Zobrazeno 1 - 10
of 74
pro vyhledávání: '"Harald Weinstabl"'
Autor:
Lukas Junk, Volker M. Schmiedel, Somraj Guha, Katharina Fischel, Peter Greb, Kristin Vill, Violetta Krisilia, Lasse van Geelen, Klaus Rumpel, Parvinder Kaur, Ramya V. Krishnamurthy, Shridhar Narayanan, Radha Krishan Shandil, Mayas Singh, Christiane Kofink, Andreas Mantoulidis, Philipp Biber, Gerhard Gmaschitz, Uli Kazmaier, Anton Meinhart, Julia Leodolter, David Hoi, Sabryna Junker, Francesca Ester Morreale, Tim Clausen, Rainer Kalscheuer, Harald Weinstabl, Guido Boehmelt
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-15 (2024)
Abstract Antimicrobial resistance is a global health threat that requires the development of new treatment concepts. These should not only overcome existing resistance but be designed to slow down the emergence of new resistance mechanisms. Targeted
Externí odkaz:
https://doaj.org/article/762402cfc91745d09f200167975e5d00
Autor:
Christiane Kofink, Nicole Trainor, Barbara Mair, Simon Wöhrle, Melanie Wurm, Nikolai Mischerikow, Michael J. Roy, Gerd Bader, Peter Greb, Géraldine Garavel, Emelyne Diers, Ross McLennan, Claire Whitworth, Vesna Vetma, Klaus Rumpel, Maximilian Scharnweber, Julian E. Fuchs, Thomas Gerstberger, Yunhai Cui, Gabriela Gremel, Paolo Chetta, Stefan Hopf, Nicole Budano, Joerg Rinnenthal, Gerhard Gmaschitz, Moriz Mayer, Manfred Koegl, Alessio Ciulli, Harald Weinstabl, William Farnaby
Publikováno v:
Nature Communications, Vol 13, Iss 1, Pp 1-15 (2022)
Protein degraders are an emerging drug modality; however, their properties lie beyond typical drug-like space. Here the authors report optimisation via structure-based exit vector and linker design towards the VHL-recruiting PROTAC ACBI2, an orally b
Externí odkaz:
https://doaj.org/article/3f90550853c6402d8f154d10f8e2a18c
Autor:
Jiang-Ping Wu, Wei-Tong Dong, Chengsheng Chen, Alexander Sienkiewicz, Phouvieng Beyer, Jun Wang, Nizar Haddad, Jon C. Lorenz, Jonathan T. Reeves, Matthew H. Bunner, Nina C. Gonnella, Harald Weinstabl, Géraldine Garavel
Publikováno v:
Organic Process Research & Development. 27:788-797
Publikováno v:
Inducing Targeted Protein Degradation. :289-312
Autor:
Joachim Bröker, Alex G. Waterson, Chris Smethurst, Dirk Kessler, Jark Böttcher, Moriz Mayer, Gerhard Gmaschitz, Jason Phan, Andrew Little, Jason R. Abbott, Qi Sun, Michael Gmachl, Dorothea Rudolph, Heribert Arnhof, Klaus Rumpel, Fabio Savarese, Thomas Gerstberger, Nikolai Mischerikow, Matthias Treu, Lorenz Herdeis, Tobias Wunberg, Andreas Gollner, Harald Weinstabl, Andreas Mantoulidis, Oliver Krämer, Darryl B. McConnell, Stephen W. Fesik
Publikováno v:
Journal of Medicinal Chemistry. 65:14614-14629
Autor:
Thomas Scott, Christian Alan Paul Smethurst, Yvonne Westermaier, Moriz Mayer, Peter Greb, Roland Kousek, Tobias Biberger, Gerd Bader, Zuzana Jandova, Philipp S. Schmalhorst, Julian E. Fuchs, Aniket Magarkar, Christoph Hoenke, Thomas Gerstberger, Steven A. Combs, Richard Pape, Saksham Phul, Sandeepkumar Kothiwale, Andreas Bergner, Alex G. Waterson, Foldit Players, Harald Weinstabl, Darryl B. McConnell, Jark Böttcher, Jens Meiler, Rocco Moretti
Given the role of human intuition in current drug design efforts, crowd-sourced 'citizen scientist' games have the potential to greatly expand the pool of potential drug designers. Here, we introduce ‘Drugit', the small molecule design mode of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::287b3949d9d0ebf819f483d064d56529
https://doi.org/10.26434/chemrxiv-2023-lczzd
https://doi.org/10.26434/chemrxiv-2023-lczzd
Autor:
Juergen Ramharter, Michael Kulhanek, Maike Dettling, Gerhard Gmaschitz, Jale Karolyi-Oezguer, Harald Weinstabl, Andreas Gollner
Publikováno v:
Organic process researchdevelopment. 26(8)
Herein, we report the structure and synthesis of the potent MDM2-p53 inhibitor BI-0282. The complex spirooxindole scaffold bearing four stereocenters embedded in a rigid polycyclic ring-system was effectively prepared on a multi-gram scale in only fi
Autor:
David M. Hoi, Sabryna Junker, Lukas Junk, Kristin Schwechel, Katharina Fischel, David Podlesainski, Paige M.E. Hawkins, Lasse van Geelen, Farnusch Kaschani, Julia Leodolter, Francesca Ester Morreale, Stefan Kleine, Somraj Guha, Klaus Rumpel, Volker M. Schmiedel, Harald Weinstabl, Anton Meinhart, Richard J. Payne, Markus Kaiser, Markus Hartl, Guido Boehmelt, Uli Kazmaier, Rainer Kalscheuer, Tim Clausen
Publikováno v:
Cell. 186:2176-2192.e22
The ClpC1:ClpP1P2 protease is a core component of the proteostasis system in mycobacteria. To improve the efficacy of antitubercular agents targeting the Clp protease, we characterized the mechanism of the antibiotics cyclomarin A and ecumicin. Quant
Autor:
Andreas Gollner, Patrizia Sini, Dorothea Rudolph, Harald Weinstabl, Juergen Ramharter, Ulrike Weyer-Czernilofsky, Bojana Golubovic, Rolf Grempler, Alejandro Pérez Pitarch, Reinhard Sailer, Darryl B. McConnell, Norbert Kraut
Publikováno v:
Cancer Research. 83:LB003-LB003
The E3 ligase MDM2 controls the tumor suppressor function of p53, which is encoded by the TP53gene. Compounds designed to bind to MDM2 preventing its interaction with p53 restore the ability of p53 to combat the pathogenic processes that underly canc
Autor:
Andreas Gollner, Markus Köster, Paul Nicklin, Thomas Trieselmann, Elliott Klein, Jaromir Vlach, Claudia Heine, Marc Grundl, Jürgen Ramharter, David Wyatt, Menorca Chaturvedi, Alessio Ciulli, Katharine C. Carter, Susanne Müller, Daniel Bischoff, Peter Ettmayer, Eric Haaksma, Jürgen Mack, Darryl McConnell, Dirk Stenkamp, Harald Weinstabl, Matthias Zentgraf, Clive R. Wood, Florian Montel
Publikováno v:
Nature reviews. Drug discovery. 21(7)