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Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist.
Ahuja, Shivani; Mukund, Susmith; Deng, Lunbin; Khakh, Kuldip; Chang, Elaine; Ho, Hoangdung; Shriver, Stephanie; Young, Clint; Lin, Sophia; Johnson, J P; Wu, Ping; Li, Jun; Coons, Mary; Tam, Christine; Brillantes, Bobby; Sampang, Honorio; Mortara, Kyle; Bowman, Krista K; Clark, Kevin R; Estevez, Alberto; Xie, Zhiwei; Verschoof, Henry; Grimwood, Michael; Dehnhardt, Christoph; Andrez, Jean-Christophe; Focken, Thilo; Sutherlin, Daniel P; Safina, Brian S; Starovasnik, Melissa A; Ortwine, Daniel F; Franke, Yvonne; Cohen, Charles J; Hackos, David H; Koth, Christopher M; Payandeh, Jian.
Affiliation
  • Ahuja S; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Mukund S; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Deng L; Department of Neuroscience, Genentech Inc., South San Francisco, CA 94080, USA.
  • Khakh K; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Chang E; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Ho H; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Shriver S; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Young C; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Lin S; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Johnson JP; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Wu P; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Li J; Department of Discovery Chemistry, Genentech Inc., South San Francisco, CA 94080, USA.
  • Coons M; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Tam C; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Brillantes B; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Sampang H; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Mortara K; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Bowman KK; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Clark KR; Department of Biochemical and Cellular Pharmacology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Estevez A; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Xie Z; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Verschoof H; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Grimwood M; Department of Chemistry, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Dehnhardt C; Department of Chemistry, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Andrez JC; Department of Chemistry, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Focken T; Department of Chemistry, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Sutherlin DP; Department of Discovery Chemistry, Genentech Inc., South San Francisco, CA 94080, USA.
  • Safina BS; Department of Discovery Chemistry, Genentech Inc., South San Francisco, CA 94080, USA.
  • Starovasnik MA; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Ortwine DF; Department of Discovery Chemistry, Genentech Inc., South San Francisco, CA 94080, USA.
  • Franke Y; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA.
  • Cohen CJ; Department of Biology, Xenon Pharmaceuticals Inc., Burnaby, British Columbia, V5G 4W8, Canada.
  • Hackos DH; Department of Neuroscience, Genentech Inc., South San Francisco, CA 94080, USA. hackos.david@gene.com koth.christopher@gene.com payandeh.jian@gene.com.
  • Koth CM; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA. hackos.david@gene.com koth.christopher@gene.com payandeh.jian@gene.com.
  • Payandeh J; Department of Structural Biology, Genentech Inc., South San Francisco, CA 94080, USA. hackos.david@gene.com koth.christopher@gene.com payandeh.jian@gene.com.
Science ; 350(6267): aac5464, 2015 Dec 18.
Article in En | MEDLINE | ID: mdl-26680203
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Thiadiazoles / Sodium Channel Blockers / NAV1.7 Voltage-Gated Sodium Channel Limits: Humans Language: En Journal: Science Year: 2015 Document type: Article Affiliation country: United States Country of publication: United States
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Thiadiazoles / Sodium Channel Blockers / NAV1.7 Voltage-Gated Sodium Channel Limits: Humans Language: En Journal: Science Year: 2015 Document type: Article Affiliation country: United States Country of publication: United States