M
Melody Diamond
Researcher at GlaxoSmithKline
Publications - 15
Citations - 1206
Melody Diamond is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Cell growth & Phosphoinositide 3-kinase. The author has an hindex of 10, co-authored 15 publications receiving 1124 citations. Previous affiliations of Melody Diamond include DuPont.
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Journal ArticleDOI
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin
Steven D. Knight,Nicholas D. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Michael G. Darcy,Carla A. Donatelli,Juan I. Luengo,Ken A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J,Glenn S. Van Aller,Jeffrey D. Carson,Melody Diamond,Patricia A. Elkins,Christine M. Gardiner,Eric Garver,Seth A. Gilbert,Richard R. Gontarek,Jeffrey R. Jackson,Kevin L. Kershner,Lusong Luo,Kaushik Raha,Christian S. Sherk,Chiu-Mei Sung,David Sutton,Peter J. Tummino,Ronald Wegrzyn,Kurt R. Auger,Dashyant Dhanak +30 more
TL;DR: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3- pyridinyl}benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
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Antitumor activity of an allosteric inhibitor of centromere-associated protein-E
Kenneth Wood,Latesh Lad,Lusong Luo,Xiangping Qian,Steven D. Knight,Neysa Nevins,Katjuša Brejc,David Sutton,Aidan G. Gilmartin,Penelope Chua,Radhika Desai,Stephen Schauer,Dean E. McNulty,Roland S. Annan,Lisa D. Belmont,Carmen García,Yan Lee,Melody Diamond,Leo F. Faucette,Michele Giardiniere,Shu-Yun Zhang,Chiu-Mei Sun,Justin D. Vidal,Serge Lichtsteiner,William K. Cornwell,Joel Greshock,Richard Wooster,Jeffrey T. Finer,Robert A. Copeland,Pearl S. Huang,David J. Morgans,Dashyant Dhanak,Gustave Bergnes,Roman Sakowicz,Jeffrey R. Jackson +34 more
TL;DR: Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of C Enp-E to microtubules is insufficient to satisfy the mitotic checkpoint.
Journal ArticleDOI
Human mdm2 Mediates Multiple Mono-ubiquitination of p53 by a Mechanism Requiring Enzyme Isomerization *
Zhihong Lai,Katherine V. Ferry,Melody Diamond,Kevin E. Wee,Young B. Kim,Jianhong Ma,Tao Yang,Pamela A. Benfield,Robert A. Copeland,Kurt R. Auger +9 more
TL;DR: It is shown that the multistep cascade of mdm2-mediated p53 ubiquitination can be reduced to three purified recombinant proteins: ubiquitin-conjugated E2, mDM2, and p53, and it is found that p53 is modified with multiple mono-ubiquitin moieties as opposed to a poly-ubsin chain.
Journal ArticleDOI
Differentiation of Hdm2-mediated p53 ubiquitination and Hdm2 autoubiquitination activity by small molecular weight inhibitors
Zhihong Lai,Tao Yang,Young B. Kim,Thais M. Sielecki,Melody Diamond,Peter R. Strack,Mark Rolfe,Maureen Caligiuri,Pamela A. Benfield,Kurt R. Auger,Robert A. Copeland +10 more
TL;DR: These compounds establish the feasibility of selectively blocking hdm2-mediated ubiquitination of p53 by small molecule inhibitors, and provide a novel mechanism for the development of new chemotherapeutics for the treatment of human cancers.
Journal ArticleDOI
Distinct Concentration-Dependent Effects of the Polo-like Kinase 1-Specific Inhibitor GSK461364A,Including Differential Effect on Apoptosis
Aidan G. Gilmartin,Maureen R. Bleam,Mark Richter,Symon G. Erskine,Ryan G. Kruger,Lenore Madden,Daniel F. Hassler,Gary K. Smith,Richard R. Gontarek,Mary P. Courtney,David Sutton,Melody Diamond,Jeffrey R. Jackson,Sylvie Laquerre +13 more
TL;DR: A potent, selective, reversible, ATP-competitive inhibitor of Plk1, GSK461364A, capable of inhibiting cell growth of most proliferating cancer cell lines tested is identified and observed.