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Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.

Autor: Freeman DB; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Hopkins TD; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Mikochik PJ; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Vacca JP; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Gao H; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Naylor-Olsen A; Naylor Olsen Consulting, LLC, 3369 Saddle Wood Court, Lansdale, Pennsylvania 19446, United States., Rudra S; TCG Lifesciences Private Limited, Block BN, Plot 7, Salt-lake Electronics Complex, Sector V, Kolkata 700091, West Bengal, India., Li H; WuXi AppTec (Tianjin) Co., Ltd., 168 NanHai Road, 10th Avenue, TEDA, Tianjin 300457, P. R. China., Pop MS; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Villagomez RA; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Lee C; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Li H; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Zhou M; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Saffran DC; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Rioux N; Certara Strategic Consulting, 100 Overlook Center, Suite 101, Princeton, New Jersey 08540, United States., Hood TR; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Day MAL; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., McKeown MR; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Lin CY; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Bischofberger N; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States., Trotter BW; Kronos Bio, Inc., 301 Binney Street, 2nd Floor East, Cambridge, Massachusetts 02142, United States.; Kronos Bio, Inc., 1300 So. El Camino Real Suite 400, San Mateo, California 94402, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2023 Dec 14; Vol. 66 (23), pp. 15629-15647. Date of Electronic Publication: 2023 Nov 15.

Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors.

Autor: Richters A; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; MIT Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Doyle SK; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; MIT Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA., Freeman DB; Kronos Bio, Inc., Cambridge, MA 02139, USA., Lee C; Kronos Bio, Inc., Cambridge, MA 02139, USA., Leifer BS; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; MIT Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Jagannathan S; Therapeutic Innovation Center, Department of Biochemistry and Molecular Biology, Baylor College of Medicine, Houston, TX 77030, USA., Kabinger F; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; MIT Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Koren JV; Therapeutic Innovation Center, Department of Biochemistry and Molecular Biology, Baylor College of Medicine, Houston, TX 77030, USA., Struntz NB; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; MIT Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Urgiles J; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Harvard-MIT Health Sciences and Technology, Boston, MA 02115, USA., Stagg RA; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Department of Biology, Boston University, Boston, MA 02215, USA., Curtin BH; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; MIT Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Chatterjee D; Goethe-Universität Frankfurt, 60438 Frankfurt am Main, Germany., Mathea S; Goethe-Universität Frankfurt, 60438 Frankfurt am Main, Germany., Mikochik PJ; Kronos Bio, Inc., Cambridge, MA 02139, USA., Hopkins TD; Kronos Bio, Inc., Cambridge, MA 02139, USA., Gao H; Kronos Bio, Inc., Cambridge, MA 02139, USA., Branch JR; Janssen Research & Development, LLC, Spring House, PA, USA., Xin H; Janssen Research & Development, LLC, Spring House, PA, USA., Westover L; Janssen Research & Development, LLC, Spring House, PA, USA., Bignan GC; Janssen Research & Development, LLC, Spring House, PA, USA., Rupnow BA; Janssen Research & Development, LLC, Spring House, PA, USA., Karlin KL; Therapeutic Innovation Center, Department of Biochemistry and Molecular Biology, Baylor College of Medicine, Houston, TX 77030, USA., Olson CM; Therapeutic Innovation Center, Department of Biochemistry and Molecular Biology, Baylor College of Medicine, Houston, TX 77030, USA., Westbrook TF; Therapeutic Innovation Center, Department of Biochemistry and Molecular Biology, Baylor College of Medicine, Houston, TX 77030, USA., Vacca J; Kronos Bio, Inc., Cambridge, MA 02139, USA., Wilfong CM; Kronos Bio, Inc., Cambridge, MA 02139, USA., Trotter BW; Kronos Bio, Inc., Cambridge, MA 02139, USA., Saffran DC; Kronos Bio, Inc., Cambridge, MA 02139, USA., Bischofberger N; Kronos Bio, Inc., Cambridge, MA 02139, USA., Knapp S; Goethe-Universität Frankfurt, 60438 Frankfurt am Main, Germany., Russo JW; Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA., Hickson I; Janssen Research & Development, LLC, Spring House, PA, USA; Cancer Research UK Newcastle Drug Discovery Unit, Translational and Clinical Research Institute, Newcastle University, Newcastle upon Tyne NE2 4HH, UK., Bischoff JR; Janssen Research & Development, LLC, Spring House, PA, USA., Gottardis MM; Janssen Research & Development, LLC, Spring House, PA, USA., Balk SP; Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA., Lin CY; Kronos Bio, Inc., Cambridge, MA 02139, USA; Therapeutic Innovation Center, Department of Biochemistry and Molecular Biology, Baylor College of Medicine, Houston, TX 77030, USA; Department of Molecular and Human Genetics, Baylor College of Medicine, Houston, TX, USA., Pop MS; Kronos Bio, Inc., Cambridge, MA 02139, USA., Koehler AN; David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; MIT Center for Precision Cancer Medicine, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA. Electronic address: koehler@mit.edu.

Publikováno v: Cell chemical biology [Cell Chem Biol] 2021 Feb 18; Vol. 28 (2), pp. 134-147.e14. Date of Electronic Publication: 2020 Oct 20.