S
Sam Gillette
Researcher at Plexxikon
Publications - 9
Citations - 2545
Sam Gillette is an academic researcher from Plexxikon. The author has contributed to research in topics: Kinase & Phosphodiesterase. The author has an hindex of 8, co-authored 9 publications receiving 2429 citations.
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Journal ArticleDOI
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
James Tsai,John T. Lee,Weiru Wang,Jiazhong Zhang,Hanna Cho,Shumeye Mamo,Ryan Bremer,Sam Gillette,Jun Kong,Nikolas K. Haass,Katrin Sproesser,Ling Li,Keiran S.M. Smalley,D. Fong,Yong-Liang Zhu,Adhirai Marimuthu,Hoa Nguyen,Billy Lam,Jennifer S. Liu,Ivana Cheung,Julie Rice,Yoshihisa Suzuki,Catherine Luu,Calvin Settachatgul,Rafe Shellooe,John Cantwell,Sung-Hou Kim,Joseph Schlessinger,Kam Y. J. Zhang,Brian L. West,Ben Powell,Gaston Habets,Chao Zhang,Prabha N. Ibrahim,Peter Hirth,Dean R. Artis,Meenhard Herlyn,Gideon Bollag +37 more
TL;DR: PLX4720, a 7-azaindole derivative that inhibits B-RafV600E with an IC50 of 13 nM, defines a class of kinase inhibitor with marked selectivity in both biochemical and cellular assays and represents the entire discovery process from initial identification through structural and biological studies in animal models to a promising therapeutic for testing in cancer patients bearing B- RafV 600E-driven tumors.
Journal ArticleDOI
Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
Graeme L. Card,B.P. England,Yoshihisa Suzuki,D. Fong,Ben Powell,Byunghun Lee,Catherine Luu,Maryam Tabrizizad,Sam Gillette,Prabha N. Ibrahim,Dean R. Artis,Gideon Bollag,Michael V. Milburn,Sung-Hou Kim,Joseph Schlessinger,Kam Y. J. Zhang +15 more
TL;DR: Structural insights will enable the design of isoform-selective inhibitors with improved binding affinity and should facilitate the discovery of more potent and selective PDE inhibitors for the treatment of a variety of diseases.
Journal ArticleDOI
A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Kam Y. J. Zhang,Graeme L. Card,Yoshihisa Suzuki,D. Richard Artis,D. Fong,Sam Gillette,Davin Hsieh,Joshua Neiman,Brian L. West,Chao Zhang,Michael V. Milburn,Sung-Hou Kim,Joseph Schlessinger,Gideon Bollag +13 more
TL;DR: In this paper, the authors describe the mechanism of nucleotide selectivity on the basis of high-resolution co-crystal structures of three types of PDEs: cAMP-specific, cGMP-specific and dual-specific.
Short Article A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Graeme L. Card,Yoshihisa Suzuki,D. Richard Artis,D. Fong,Sam Gillette,Davin Hsieh,Joshua Neiman,Brian L. West,Chao Zhang,Michael V. Milburn,Sung-Hou Kim,Joseph Schlessinger,Gideon Bollag +12 more
TL;DR: The structure of the PDE1B structure shows that in dual-specific PDEs a key histidine residue may enable the invariant glutamine to toggle between cAMP and cGMP, and the structural understanding of nucleotide binding enables the design of new PDE inhibitors that may treat diseases in which cyclic nucleotides play a critical role.
Journal ArticleDOI
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Graeme L. Card,Landy K. Blasdel,Landy K. Blasdel,B.P. England,Chao Zhang,Yoshihisa Suzuki,Sam Gillette,D. Fong,Prabha N. Ibrahim,Dean R. Artis,Gideon Bollag,Michael V. Milburn,Sung-Hou Kim,Joseph Schlessinger,Kam Y. J. Zhang +14 more
TL;DR: A family of potent PDE4 inhibitors discovered using an efficient method for scaffold-based drug design and the robustness of this approach for identifying new inhibitors that can be further developed into drug candidates is revealed.