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Wolfgang Sippl
Researcher at Martin Luther University of Halle-Wittenberg
Publications - 332
Citations - 10346
Wolfgang Sippl is an academic researcher from Martin Luther University of Halle-Wittenberg. The author has contributed to research in topics: Docking (molecular) & Virtual screening. The author has an hindex of 54, co-authored 297 publications receiving 8683 citations. Previous affiliations of Wolfgang Sippl include University of Freiburg & CAS-MPG Partner Institute for Computational Biology.
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Journal ArticleDOI
Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT
Patrice Dubreuil,Sébastien Letard,Marco A. Ciufolini,Laurent Gros,Martine Humbert,Nathalie Casteran,Laurence Borge,Berengere Hajem,Anne Lermet,Wolfgang Sippl,Edwige Voisset,Michel Arock,Christian Auclair,Phillip S. Leventhal,Colin Mansfield,Alain Moussy,Olivier Hermine +16 more
TL;DR: Masitinib is a potent and selective tyrosine kinase inhibitor targeting KIT that is active, orally bioavailable in vivo, and has low toxicity.
Journal ArticleDOI
Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells
Frédéric Colland,Etienne Formstecher,Xavier Jacq,Céline Reverdy,Cecile Planquette,Susan Conrath,Virginie Trouplin,Julie Bianchi,Vasily N. Aushev,Jacques Camonis,Alessandra Calabrese,Catherine Borg-Capra,Wolfgang Sippl,Vincent Collura,Guillaume Boissy,Jean-Christophe Rain,Philippe Guedat,Remi Delansorne,Laurent Daviet +18 more
TL;DR: HBX 41,108 is reported, a small-molecule compound that inhibits USP7 deubiquitinating activity with an IC50 in the submicromolar range, providing a structural basis for the development of new anticancer drugs.
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Discovery of Specific Inhibitors of Human USP7/HAUSP Deubiquitinating Enzyme
Céline Reverdy,Susan Conrath,Roman Lopez,Cecile Planquette,Cédric Atmanene,Vincent Collura,Jane Harpon,Véronique Battaglia,Valérie Vivat,Wolfgang Sippl,Frédéric Colland +10 more
TL;DR: The data presented in this report provide proof of principle that USP7 inhibitors may be a valuable therapeutic for cancer and the discovery of such molecules offers interesting tools for studying deubiquitination.
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Selective Sirt2 inhibition by ligand-induced rearrangement of the active site.
Tobias Rumpf,Matthias Schiedel,Berin Karaman,Claudia Roessler,Brian J. North,Attila Lehotzky,Judit Oláh,Kathrin I. Ladwein,Karin Schmidtkunz,Markus Gajer,Martin Pannek,Clemens Steegborn,David A. Sinclair,Stefan Gerhardt,Judit Ovádi,Mike Schutkowski,Wolfgang Sippl,Oliver Einsle,Manfred Jung +18 more
TL;DR: High-resolution structures of human Sirt2 in complex with highly selective drug-like inhibitors that show a unique inhibitory mechanism are presented and structural insights into this unique mechanism of selective sirtuin inhibition provide the basis for further inhibitor development and selective tools for sIRTuin biology.
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HDAC8: a multifaceted target for therapeutic interventions
Alokta Chakrabarti,Ina Oehme,Olaf Witt,Guilherme Oliveira,Wolfgang Sippl,Christophe Romier,Raymond J. Pierce,Manfred Jung +7 more
TL;DR: The current challenge remains in the development of potent selective inhibitors that would specifically target HDAC8 with fewer adverse effects compared with pan-HDAC inhibitors.