L
Lionel Rouge
Researcher at Genentech
Publications - 35
Citations - 2030
Lionel Rouge is an academic researcher from Genentech. The author has contributed to research in topics: Deubiquitinating enzyme & Kinase. The author has an hindex of 19, co-authored 31 publications receiving 1556 citations.
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Journal ArticleDOI
A Therapeutic Antibody Targeting BACE1 Inhibits Amyloid-β Production in Vivo
Jasvinder K. Atwal,Yongmei Chen,Cecilia Chiu,Deborah L. Mortensen,William J. Meilandt,Yichin Liu,Christopher E. Heise,Kwame Hoyte,Wilman Luk,Yanmei Lu,Kun Peng,Ping Wu,Lionel Rouge,Yingnan Zhang,Robert A. Lazarus,Kimberly Scearce-Levie,Weiru Wang,Yan Wu,Marc Tessier-Lavigne,Ryan J. Watts +19 more
TL;DR: This elegant pair of papers demonstrates the therapeutic potential of an anti-BACE1 antibody for treating Alzheimer’s disease but also provides a strategy worthy of the ancient Greeks that could be applied to other therapeutic antibodies that require safe passage into the human brain.
Journal ArticleDOI
USP7 small-molecule inhibitors interfere with ubiquitin binding
Lorna Kategaya,Paola Di Lello,Lionel Rouge,Richard Pastor,Kevin R Clark,Jason Drummond,Tracy Kleinheinz,Eva Lin,John-Paul Upton,Sumit Prakash,Johanna Heideker,Mark McCleland,Maria Stella Ritorto,Dario R. Alessi,Matthias Trost,Travis W. Bainbridge,Michael C. M. Kwok,Taylur P. Ma,Zachary Stiffler,Bradley B. Brasher,Yinyan Tang,Priyadarshini Jaishankar,Brian R. Hearn,Adam R. Renslo,Michelle R. Arkin,Frederick Cohen,Kebing Yu,Frank Peale,Florian Gnad,Matthew T. Chang,Christiaan Klijn,Elizabeth Blackwood,Scott E. Martin,William F. Forrest,James A. Ernst,Chudi Ndubaku,Xiaojing Wang,Maureen Beresini,Vickie Tsui,Carsten Schwerdtfeger,Robert A. Blake,Jeremy Murray,Till Maurer,Ingrid E. Wertz +43 more
TL;DR: Engineering compounds that inhibit USP7 activity by attenuating ubiquitin binding suggests opportunities for developing other deubiquitinase inhibitors and may be a strategy more broadly applicable to inhibiting proteins that require ubiquit in binding for full functional activity.
Journal ArticleDOI
Optimized arylomycins are a new class of Gram-negative antibiotics.
Peter A. S. Smith,Michael F. T. Koehler,Hany S. Girgis,Donghong Yan,Yongsheng Chen,Yuan Chen,James J. Crawford,Matthew R. Durk,Robert I. Higuchi,Jing Kang,Jeremy Murray,Prasuna Paraselli,Summer Park,Wilson Phung,John G. Quinn,Tucker C. Roberts,Lionel Rouge,Jacob Schwarz,Elizabeth Skippington,John S. Wai,Min Xu,Zhiyong Yu,Hua Zhang,Man-Wah Tan,Christopher E. Heise +24 more
TL;DR: Chemical optimization of arylomycins results in an inhibitor of bacterial type I signal peptidase that shows activity both against multidrug-resistant clinical isolates of Gram-negative bacteria in vitro and in several in vivo infection models.
Journal ArticleDOI
Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer
Daniel P. Sutherlin,Linda Bao,Megan Berry,Georgette Castanedo,Irina Chuckowree,Jenna Dotson,Adrian Folks,Lori Friedman,Richard Goldsmith,Janet L. Gunzner,Timothy P. Heffron,John Lesnick,Cristina Lewis,Simon Mathieu,Jeremy Murray,Jim Nonomiya,Jodie Pang,Niel Pegg,Wei Wei Prior,Lionel Rouge,Laurent Salphati,Deepak Sampath,Qingping Tian,Vickie Tsui,Nan Chi Wan,Shumei Wang,Binqing Wei,Christian Wiesmann,Ping Wu,Bing-Yan Zhu,Alan G. Olivero +30 more
TL;DR: The discovery of 2 (GDC-0980), a class I PI3K and mTOR kinase inhibitor for oncology indications, has demonstrated significant efficacy in mouse xenografts when dosed as low as 1 mg/kg orally and is currently in phase I clinical trials for cancer.
Journal ArticleDOI
Structure of TIGIT immunoreceptor bound to poliovirus receptor reveals a cell–cell adhesion and signaling mechanism that requires cis-trans receptor clustering
Katharina F. Stengel,Kristin Harden-Bowles,Xin Yu,Lionel Rouge,Jianping Yin,Laetitia Comps-Agrar,Christian Wiesmann,J. Fernando Bazan,Dan L. Eaton,Jane L. Grogan +9 more
TL;DR: The crystal structure of poliovirus receptor (PVR)/Nectin-like-5/CD155) in complex with its cognate immunoreceptor ligand T-cell-Ig- and-ITIM-domain (TIGIT) is reported and the TIGIT/PVR interface reveals a conserved specific “lock-and-key” interaction.