D
Douglas R. Dougan
Researcher at Takeda Pharmaceutical Company
Publications - 32
Citations - 733
Douglas R. Dougan is an academic researcher from Takeda Pharmaceutical Company. The author has contributed to research in topics: Crystallization & Protein kinase A. The author has an hindex of 14, co-authored 32 publications receiving 625 citations.
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Journal ArticleDOI
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.
Morihisa Saitoh,Jun Kunitomo,Eiji Kimura,Hiroki Iwashita,Yumiko Uno,Tomohiro Onishi,Noriko Uchiyama,Tomohiro Kawamoto,Toshimasa Tanaka,Clifford D. Mol,Douglas R. Dougan,Garret P. Textor,Gyorgy Snell,Masayuki Takizawa,Fumio Itoh,Masakuni Kori +15 more
TL;DR: These compounds exhibited not only highly selective and potent inhibitory activity against GSK-3beta but also showed good pharmacokinetic profiles including favorable BBB penetration and significantly inhibited cold water stress-induced tau hyperphosphorylation in mouse brain.
Journal ArticleDOI
Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer
Qing Dong,Douglas R. Dougan,Xianchang Gong,Petro Halkowycz,Bohan Jin,Toufike Kanouni,Shawn M. O’Connell,Nicholas Scorah,Lihong Shi,Michael B. Wallace,Feng Zhou +10 more
TL;DR: A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design and lead optimization of this series led to the discovery of TAK-733.
Journal ArticleDOI
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Morihisa Saitoh,Jun Kunitomo,Eiji Kimura,Yoji Hayase,Hiromi Kobayashi,Noriko Uchiyama,Tomohiro Kawamoto,Toshimasa Tanaka,Clifford D. Mol,Douglas R. Dougan,Garret S. Textor,Gyorgy Snell,Fumio Itoh +12 more
TL;DR: Among these inhibitors, compound 20x showed highly selective and potent GSK-3beta inhibitory activity in vitro and its binding mode was determined by obtaining the X-ray co-crystal structure of 20x and GK3beta.
Journal ArticleDOI
Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton’s Tyrosine Kinase
Smith Christopher,Douglas R. Dougan,Mallareddy Komandla,Toufike Kanouni,Beverly M. Knight,J. David Lawson,Mark Sabat,Ewan Taylor,Phong H. Vu,Corey Wyrick +9 more
TL;DR: The discovery and optimization of a series of 4-aminocinnoline-3-carboxamide inhibitors of Bruton's tyrosine kinase are reported, resulting in the identification of a lead compound which reduced paw swelling in a dose- and exposure-dependent fashion in a rat model of collagen-induced arthritis.
Journal ArticleDOI
Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors
Michael B. Wallace,Mark E. Adams,Toufike Kanouni,Clifford D. Mol,Douglas R. Dougan,Feher Victoria,Shawn M. O’Connell,Lihong Shi,Petro Halkowycz,Qing Dong +9 more
TL;DR: A novel series of pyrrole inhibitors of MEK kinase has been developed using structure-based drug design and Optimization of the series led to the identification of potent inhibitors with good pharmaceutical properties.