Imlunestrant is an Oral, Brain-Penetrant Selective Estrogen Receptor Degrader with Potent Antitumor Activity in ESR1 Wildtype and Mutant Breast Cancer.

Autor: Bhagwat SV; Eli Lilly and Company, Indianapolis, Indiana, United States., Mur C; Eli Lilly and Company, Madrid, Spain., Vandekopple M; Eli Lilly and Company, Indianapolis, IN, United States., Zhao B; Eli Lilly and Company, Indianapolis, IN, United States., Shen W; Eli Lilly and Company, Indianapolis, Indiana, United States., Marugán C; Eli Lilly (Spain), Alcobendas, Madrid, Spain., Capen A; Eli Lilly and Company, Indianapolis, IN, United States., Kindler L; Eli Lilly and Company, Indianapolis, IN, United States., Stephens JR; Eli Lilly and Company, Indianapolis, Indiana, United States., Huber L; Eli Lilly and Company, Indianapolis, IN, United States., Castanares MA; Eli Lilly and Company, Indianapolis, IN, United States., Garcia-Tapia D; Eli Lilly and Company, Indianapolis, IN, United States., Cohen JD; Eli Lilly and Company, Indianapolis, IN, United States., Bastian J; Eli Lilly and Company, Indianapolis, IN, United States., Mattioni B; Eli Lilly and Company, Indianapolis, IN, United States., Yuen E; Eli Lilly and Company, United States., Baker TK; Eli Lilly and Company, United States., Rodriguez Cruz V; Eli Lilly and Company, United States., Fei D; Eli Lilly and Company, United States., Manro JR; Eli Lilly and Company, Indianapolis, IN, United States., Pulliam N; Eli Lilly and Company, Indianapolis, IN, United States., Dowless MS; Eli Lilly and Company, Indianapolis, Indiana, United States., Ortiz Ruiz MJ; Eli Lilly and Company, Madrid, Spain., Yu C; Lilly (China), Shanghai, Shanghai, China., Puca L; Eli Lilly (United States), New York, New York, United States., Klippel A; Eli Lilly and Company, New York City, New York, United States., Bacchion F; Eli Lilly and Company, Indianapolis, IN, United States., Ismail-Khan R; Eli Lilly and Company, Indianapolis, IN, United States., Rodrik-Outmezguine V; Eli Lilly and Company, Indianapolis, IN, United States., Peng SB; Eli Lilly and Company, Indianapolis, IN, United States., Lallena MJ; Eli Lilly and Company, Madrid, Spain., Gong X; Eli Lilly and Company, Indianapolis, Indiana, United States., de Dios A; Eli Lilly (United States), Indianapolis, United States.

Publikováno v: Cancer research [Cancer Res] 2024 Dec 09. Date of Electronic Publication: 2024 Dec 09.

Novel Methionine Aminopeptidase 2 Inhibitor M8891 Synergizes with VEGF Receptor Inhibitors to Inhibit Tumor Growth of Renal Cell Carcinoma Models.

Autor: Friese-Hamim M; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Ortiz Ruiz MJ; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Bogatyrova O; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Keil M; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Rohdich F; Discovery Technologies, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Blume B; Discovery Technologies, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Leuthner B; Discovery Technologies, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Czauderna F; Research Unit Oncology, EMD Serono Research & Development Institute Inc., Billerica, Massachusetts., Hahn D; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Jabs J; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Jaehrling F; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Heinrich T; Discovery Technologies, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Kellner R; Discovery Technologies, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Chan K; Donnelly Centre, University of Toronto, Toronto, Ontario, Canada., Tong AHY; Donnelly Centre, University of Toronto, Toronto, Ontario, Canada., Wienke D; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Moffat J; Donnelly Centre, University of Toronto, Toronto, Ontario, Canada.; Department of Molecular Genetics, University of Toronto, Toronto, Ontario, Canada.; Institute for Biomedical Engineering, University of Toronto, Toronto, Ontario, Canada., Blaukat A; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany., Zenke FT; Research Unit Oncology, Merck Healthcare KGaA, the healthcare business of Merck KGaA, Darmstadt, Germany.

