AGC kinases, mechanisms of regulation ‎and innovative drug development

Autor: Alejandro E. Leroux, Ricardo M. Biondi, Jörg O. Schulze

Publikováno v: Seminars in Cancer Biology. 48:1-17

The group of AGC kinases consists of 63 evolutionarily related serine/threonine protein kinases comprising PDK1, PKB/Akt, SGK, PKC, PRK/PKN, MSK, RSK, S6K, PKA, PKG, DMPK, MRCK, ROCK, NDR, LATS, CRIK, MAST, GRK, Sgk494, and YANK, while two other fami

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::280836555d19adccd8a335ea0a7d721d
https://doi.org/10.1016/j.semcancer.2017.05.011

Bidirectional Allosteric Communication between the ATP-Binding Site and the Regulatory PIF Pocket in PDK1 Protein Kinase

Autor: Ricardo M. Biondi, Sonja Neimanis, Katrien Busschots, Pedro M. Alzari, Jörg O. Schulze, Evelyn Süß, Giorgio Saladino, Dalibor Odadzic, María-Natalia Lisa, Francesco Luigi Gervasio, Stefan Zeuzem, V. Hindie, Amanda K. Herbrand

Publikováno v: Cell Chemical Biology
Cell Chemical Biology, 2016, 23 (10), pp.1193-1205. ⟨10.1016/j.chembiol.2016.06.017⟩
Cell Chemical Biology, Cell Press, 2016, 23 (10), pp.1193-1205. ⟨10.1016/j.chembiol.2016.06.017⟩

Allostery is a phenomenon observed in many proteins where binding of a macromolecular partner or a small-molecule ligand at one location leads to specific perturbations at a site not in direct contact with the region where the binding occurs. The lis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d867b386e72af28a9d576ede95d57628
https://doi.org/10.1016/j.chembiol.2016.06.017

Discovery of a Potent Allosteric Kinase Modulator by Combining Computational and Synthetic Methods

Autor: Alexander Dömling, Carlos J. Camacho, Evelyn Süß, Jörg O. Schulze, Ricardo M. Biondi, Edwin Kroon

Publikováno v: Angewandte Chemie-International Edition, 54(47), 13933-13936. WILEY-V C H VERLAG GMBH

The rational design of allosteric kinase modulators is challenging but rewarding. The protein kinase PDK1, which lies at the center of the growth-factor signaling pathway, possesses an allosteric regulatory site previously validated both in vitro and

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https://doi.org/10.1002/ange.201506310

Molecular Mechanism of Regulation of the Atypical Protein Kinase C by N-terminal Domains and an Allosteric Small Compound

Autor: Ricardo M. Biondi, Katrien Busschots, Stefan Zeuzem, Ewgen Proschak, Jörg O. Schulze, Holger Stark, Jose M. Arencibia, Laura A. Lopez-Garcia, Sabine Amon, Hua Zhang, Thomas J. D. Jørgensen, Matthias Engel, Angelika F. Bauer, Sonja Neimanis, Adriana Stroba

Publikováno v: Zhang, H, Neimanis, S, Lopez-Garcia, L A, Arencibia, J M, Amon, S, Stroba, A, Zeuzem, S, Proschak, E, Stark, H, Bauer, A F, Busschots, K, Jørgensen, T J D, Engel, M, Schulze, J O & Biondi, R M 2014, ' Molecular mechanism of regulation of the atypical protein kinase C by N-terminal domains and an allosteric small compound ', Cell Chemical Biology, vol. 21, no. 6, pp. 754-65 . https://doi.org/10.1016/j.chembiol.2014.04.007

SummaryProtein kinases play important regulatory roles in cells and organisms. Therefore, they are subject to specific and tight mechanisms of regulation that ultimately converge on the catalytic domain and allow the kinases to be activated or inhibi

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https://doi.org/10.1016/j.chembiol.2014.04.007

Neutralisation of factor VIII inhibitors by anti-idiotypes isolated from phage-displayed libraries

Autor: Dirk Schwabe, Christoph Königs, Diana Stichel, Anja Schmidt, Markus Braner, Kerstin Brettschneider, Aleksander Orlowski, J. Kahle, Robert Tampé, Jörg O. Schulze, Karin Becker-Peters

Publikováno v: Thrombosis and haemostasis. 116(1)

SummaryFollowing replacement therapy with coagulation factor VIII (FVIII), up to 30 % of haemophilia A patients develop FVIII-specific inhibitory antibodies (FVIII inhibitors). Immune tolerance induction (ITI) is not always successful, resulting in a

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https://pubmed.ncbi.nlm.nih.gov/27009573