Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer

Selective inhibition of exclusively transcription‐regulating PTEFb/CDK9 is a promising new approach in cancer therapy. Starting from lead compound BAY‐958, lead optimization efforts strictly focusing on kinase selectivity, physicochemical and DMPK properties finally led to the identification of the...

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Foilsithe in:ChemMedChem
Main Authors: Lücking, Ulrich, Scholz, Arne, Lienau, Philip, Siemeister, Gerhard, Kosemund, Dirk, Bohlmann, Rolf, Briem, Hans, Terebesi, Ildiko, Meyer, Kirstin, Prelle, Katja, Denner, Karsten, Bömer, Ulf, Schäfer, Martina, Eis, Knut, Valencia, Ray, Ince, Stuart, von Nussbaum, Franz, Mumberg, Dominik, Ziegelbauer, Karl, Klebl, Bert, Choidas, Axel, Nussbaumer, Peter, Baumann, Matthias, Schultz‐Fademrecht, Carsten, Rühter, Gerd, Eickhoff, Jan, Brands, Michael
Formáid: Artigo
Teanga:Inglês
Foilsithe: John Wiley and Sons Inc. 2017
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Rochtain Ar Líne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5698704/
https://ncbi.nlm.nih.gov/pubmed/28961375
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/cmdc.201700447
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