Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist

Science

Volumn 350, Issue 6267, 2015, Pages

  Ahuja, Shivani ^a,c   Mukund, Susmith ^a   Deng, Lunbin ^a   Khakh, Kuldip ^b   Chang, Elaine ^b   Ho, Hoangdung ^a   Shriver, Stephanie ^a   Young, Clint ^b   Lin, Sophia ^b   Johnson, J P ^b   Wu, Ping ^a   Li, Jun ^a   Coons, Mary ^a,d   Tam, Christine ^a   Brillantes, Bobby ^a   Sampang, Honorio ^a   Mortara, Kyle ^a   Bowman, Krista K ^a   Clark, Kevin R ^a   Estevez, Alberto ^a   Xie, Zhiwei ^b   Verschoof, Henry ^b   Grimwood, Michael ^b   Dehnhardt, Christoph ^b   Andrez, Jean Christophe ^b   Focken, Thilo ^b   Sutherlin, Daniel P ^a   Safina, Brian S ^a   Starovasnik, Melissa A ^a   Ortwine, Daniel F ^a   Franke, Yvonne ^a   Cohen, Charles J ^b   Hackos, David H ^a   Koth, Christopher M ^a   Payandeh, Jian ^a   more..

^a GENENTECH INC   (United States)

^b Xenon Pharmaceuticals Inc   (Canada)

^c OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

^d Caribou Biosciences Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ARGININE; GX 936; PHOSPHOLIPID; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; SODIUM CHANNEL NAV1.7; SULFONAMIDE; UNCLASSIFIED DRUG; VOLTAGE GATED SODIUM CHANNEL BLOCKING AGENT; GX-936; ISOPROTEIN; SCN9A PROTEIN, HUMAN; SODIUM CHANNEL BLOCKING AGENT; THIADIAZOLE DERIVATIVE;

BIOENGINEERING; CRYSTAL STRUCTURE; INHIBITION; INHIBITOR; PROTEIN; SODIUM;

ACTION POTENTIAL; ARTICLE; COMPLEX FORMATION; CRYSTAL STRUCTURE; CRYSTALLIZATION; DRUG DESIGN; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG TARGETING; HUMAN; HUMAN CELL; NOCICEPTION; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN ENGINEERING; AMINO ACID SEQUENCE; ANTAGONISTS AND INHIBITORS; CELL MEMBRANE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; GENETICS; MOLECULAR GENETICS; NUCLEOTIDE SEQUENCE; PROCEDURES; PROTEIN SECONDARY STRUCTURE; PROTEIN TERTIARY STRUCTURE; X RAY CRYSTALLOGRAPHY;

MAMMALIA;

AMINO ACID SEQUENCE; CELL MEMBRANE; CRYSTALLIZATION; CRYSTALLOGRAPHY, X-RAY; DNA MUTATIONAL ANALYSIS; HUMANS; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; NAV1.7 VOLTAGE-GATED SODIUM CHANNEL; PAIN PERCEPTION; PROTEIN ENGINEERING; PROTEIN ISOFORMS; PROTEIN STRUCTURE, SECONDARY; PROTEIN STRUCTURE, TERTIARY; SODIUM CHANNEL BLOCKERS; SULFONAMIDES; THIADIAZOLES;

EID: 84950257999     PISSN: 00368075     EISSN: 10959203     Source Type: Journal    
DOI: 10.1126/science.aac5464     Document Type: Article

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