Dapeng Chen
Merck & Co.
12 Papers
29 Citations
Dapeng Chen is an academic researcher from Merck & Co.. The author has contributed to research in topics: Medicine & Chemistry. The author has an hindex of 4, co-authored 9 publications.
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Papers
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
Ryan V Quiroz,Michael H. Reutershan,Sebastian Schneider,David L. Sloman,Brian M. Lacey,Brooke M Swalm,Charles S. Yeung,Craig R. Gibeau,Daniel S. Spellman,Danica A. Rankic,Dapeng Chen,David J. Witter,Doug Linn,Erik Munsell,Guo Feng,Haiyan Xu,Jonathan M E Hughes,Jongwon Lim,Josep Saurí,Kristin Geddes,Murray Wan,My Sam Mansueto,Nicole Follmer,Patrick S. Fier,Phieng Siliphaivanh,Pierre Daublain,Rachel L. Palte,Robert P Hayes,Sandra Lee,Shuhei Kawamura,Steven M. Silverman,Sulagna Sanyal,Timothy J. Henderson,Yingchun Ye,Yuanwei Gao,Benjamin Nicholson,Michelle R. Machacek +36 more
TL;DR: In this article, the structure-based drug designs, robust synthetic efforts, and lead optimization strategies toward the identification of two novel 5,5-fused bicyclic nucleoside-derived classes of potent and efficacious protein arginine methyltransferase 5 inhibitors are presented.
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Discovery of MK-4688: an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction.
Michael H. Reutershan,Michelle R. Machacek,Michael D. Altman,Stephane L. Bogen,Mingmei Cai,Carolyn Michele Cammarano,Dapeng Chen,Matthew Christopher,John G. Cryan,Pierre Daublain,Xavier Fradera,Prasanthi Geda,Peter Goldenblatt,Armetta D. Hill,Raymond A. Kemper,Victoria Kutilek,Chaomin Li,Michelle Martinez,Mark A. McCoy,Latha G. Nair,Weidong Pan,Christopher F. Thompson,Giovanna Scapin,Manami Shizuka,Marianne L. Spatz,Dietrich Steinhuebel,Binyuan Sun,Matthew Ernst Voss,Xiao Wang,Liping Yang,Tammie C. Yeh,Isabelle Dussault,C. Gary Marshall,B. Wesley Trotter +33 more
TL;DR: In this paper, a purine carboxylic acid-derived inhibitor of the HDM2-p53 PPI, MK-4688 (compound 56), was proposed.
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Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors.
Joey L. Methot,Abdelghani Achab,Matthew Christopher,Hua Zhou,Meredeth A. McGowan,B. Wesley Trotter,Xavier Fradera,Charles A. Lesburg,Peter Goldenblatt,Armetta D. Hill,Dapeng Chen,Karin M. Otte,Martin Augustin,Sanjiv J. Shah,Jason D. Katz +14 more
TL;DR: By attenuating the lypophilicity and metabolic liabilities of an oxindole moiety, this work improved the preclinical species PK and solubility and reduced adenosine uptake activity and supported a low once-daily predicted human dose.
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The treatment of inflammatory bowel disease with monoclonal antibodies in Asia.
Yu Chen,Guolin Zhang,Yuewen Yang,Shuangshuang Zhang,Kang Song Tian,Arenbaoligao,Dapeng Chen +6 more
TL;DR: In this paper , a review comprehensively summarizes the clinical reports and studies related to the use of monoclonal antibodies for the treatment of inflammatory bowel disease in Asian countries and regions in recent years.
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Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
David L. Sloman,Njamkou Noucti,Michael D. Altman,Dapeng Chen,Andrea C. Mislak,Alexander A. Szewczak,Mansuo Hayashi,Lee Warren,Tammy Dellovade,Zhenhua Wu,Jacob Marcus,Deborah Walker,Hua-Poo Su,Suzanne C. Edavettal,Sanjeev Munshi,Michael Hutton,Hugh Nuthall,Matthew G. Stanton +17 more
TL;DR: A unique cylcyclohexyldiamine scaffold was identified that led to remarkable improvements in potency, opening up opportunities to reduce MW, Pgp efflux and improve pharmacokinetic properties while also conferring improved solubility.
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