BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models

The MCL1 gene is frequently amplified in cancer and codes for the antiapoptotic protein myeloid cell leukemia 1 (MCL1), which confers resistance to the current standard of care. Therefore, MCL1 is an attractive anticancer target. Here we describe BRD-810 as a potent and selective MCL1 inhibitor and...

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Veröffentlicht in:	Nature cancer 2024-10, Vol.5 (10), p.1479-1493
Hauptverfasser:	Rauh, Ulrike, Wei, Guo, Serrano-Wu, Michael, Kosmidis, Georgios, Kaulfuss, Stefan, Siegel, Franziska, Thede, Kai, McFarland, James, Lemke, Christopher T., Werbeck, Nicolas, Nowak-Reppel, Katrin, Pilari, Sabine, Menz, Stephan, Ocker, Matthias, Zhang, Weiqun, Davis, Kyle, Poncet-Montange, Guillaume, Roth, Jennifer, Daniels, Douglas, Kaushik, Virendar K., Hubbard, Brian, Ziegelbauer, Karl, Golub, Todd R.
Format:	Artikel
Sprache:	eng
Schlagworte:	13/1 13/2 13/51 14 38 38/43 38/47 38/77 631/67 631/80/82/23 64 64/60 692/4028/67/1059/153 82 82/103 82/83 96 96/95 Animals Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Apoptosis - drug effects Biomedical and Life Sciences Cell Line, Tumor Cell Survival - drug effects Female Hematologic Neoplasms - drug therapy Humans Life Sciences Mice Myeloid Cell Leukemia Sequence 1 Protein - antagonists & inhibitors Xenograft Model Antitumor Assays
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