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8 results on '"Brause, Alexandra"'

3. The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation

Author

Flegel, Jana, primary, Shaaban, Saad, additional, Jia, Zhi Jun, additional, Schulte, Britta, additional, Lian, Yilong, additional, Krzyzanowski, Adrian, additional, Metz, Malte, additional, Schneidewind, Tabea, additional, Wesseler, Fabian, additional, Flegel, Anke, additional, Reich, Alisa, additional, Brause, Alexandra, additional, Xue, Gang, additional, Zhang, Minghao, additional, Dötsch, Lara, additional, Stender, Isabelle D., additional, Hoffmann, Jan-Erik, additional, Scheel, Rebecca, additional, Janning, Petra, additional, Rastinejad, Fraydoon, additional, Schade, Dennis, additional, Strohmann, Carsten, additional, Antonchick, Andrey P., additional, Sievers, Sonja, additional, Moura-Alves, Pedro, additional, Ziegler, Slava, additional, and Waldmann, Herbert, additional

Published
2022
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6. Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß

Author

Kremer, Lea, primary, Hennes, Elisabeth, additional, Brause, Alexandra, additional, Ursu, Andrei, additional, Robke, Lucas, additional, Matsubayashi, Hideaki T., additional, Nihongaki, Yuta, additional, Flegel, Jana, additional, Mejdrová, Ivana, additional, Eickhoff, Jan, additional, Baumann, Matthias, additional, Nencka, Radim, additional, Janning, Petra, additional, Kordes, Susanne, additional, Schöler, Hans R., additional, Sterneckert, Jared, additional, Inoue, Takanari, additional, Ziegler, Slava, additional, and Waldmann, Herbert, additional

Published
2019
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7. Chemical Genetics Reveals a Role of dCTP Pyrophosphatase 1 in Wnt Signaling

Author

Friese, Alexandra, primary, Kapoor, Shobhna, additional, Schneidewind, Tabea, additional, Vidadala, Srinivasa Rao, additional, Sardana, Juhi, additional, Brause, Alexandra, additional, Förster, Tim, additional, Bischoff, Matthias, additional, Wagner, Jessica, additional, Janning, Petra, additional, Ziegler, Slava, additional, and Waldmann, Herbert, additional

Published
2019
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8. Monovalent Pseudo-Natural Product Degraders Supercharge the Native Degradation of IDO1 by KLHDC3.

Author

Hennes E, Lucas B, Scholes NS, Cheng XF, Scott DC, Bischoff M, Reich K, Gasper R, Lucas M, Xu TT, Pulvermacher LM, Dötsch L, Imrichova H, Brause A, Naredla KR, Sievers S, Kumar K, Janning P, Gersch M, Murray PJ, Schulman BA, Winter GE, Ziegler S, and Waldmann H

Abstract

Targeted protein degradation (TPD) modulates protein function beyond inhibition of enzyme activity or protein-protein interactions. Most degraders function by proximity induction, and directly bridge an E3 ligase with the target to be degraded. However, many proteins might not be addressable via proximity-based degraders, and other challenges, such as resistance acquisition, exist. Here, we identified pseudo-natural products derived from (-)-myrtanol, termed iDegs, that inhibit and induce degradation of the immunomodulatory enzyme indoleamine-2,3-dioxygenase 1 (IDO1) by a distinct mechanism. iDegs induce a unique conformational change and, thereby, boost IDO1 ubiquitination and degradation by the cullin-RING E3 ligase CRL2 KLHDC3 , which we identified to also mediate native IDO1 degradation. Therefore, iDegs supercharge the native proteolytic pathway of IDO1, rendering this mechanism of action distinct from traditional degrader approaches involving proteolysis-targeting chimeras (PROTACs) or molecular-glue degraders (MGDs). In contrast to clinically explored IDO1 inhibitors, iDegs reduce formation of kynurenine by both inhibition and induced degradation of the enzyme and should also modulate non-enzymatic functions of IDO1. This unique mechanism of action may open up new therapeutic opportunities for the treatment of cancer beyond classical inhibition of IDO1.

Published
2024
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