Zeitschrift: Journal of Medicinal Chemistry

2024

Pannek, Martin ; Alhalabi, Zayan ; Tomaselli, Daniela ; Menna, Martina ; Fiorentino, Francesco ; Robaa, Dina ; Weyand, Michael ; Puhlmann, Maximilian ; Tomassi, Stefano ; Barreca, Federica ; Tafani, Marco ; Zaganjor, Elma ; Haigis, Marcia C. ; Sippl, Wolfgang ; Rotili, Dante ; Mai, Antonello ; Steegborn, Clemens:
Specific Inhibitors of Mitochondrial Deacylase Sirtuin 4 Endowed with Cellular Activity.
In: Journal of Medicinal Chemistry. Bd. 67 (2024) Heft 3 . - S. 1843-1860.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.3c01496

2023

Zwergel, Clemens ; Aventaggiato, Michele ; Garbo, Sabrina ; Di Bello, Elisabetta ; Fassari, Bruno ; Noce, Beatrice ; Castiello, Carola ; Lambona, Chiara ; Barreca, Federica ; Rotili, Dante ; Fioravanti, Rossella ; Schmalz, Thomas ; Weyand, Michael ; Niedermeier, Amelie ; Tripodi, Marco ; Colotti, Gianni ; Steegborn, Clemens ; Battistelli, Cecilia ; Tafani, Marco ; Valente, Sergio ; Mai, Antonello:
Novel 1,4-Dihydropyridines as Specific Binders and Activators of SIRT3 Impair Cell Viability and Clonogenicity and Downregulate Hypoxia-Induced Targets in Cancer Cells.
In: Journal of Medicinal Chemistry. Bd. 66 (2023) Heft 14 . - S. 9622-9641.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.3c00337

2022

Miller, Michael ; Rossetti, Thomas ; Ferreira, Jacob ; Ghanem, Lubna ; Balbach, Melanie ; Kaur, Navpreet ; Levin, Lonny R. ; Buck, Jochen ; Kehr, Maria ; Coquille, Sandrine ; van den Heuvel, Joop ; Steegborn, Clemens ; Fushimi, Makoto ; Finkin-Groner, Efrat ; Myers, Robert W. ; Kargman, Stacia ; Liverton, Nigel J. ; Huggins, David J. ; Meinke, Peter T.:
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
In: Journal of Medicinal Chemistry. Bd. 65 (2022) Heft 22 . - S. 15208-15226.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.2c01133

Suenkel, Benjamin ; Valente, Sergio ; Zwergel, Clemens ; Weiss, Sandra ; Di Bello, Elisabetta ; Fioravanti, Rossella ; Aventaggiato, Michele ; Amorim, João A. ; Garg, Neha ; Kumar, Surinder ; Lombard, David B. ; Hu, Tuo ; Singh, Pankaj K. ; Tafani, Marco ; Palmeira, Carlos M. ; Sinclair, David ; Mai, Antonello ; Steegborn, Clemens:
Potent and Specific Activators for Mitochondrial Sirtuins Sirt3 and Sirt5.
In: Journal of Medicinal Chemistry. Bd. 65 (2022) Heft 20 . - S. 14015-14031.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.2c01215

2018

Kalbas, Diana ; Liebscher, Sandra ; Nowak, Theresa ; Meleshin, Marat ; Pannek, Martin ; Popp, Corinna ; Alhalabi, Zayan ; Bordusa, Frank ; Sippl, Wolfgang ; Steegborn, Clemens ; Schutkowski, Mike:
Potent and Selective Inhibitors of Human Sirtuin 5.
In: Journal of Medicinal Chemistry. Bd. 61 (2018) Heft 6 . - S. 2460-2471.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.7b01648

You, Weijie ; Steegborn, Clemens:
Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A : Implications for Protein Deacylase Drug Development.
In: Journal of Medicinal Chemistry. Bd. 61 (2018) Heft 23 . - S. 10922-10928.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.8b01455

