D
Deena Waddleton
Researcher at Merck & Co.
Publications - 9
Citations - 467
Deena Waddleton is an academic researcher from Merck & Co.. The author has contributed to research in topics: Protein tyrosine phosphatase & Binding site. The author has an hindex of 8, co-authored 9 publications receiving 421 citations.
Papers
More filters
Journal ArticleDOI
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
Renata Oballa,Liette Belair,W. Cameron Black,Kelly Bleasby,Chi-Chung Chan,Carole Desroches,Xiaobing Du,R. Gordon,Jocelyne Guay,Sébastien Guiral,Michael J. Hafey,Emelie Hamelin,Zheng Huang,Brian P. Kennedy,Nicolas Lachance,Chun Sing Li,Joseph A. Mancini,Denis Normandin,Alessandro Pocai,David A. Powell,Yeeman K. Ramtohul,Kathryn Skorey,Dan Sørensen,Wayne Sturkenboom,Angela Styhler,Deena Waddleton,Hao Wang,Simon Wong,Lijing Xu,Lei Zhang +29 more
TL;DR: The discovery of MK-8245 is found, a potent, liver-targeted SCD inhibitor with preclinical antidiabetic and antidyslipidemic efficacy with a significantly improved therapeutic window.
Journal ArticleDOI
The structural basis for the selectivity of benzotriazole inhibitors of PTP1B
Giovanna Scapin,Sangita B. Patel,Joseph W. Becker,Qingping Wang,Caroline Desponts,Deena Waddleton,Kathryn Skorey,Wanda Cromlish,Christopher I. Bayly,Michel Therien,Jacques Yves Gauthier,Chun Sing Li,Cheuk K. Lau,Chidambaram Ramachandran,Brian P. Kennedy,Ernest Asante-Appiah +15 more
TL;DR: In this article, the crystal structures of protein tyrosine phosphatase 1B (PTP1B) in complex with first and second generation aryldifluoromethyl-phosphonic acid inhibitors were reported.
Journal ArticleDOI
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Cheuk K. Lau,Christopher I. Bayly,Jacques Yves Gauthier,Chun Sing Li,Michel Therien,Ernest Asante-Appiah,Wanda Cromlish,Yves Boie,Farnaz Forghani,Sylvie Desmarais,Qingping Wang,Kathryn Skorey,Deena Waddleton,Paul Payette,Chidambaram Ramachandran,Brian P. Kennedy,Giovana Scapin +16 more
TL;DR: Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphatase.
Journal ArticleDOI
Phosphodiesterase 3 and 4 comprise the major cAMP metabolizing enzymes responsible for insulin secretion in INS-1 (832/13) cells and rat islets.
Deena Waddleton,Weizhen Wu,Yue Feng,Chris M. Thompson,Michael Wu,Yun-Ping Zhou,Andrew D. Howard,Nancy A. Thornberry,Jing Li,Joseph A. Mancini +9 more
TL;DR: The combination of PDE3 and PDE4 selective inhibitors demonstrate that these enzymes comprise a significant proportion of the cAMP metabolizing activity in INS-1 cells and rat islets.
Journal ArticleDOI
The development of potent non-peptidic PTP-1B inhibitors.
Claude Dufresne,Patrick Roy,Zhaoyin Wang,Ernest Asante-Appiah,Wanda Cromlish,Yves Boie,Farnaz Forghani,Sylvie Desmarais,Qingping Wang,Kathryn Skorey,Deena Waddleton,Chidambaram Ramachandran,Brian P. Kennedy,Lijing Xu,Robert Gordon,Chi-Chung Chan,Yves Leblanc +16 more
TL;DR: The SAR from peptide libraries was exploited to design a series of potent deoxybenzoin PTP-1B inhibitors that were orally bioavailable and active in the animal models of non-insulin dependent diabetes mellitus (NIDDM).