MultiBacMam Bimolecular Fluorescence Complementation (BiFC) tool-kit identifies new small-molecule inhibitors of the CDK5-p25 protein-protein interaction (PPI)

Autor: Itxaso Bellon-Echeverria, Andrea Araujo Del Rosario, Jean Philippe Carralot, Imre Berger, Georg Schmid, Ralf Thoma, Harald Mauser, Stephanie Kueng

Publikováno v: Scientific Reports, Vol 8, Iss 1, Pp 1-10 (2018)
Scientific Reports
Bellón-Echeverría, I, Carralot, J P, Del Rosario, A A, Kueng, S, Mauser, H, Schmid, G, Thoma, R & Berger, I 2018, ' MultiBacMam Bimolecular Fluorescence Complementation (BiFC) tool-kit identifies new small-molecule inhibitors of the CDK5-p25 protein-protein interaction (PPI) ', Scientific Reports, vol. 8, 5083 . https://doi.org/10.1038/s41598-018-23516-x

Protein-protein interactions (PPIs) are at the core of virtually all biological processes in cells. Consequently, targeting PPIs is emerging at the forefront of drug discovery. Cellular assays which closely recapitulate native conditions in vivo are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::440d2b95ea6b1315058ef1382ca19ca5
http://link.springer.com/article/10.1038/s41598-018-23516-x

Design of Libraries Targeting Protein-Protein Interfaces

Autor: Kuo-Sen Huang, Paola Di Lello, Sung-Sau So, David C. Fry, Peter Mohr, Martin Stahl, Harald Mauser, Klaus Müller, Takeo Harada, Binh Thanh Vu

Publikováno v: ChemMedChem. 8:726-732

TARGETING PPIS: A novel strategy for designing libraries targeting protein-protein interfaces enabled us to identify diverse chemical entry points to interact with therapeutic targets for which conventional screening libraries delivered no or only fe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2aa2c6024f24914f292e1d8468b7ebf
https://doi.org/10.1002/cmdc.201200540

Substituted 2-oxo-azepane derivatives are potent, orally active γ-secretase inhibitors

Autor: Alexander Flohr, Pascale David-Pierson, Eric A. Kitas, Wolfgang Wostl, Harald Mauser, André Alker, Guido Galley, Dieter P. Reinhardt, Helmut Jacobsen, Laurence Ozmen, Roland Jakob-Roetne, Christian Czech

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:304-308

A hydroxamic acid screening hit 1 was elaborated to 5,5-dimethyl-2-oxoazepane derivatives exhibiting low nanomolar inhibition of γ-secretase, a key proteolytic enzyme involved in Alzheimer’s disease. Early ADME data showed a high metabolic clearan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78b6f51a292ea3a0364da0ecb41fd68f
https://doi.org/10.1016/j.bmcl.2007.10.074

Prediction of UV and ESI−MS Signal Intensities

Autor: Harald Mauser, Martin Stahl, Olivier Roche, Stephan Müller

Publikováno v: Journal of Chemical Information and Modeling. 45:1039-1046

All major pharmaceutical companies maintain large collections of compounds that are used either for screening against biological targets or as synthetic precursors. The quality assessment of these compounds is typically done by liquid chromatography

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::939d804c6c226e7a725073b7e572c32b
https://doi.org/10.1021/ci0496548

[Untitled]

Autor: Martin Stahl, Nikolay P. Todorov, Harald Mauser, Tim James, Philip M. Dean, Hans-Joachim Boehm

Publikováno v: Journal of Computer-Aided Molecular Design. 16:459-478

The de novo design program Skelgen has been used to design inhibitor structures for four targets of pharmaceutical interest. The designed structures are compared to modeled binding modes of known inhibitors (i) visually and (ii) by means of a novel s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fd6891a41357239f47d3c3909b87714d
https://doi.org/10.1023/a:1021242018286