Publikováno v: Molecular cancer therapeutics [Mol Cancer Ther] 2024 Feb 01; Vol. 23 (2), pp. 159-173.

De Novo Missense Substitutions in the Gene Encoding CDK8, a Regulator of the Mediator Complex, Cause a Syndromic Developmental Disorder.

Autor: Calpena E; Clinical Genetics Group, MRC Weatherall Institute of Molecular Medicine, University of Oxford, Oxford OX3 9DS, UK., Hervieu A; Cancer Research UK Cancer Therapeutics Unit, the Institute of Cancer Research, London SM2 5NG, UK., Kaserer T; Cancer Research UK Cancer Therapeutics Unit, the Institute of Cancer Research, London SM2 5NG, UK., Swagemakers SMA; Department of Pathology and Department of Bioinformatics, Erasmus University Medical Center, University Medical Center Rotterdam, PO Box 2040, 3000 CA, Rotterdam, the Netherlands., Goos JAC; Department of Plastic and Reconstructive Surgery, Erasmus MC, University Medical Center Rotterdam, PO Box 2040, 3000 CA, Rotterdam, the Netherlands., Popoola O; Cancer Research UK Cancer Therapeutics Unit, the Institute of Cancer Research, London SM2 5NG, UK., Ortiz-Ruiz MJ; Cancer Research UK Cancer Therapeutics Unit, the Institute of Cancer Research, London SM2 5NG, UK., Barbaro-Dieber T; Genetics Division, Cook Children's Medical Center, Fort Worth, TX 76102, USA., Bownass L; Department of Clinical Genetics, University Hospitals Bristol NHS Foundation Trust, St. Michael's Hospital, Bristol BS2 8EG, UK., Brilstra EH; Department of Genetics, University Medical Center Utrecht, Utrecht University, 3508 AB Utrecht, the Netherlands., Brimble E; Department of Neurology and Neurological Sciences, Stanford University School of Medicine, Stanford, CA 94305, USA., Foulds N; Wessex Clinical Genetics Services, University Hospital Southampton, Southampton SO16 5YA, UK., Grebe TA; Department of Child Health, University of Arizona College of Medicine, Division of Genetics and Metabolism, Phoenix Children's Hospital, Phoenix, AZ 85016, USA., Harder AVE; Department of Genetics, University Medical Center Utrecht, Utrecht University, 3508 AB Utrecht, the Netherlands., Lees MM; North Thames Regional Genetics Service, Great Ormond Street Hospital for Children NHS Foundation Trust, London WC1N 3EH, UK., Monaghan KG; GeneDx, Gaithersburg, MD 20877, USA., Newbury-Ecob RA; Department of Clinical Genetics, University Hospitals Bristol NHS Foundation Trust, St. Michael's Hospital, Bristol BS2 8EG, UK., Ong KR; Department of Clinical Genetics, Birmingham Women's and Children's NHS Foundation Trust, Birmingham B15 2TG, UK., Osio D; Department of Clinical Genetics, Birmingham Women's and Children's NHS Foundation Trust, Birmingham B15 2TG, UK., Reynoso Santos FJ; Genetics Division, Joe DiMaggio Children's Hospital, Hollywood, FL 33021, USA; Charles E. Schmidt College of Medicine, Florida Atlantic University, Hollywood, FL 33021, USA., Ruzhnikov MRZ; Department of Neurology and Neurological Sciences, Stanford University School of Medicine, Stanford, CA 94305, USA., Telegrafi A; GeneDx, Gaithersburg, MD 20877, USA., van Binsbergen E; Department of Genetics, University Medical Center Utrecht, Utrecht University, 3508 AB Utrecht, the Netherlands., van Dooren MF; Department of Clinical Genetics, Erasmus MC University Medical Center Rotterdam, PO Box 2040, 3000 CA, Rotterdam, the Netherlands., van der Spek PJ; Department of Pathology and Department of Bioinformatics, Erasmus University Medical Center, University Medical Center Rotterdam, PO Box 2040, 3000 CA, Rotterdam, the Netherlands., Blagg J; Cancer Research UK Cancer Therapeutics Unit, the Institute of Cancer Research, London SM2 5NG, UK., Twigg SRF; Clinical Genetics Group, MRC Weatherall Institute of Molecular Medicine, University of Oxford, Oxford OX3 9DS, UK., Mathijssen IMJ; Department of Plastic and Reconstructive Surgery, Erasmus MC, University Medical Center Rotterdam, PO Box 2040, 3000 CA, Rotterdam, the Netherlands., Clarke PA; Cancer Research UK Cancer Therapeutics Unit, the Institute of Cancer Research, London SM2 5NG, UK. Electronic address: paul.clarke@icr.ac.uk., Wilkie AOM; Clinical Genetics Group, MRC Weatherall Institute of Molecular Medicine, University of Oxford, Oxford OX3 9DS, UK. Electronic address: andrew.wilkie@imm.ox.ac.uk.

