C
Celine Bonnefous
Researcher at Merck & Co.
Publications - 42
Citations - 2160
Celine Bonnefous is an academic researcher from Merck & Co.. The author has contributed to research in topics: Estrogen receptor & Metabotropic glutamate receptor 5. The author has an hindex of 24, co-authored 42 publications receiving 1965 citations. Previous affiliations of Celine Bonnefous include General Atomics & Memorial Sloan Kettering Cancer Center.
Papers
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Journal ArticleDOI
ARN-509: A Novel Antiandrogen for Prostate Cancer Treatment
Nicola J. Clegg,John Wongvipat,James Joseph,Chris Tran,Samedy Ouk,Anna Dilhas,Yu Chen,Kate Grillot,Eric D. Bischoff,Ling Cai,Anna Aparicio,Steven Dorow,Vivek K. Arora,Gang Shao,Jing Qian,Hong Zhao,Guangbin Yang,Chunyan Cao,John Sensintaffar,Teresa Wasielewska,Herbert Mark R,Celine Bonnefous,Beatrice Darimont,Howard I. Scher,Peter Smith-Jones,Mark Klang,Nicholas D. Smith,Elisa de Stanchina,Nian Wu,Ouathek Ouerfelli,Peter J. Rix,Richard A. Heyman,Michael E. Jung,Charles L. Sawyers,Jeffrey H. Hager +34 more
TL;DR: ARS-509 exhibits characteristics predicting a higher therapeutic index with a greater potential to reach maximally efficacious doses in man than current AR antagonists, and offers preclinical proof of principle for ARN-509 as a promising therapeutic in bothCastration-sensitive and castration-resistant forms of prostate cancer.
Journal ArticleDOI
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts
Andiliy G. Lai,Mehmet Kahraman,Steven P. Govek,Johnny Y. Nagasawa,Celine Bonnefous,Jackie Julien,Karensa L. Douglas,John Sensintaffar,Nhin Lu,Kyoung-Jin Lee,Anna Aparicio,Josh Kaufman,Jing Qian,Gang Shao,Rene Prudente,Michael J. Moon,James Joseph,Beatrice Darimont,Daniel Brigham,Kate Grillot,Richard A. Heyman,Peter J. Rix,Jeffrey H. Hager,Nicholas D. Smith +23 more
TL;DR: The identification and characterization of a series of small-molecule, orally bioavailable SERDs which are potent antagonists and degraders of ER-α and in which the ER- α degrading properties were prospectively optimized are described.
Journal ArticleDOI
Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers
Terence G. Hamill,Stephen Krause,Christine Ryan,Celine Bonnefous,Steve Govek,T. Jon Seiders,Nicholas D. P. Cosford,Jeffrey R. Roppe,Theodore M. Kamenecka,Shil Patel,Raymond E. Gibson,Sandra Sanabria,Kerry Riffel,Wai-Si Eng,Christopher D. King,Xiaoqing Yang,Mitchell D. Green,Stacey O'Malley,Richard Hargreaves,H. Donald Burns +19 more
TL;DR: PET imaging studies in monkey showed that all three tracers readily enter the brain and provide an mGluR5‐specific signal in all gray matter regions, including the cerebellum, which was confirmed by the autoradiographic studies and saturation binding experiments that showed tracer binding in the Cerebellum of rhesus monkeys.
Patent
Heterocyclic modulators of gpr119 for treatment of disease
TL;DR: In this article, the present invention relates to compounds and methods which may be useful as inhibitors of GPR119 for the treatment or prevention of metabolic, cardiovascular, and metabolic diseases.
Journal ArticleDOI
The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer
James Joseph,Beatrice Darimont,Wei Zhou,Alfonso Arrazate,Amy Young,Ellen Ingalla,Kimberly Walter,Robert A. Blake,Jim Nonomiya,Zhengyu Guan,Lorna Kategaya,Steven P. Govek,Andiliy G. Lai,Mehmet Kahraman,Dan Brigham,John Sensintaffar,Nhin Lu,Gang Shao,Jing Qian,Kate Grillot,Michael Moon,Rene Prudente,Eric D. Bischoff,Kyoung Jin Lee,Celine Bonnefous,Karensa L. Douglas,Julien Jackaline D,Johnny Y. Nagasawa,Anna Aparicio,Josh Kaufman,Benjamin Haley,Jennifer M. Giltnane,Ingrid E. Wertz,Mark R. Lackner,Michelle Nannini,Deepak Sampath,Luis J. Schwarz,Henry C. Manning,Mohammed N. Tantawy,Carlos L. Arteaga,Richard A. Heyman,Peter J. Rix,Lori Friedman,Nicholas D. Smith,Ciara Metcalfe,Jeffrey H. Hager +45 more
TL;DR: A novel, non-steroidal, orally bioavailable selective ER downregulator (SERD), which was identified by prospectively optimizing ERα degradation, antagonism and pharmacokinetic properties, and induces a distinct ERα conformation, relative to that induced by currently approved therapeutics, suggesting a unique mechanism of action.