ricky Wirawan, Matthias Frei, Anna Heider, Niklas Papenkordt, Florian Friedrich, Thomas Wein, Manfred Jung, Michael Groll, Eva M. Huber and Franz Bracher

RSC Med. Chem., 2025
DOI: 10.1039/D5MD00144G

In silico approach reveals N -(5-phenoxythiophen-2-yl)-2-(arylthio)acetamides as promising selective SIRT2 inhibitors: the case of structural optimization of virtual screening-derived hits

Mahmut Gozelle, Filiz Bakar-Ates, Alberto Massarotti, Erva Ozkan, Habibe Beyza Gunindi, Yesim Ozkan and Gokcen Eren

Journal of Biomolecular Structure and Dynamics, 2025, 43, 1756
DOI: 10.1080/07391102.2023.2293252

Structure–Activity Studies of 1,2,4-Oxadiazoles for the Inhibition of the NAD+-Dependent Lysine Deacylase Sirtuin 2

Arianna Colcerasa, Florian Friedrich, Jelena Melesina, Patrick Moser, Anja Vogelmann, Pavlos Tzortzoglou, Emilia Neuwirt, Manuela Sum, Dina Robaa, Lin Zhang, Elizabeth Ramos-Morales, Christophe Romier, Oliver Einsle, Eric Metzger, Roland Schüle, Olaf Groß, Wolfgang Sippl and Manfred Jung

J. Med. Chem., 2024, 67, 10076
DOI: 10.1021/acs.jmedchem.4c00229

Symmetrical 2,7‐disubstituted 9H‐fluoren‐9‐one as a novel and promising scaffold for selective targeting of SIRT2

Selen Gozde Kaya, Gokcen Eren, Alberto Massarotti, Habibe Beyza Gunindi, Filiz Bakar‐Ates and Erva Ozkan

Archiv der Pharmazie, 2024, 357
DOI: 10.1002/ardp.202400661

2‐(Methyl(phenyl)amino)‐N‐(phenyloxyphenyl)acetamide structural motif representing a framework for selective SIRT2 inhibition

Selen Gozde Kaya, Gokcen Eren, Alberto Massarotti, Filiz Bakar‐Ates, Erva Ozkan, Mahmut Gozelle and Yesim Ozkan

Drug Development Research, 2024, 85
DOI: 10.1002/ddr.22224

Structure, functions, and recent advances in the development of SIRT2 inhibitors

Junxin Xue, Xuben Hou and Hao Fang

Pharmaceutical Science Advances, 2023, 1, 100010
DOI: 10.1016/j.pscia.2023.100010

Efficient Crystallization of Apo Sirt2 for Small-Molecule Soaking and Structural Analysis of Ligand Interactions

Florian Friedrich, Matthias Schiedel, Sören Swyter, Lin Zhang, Wolfgang Sippl, Mike Schutkowski, Oliver Einsle and Manfred Jung

J. Med. Chem., 2025, 68, 10771
DOI: 10.1021/acs.jmedchem.4c02896

Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation

Laura Sinatra, Anja Vogelmann, Florian Friedrich, Margarita A. Tararina, Emilia Neuwirt, Arianna Colcerasa, Philipp König, Lara Toy, Talha Z. Yesiloglu, Sebastian Hilscher, Lena Gaitzsch, Niklas Papenkordt, Shiyang Zhai, Lin Zhang, Christophe Romier, Oliver Einsle, Wolfgang Sippl, Mike Schutkowski, Olaf Gross, Gerd Bendas, David W. Christianson, Finn K. Hansen, Manfred Jung and Matthias Schiedel

J. Med. Chem., 2023, 66, 14787
DOI: 10.1021/acs.jmedchem.3c01385

Molecular Sentinels: Unveiling the Role of Sirtuins in Prostate Cancer Progression

Surbhi Chouhan, Naoshad Muhammad, Darksha Usmani, Tabish H. Khan and Anil Kumar

IJMS, 2024, 26, 183
DOI: 10.3390/ijms26010183

Continuous Fluorescent Sirtuin Activity Assay Based on Fatty Acylated Lysines

Matthes Zessin, Marat Meleshin, Sebastian Hilscher, Cordelia Schiene-Fischer, Cyril Barinka, Manfred Jung and Mike Schutkowski

IJMS, 2023, 24, 7416
DOI: 10.3390/ijms24087416

Target Engagement Studies and Kinetic Live-Cell Degradation Assays Enable the Systematic Characterization of Histone Deacetylase 6 Degraders

Maria Hanl, Felix Feller, Irina Honin, Kathrin Tan, Martina Miranda, Linda Schäker-Hübner, Nico Bückreiß, Matthias Schiedel, Michael Gütschow, Gerd Bendas and Finn K. Hansen

ACS Pharmacol. Transl. Sci., 2025, 8, 3074
DOI: 10.1021/acsptsci.5c00247

The (patho)physiological roles of the individual deacylase activities of a sirtuin

Weiping Zheng

Chem Biol Drug Des, 2024, 103
DOI: 10.1111/cbdd.14460

Selective inhibition of SIRT2: A disputable therapeutic approach in cancer therapy

Selen Gozde Kaya and Gokcen Eren

Bioorganic Chemistry, 2024, 143, 107038
DOI: 10.1016/j.bioorg.2023.107038

A homogeneous time-resolved fluorescence screen to identify SIRT2 deacetylase and defatty-acylase inhibitors

Jie Yang, Joel Cassel, Brian C. Boyle, Daniel Oppong, Young-Hoon Ahn, Brian P. Weiser and Michael Massiah

PLoS ONE, 2024, 19, e0305000
DOI: 10.1371/journal.pone.0305000