G
Gaulin Jeffrey L
Researcher at Millennium Pharmaceuticals
Publications - 4
Citations - 1660
Gaulin Jeffrey L is an academic researcher from Millennium Pharmaceuticals. The author has contributed to research in topics: Ubiquitin-activating enzyme & SUMO protein. The author has an hindex of 4, co-authored 4 publications receiving 1403 citations.
Papers
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Journal ArticleDOI
An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer
Teresa A. Soucy,Peter G. Smith,Michael Milhollen,Allison Berger,James M. Gavin,Sharmila Adhikari,James E. Brownell,Kristin E. Burke,Cardin David P,Stephen Critchley,Courtney Cullis,Amanda Doucette,James J. Garnsey,Gaulin Jeffrey L,Rachel E. Gershman,Anna R. Lublinsky,Alice McDonald,Hirotake Mizutani,Usha Narayanan,Edward J. Olhava,Stephane Peluso,Mansoureh Rezaei,Michael D. Sintchak,Tina Talreja,Michael P. Thomas,Tary Traore,Stepan Vyskocil,Jie Yu,Julie Zhang,Lawrence R. Dick,Christopher F. Claiborne,Mark Rolfe,Joseph B. Bolen,Steven P. Langston +33 more
TL;DR: MLN4924 disrupts cullin-RING ligase-mediated protein turnover leading to apoptotic death in human tumour cells by a new mechanism of action, the deregulation of S-phase DNA synthesis, suggesting that NAE inhibitors may hold promise for the treatment of cancer.
Journal ArticleDOI
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer
Steven P. Langston,Stephen Grossman,Dylan Bradley England,Roushan Afroze,Neil Bence,Douglas Bowman,Nancy Bump,Ryan Chau,Bei-Ching Chuang,Christopher F. Claiborne,Larry Cohen,Kelly Connolly,Matthew O. Duffey,Nitya Durvasula,Scott Freeze,Melissa Gallery,Katherine M. Galvin,Gaulin Jeffrey L,Rachel E. Gershman,Paul D. Greenspan,Jessica Grieves,Jianping Guo,Nanda Gulavita,Shumet A. Hailu,Xingyue He,Kara Hoar,Yongbo Hu,Zhigen Hu,Mitsuhiro Ito,Mi-Sook Kim,Scott Weston Lane,David Lok,Anya Lublinsky,William D. Mallender,Mcintyre Charles,James J. Minissale,Hirotake Mizutani,Miho Mizutani,Nina Molchinova,Koji Ono,A D Patil,Mark G. Qian,Jessica Riceberg,Vaishali Shindi,Michael D. Sintchak,Keli Song,Teresa A. Soucy,Yana Wang,He Xu,Xiaofeng Yang,Agatha Zawadzka,Ji Zhang,Sai M. Pulukuri +52 more
TL;DR: TAK-981 as mentioned in this paper is a mechanism-based inhibitor of SAE which forms a SUMO-TAK-98 1 adduct as the inhibitory species within the enzyme catalytic site.
Patent
Thiophene or thiazole derivatives and their use as pi3k inhibitors
Cardin David P,Gaulin Jeffrey L,Paul D. Greenspan,Stephen Vyskocil,Xu Tianlin,Christelle C. Renou +5 more
TL;DR: In this article, the authors provided compounds of formula (I) wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification.
Patent
Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
Roushan Afroze,Indu T. Bharathan,Jeffrey Ciavarri,Paul E. Fleming,Gaulin Jeffrey L,Mario Girard,Steven P. Langston,Francois Soucy,Tzu-Tshin Wong,Yingchun Ye +9 more
TL;DR: In this paper, chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is the number of amino acid residues in a molecule, and W, Z, X Y, R Y1, R Y2 and R Y3 are defined.