Discovery and Biological Evaluation of Potent and Selective N-Methylene Saccharin-Derived Inhibitors for Rhomboid Intramembrane Proteases

Author:

Goel Parul12,Jumpertz Thorsten1,Mikles David C.3,Tichá Anežka3,Nguyen Minh T. N.4,Verhelst Steven45,Hubalek Martin3,Johnson Darren C.6,Bachovchin Daniel A.6,Ogorek Isabella1,Pietrzik Claus U.7,Strisovsky Kvido3ORCID,Schmidt Boris2ORCID,Weggen Sascha1ORCID

Affiliation:

1. Department of Neuropathology, Heinrich-Heine University Duesseldorf, Moorenstrasse 5, 40225 Duesseldorf, Germany

2. Clemens Schoepf Institute for Organic Chemistry and Biochemistry, Technical University of Darmstadt, Alarich-Weiss-Strasse 4-8, 64287 Darmstadt, Germany

3. Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Flemingovo n. 2, 166 10 Praha 6, Czech Republic

4. Chemical Proteomics Group, Leibnitz Institute for Analytical Sciences (ISAS) e.V., Otto-Hahn-Strasse 6b, 44227 Dortmund, Germany

5. Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, University of Leuven, Herestraat 49, Box 802, 3000 Leuven, Belgium

6. Chemical Biology Program, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, Box 428, New York, New York 10065, United States

7. Institute for Pathobiochemistry, University Medical Center of the Johannes Gutenberg University Mainz, Duesbergweg 6, 55128 Mainz, Germany

Funder

Bundesministerium f?r Bildung und Forschung

FP7 People: Marie-Curie Actions

Ministerstvo ?kolstv?, Ml?de?e a Telov?chovy

Deutsche Forschungsgemeinschaft

Akademie Ved Cesk? Republiky

Memorial Sloan-Kettering Cancer Center

National Institute of General Medical Sciences

European Molecular Biology Organization

Josie Robertson Foundation

Ministerium f?r Innovation, Wissenschaft und Forschung des Landes Nordrhein-Westfalen

Senatsverwaltung f?r Wirtschaft, Technologie und Forschung, Berlin

Publisher

American Chemical Society (ACS)

Subject

Biochemistry

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