Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists

Proceedings of the National Academy of Sciences of the United States of America

Volumn 115, Issue 47, 2018, Pages 12045-12050

  Liu, Hongtao ^a   Hofmann, Josefa ^b   Fish, Inbar ^c,d   Schaake, Benjamin ^b   Eitel, Katrin ^b   Bartuschat, Amelie ^b   Kaindl, Jonas ^b   Rampp, Hannelore ^b   Banerjee, Ashutosh ^b   Hübner, Harald ^b   Clark, Mary J ^e   Vincent, Sandra G ^f   Fisher, John T ^f   Heinrich, Markus R ^b   Hirata, Kunio ^g   Liu, Xiangyu ^a   Sunahara, Roger K ^e   Shoichet, Brian K ^c   Kobilka, Brian K ^a,h   Gmeiner, Peter ^b  

^a Tsinghua University   (China)

^b UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d TEL AVIV UNIVERSITY   (Israel)

^e UNIVERSITY OF CALIFORNIA   (United States)

^f QUEEN S UNIVERSITY   (Canada)

^g RIKEN/SPring 8 Center ^*  (Japan)

^h STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Crystal structure; Drug design; G protein coupled receptor; Muscarinic receptor; Subtype selectivity

Indexed keywords

CHOLINERGIC RECEPTOR BLOCKING AGENT; ACETYLCHOLINE; CHRM3 PROTEIN, HUMAN; MUSCARINIC M2 RECEPTOR; MUSCARINIC M3 RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; DRUG BINDING; DRUG DETERMINATION; DRUG EFFECT; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; IN VIVO STUDY; MOLECULAR DOCKING; MOUSE; NONHUMAN; PREDICTION; PRIORITY JOURNAL; AMINO ACID SEQUENCE; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DESIGN; GENETICS; HUMAN; METABOLISM; PROCEDURES; X RAY CRYSTALLOGRAPHY;

ACETYLCHOLINE; AMINO ACID SEQUENCE; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; MOLECULAR DOCKING SIMULATION; MUSCARINIC ANTAGONISTS; RECEPTOR, MUSCARINIC M2; RECEPTOR, MUSCARINIC M3;

EID: 85056801761     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1813988115     Document Type: Article

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