2017

Moniot, Sébastien ; Forgione, Mariantonietta ; Lucidi, Alessia ; Hailu, Gebremedhin S. ; Nebbioso, Angela ; Carafa, Vincenzo ; Baratta, Francesca ; Altucci, Lucia ; Giacché, Nicola ; Passeri, Daniela ; Pellicciari, Roberto ; Mai, Antonello ; Steegborn, Clemens ; Rotili, Dante:
Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2 : Structure-Activity Relationship, X-ray Crystal Structure, and Anticancer Activity.
In: Journal of Medicinal Chemistry. Bd. 60 (2017) Heft 6 . - S. 2344-2360.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.6b01609

Sundriyal, Sandeep ; Moniot, Sébastien ; Mahmud, Zimam ; Yao, Shang ; di Fruscia, Paolo ; Reynolds, Christopher R. ; Dexter, David T. ; Sternberg, Michael J. E. ; Lam, Eric W.-F. ; Steegborn, Clemens ; Fuchter, Matthew J.:
Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket.
In: Journal of Medicinal Chemistry. Bd. 60 (2017) Heft 5 . - S. 1928-1945.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.6b01690

2016

Valente, Sergio ; Mellini, Paolo ; Spallotta, Francesco ; Carafa, Vincenzo ; Nebbioso, Angela ; Polletta, Lucia ; Carnevale, Ilaria ; Saladini, Serena ; Trisciuoglio, Daniela ; Gabellini, Chiara ; Tardugno, Maria ; Zwergel, Clemens ; Cencioni, Chiara ; Atlante, Sandra ; Moniot, Sébastien ; Steegborn, Clemens ; Budriesi, Roberta ; Tafani, Marco ; del Bufalo, Donatella ; Altucci, Lucia ; Gaetano, Carlo ; Mai, Antonello:
1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells.
In: Journal of Medicinal Chemistry. Bd. 59 (2016) Heft 4 . - S. 1471-1491.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.5b01117

2015

Roessler, Claudia ; Tüting, Christian ; Meleshin, Marat ; Steegborn, Clemens ; Schutkowski, Mike:
A Novel Continuous Assay for the Deacylase Sirtuin 5 and Other Deacetylases.
In: Journal of Medicinal Chemistry. Bd. 58 (2015) Heft 18 . - S. 7217-7223.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.5b00293

2011

Juli, Christina ; Sippel, Martin ; Jäger, Jens ; Thiele, Alexandra ; Weiwad, Matthias ; Schweimer, Kristian ; Rösch, Paul ; Steinert, Michael ; Sotriffer, Christoph ; Holzgrabe, Ulrike:
Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
In: Journal of Medicinal Chemistry. Bd. 54 (2011) Heft 1 . - S. 277-283.
ISSN 1520-4804
DOI: https://doi.org/10.1021/jm101156y

2008

Rothweiler, Ulli ; Czarna, Anna ; Weber, Lutz ; Popowicz, Grzegorz M. ; Brongel, Kinga ; Kowalska, Kaja ; Orth, Michael ; Stemmann, Olaf ; Holak, Tad A.:
NMR screening for lead compounds using tryptophan-mutated proteins.
In: Journal of Medicinal Chemistry. Bd. 51 (2008) Heft 16 . - S. 5035-5042.
ISSN 1520-4804
DOI: https://doi.org/10.1021/jm8002813

Schlicker, Christine ; Rauch, Annika ; Hess, Ken C. ; Kachholz, Barbara ; Levin, Lonny R. ; Buck, Jochen ; Steegborn, Clemens:
Structure-based development of novel adenylyl cyclase inhibitors.
In: Journal of Medicinal Chemistry. Bd. 51 (2008) Heft 15 . - S. 4456-4464.
ISSN 1520-4804
DOI: https://doi.org/10.1021/jm800481q

2002

Ewert, Kai ; Ahmad, Ayesha ; Evans, Heather M. ; Schmidt, Hans-Werner ; Safinya, Cyrus R.:
Efficient Synthesis and Cell-Transfection Properties of a New Multivalent Cationic Lipid for Nonviral Gene Delivery.
In: Journal of Medicinal Chemistry. Bd. 45 (2002) Heft 23 . - S. 5023-5029.
ISSN 1520-4804
DOI: https://doi.org/10.1021/jm020233w