Publikováno v: American journal of human genetics [Am J Hum Genet] 2019 Apr 04; Vol. 104 (4), pp. 709-720. Date of Electronic Publication: 2019 Mar 21.

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases.

Autor: Clarke PA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Ortiz-Ruiz MJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., TePoele R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Adeniji-Popoola O; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Box G; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Court W; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Czasch S; Merck KGaA, Darmstadt, Germany., El Bawab S; Merck KGaA, Darmstadt, Germany., Esdar C; Merck KGaA, Darmstadt, Germany., Ewan K; School of Bioscience, Cardiff University, Cardiff, United Kingdom., Gowan S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., De Haven Brandon A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Hewitt P; Merck KGaA, Darmstadt, Germany., Hobbs SM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Kaufmann W; Merck KGaA, Darmstadt, Germany., Mallinger A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Raynaud F; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Roe T; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Rohdich F; Merck KGaA, Darmstadt, Germany., Schiemann K; Merck KGaA, Darmstadt, Germany., Simon S; Merck KGaA, Darmstadt, Germany., Schneider R; Merck KGaA, Darmstadt, Germany., Valenti M; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Weigt S; Merck KGaA, Darmstadt, Germany., Blagg J; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Blaukat A; Merck KGaA, Darmstadt, Germany., Dale TC; School of Bioscience, Cardiff University, Cardiff, United Kingdom., Eccles SA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Hecht S; Merck KGaA, Darmstadt, Germany., Urbahns K; Merck KGaA, Darmstadt, Germany., Workman P; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom., Wienke D; Merck KGaA, Darmstadt, Germany.

Publikováno v: ELife [Elife] 2016 Dec 09; Vol. 5. Date of Electronic Publication: 2016 Dec 09.

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.

Autor: Mallinger A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Schiemann K; Merck KGaA , Darmstadt, 64293, Germany., Rink C; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Stieber F; Merck KGaA , Darmstadt, 64293, Germany., Calderini M; Merck KGaA , Darmstadt, 64293, Germany., Crumpler S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Stubbs M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Adeniji-Popoola O; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Poeschke O; Merck KGaA , Darmstadt, 64293, Germany., Busch M; Merck KGaA , Darmstadt, 64293, Germany., Czodrowski P; Merck KGaA , Darmstadt, 64293, Germany., Musil D; Merck KGaA , Darmstadt, 64293, Germany., Schwarz D; Merck KGaA , Darmstadt, 64293, Germany., Ortiz-Ruiz MJ; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Schneider R; Merck KGaA , Darmstadt, 64293, Germany., Thai C; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Valenti M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., de Haven Brandon A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Burke R; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Workman P; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Dale T; School of Bioscience, Cardiff University , Cardiff, CF10 3AX, U.K., Wienke D; Merck KGaA , Darmstadt, 64293, Germany., Clarke PA; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Esdar C; Merck KGaA , Darmstadt, 64293, Germany., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Eccles SA; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K., Rohdich F; Merck KGaA , Darmstadt, 64293, Germany., Blagg J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2016 Feb 11; Vol. 59 (3), pp. 1078-101. Date of Electronic Publication: 2016 Jan 21.