Distinct ETAreceptor binding mode of macitentan as determined by site directed mutagenesis

PLoS ONE

Volumn 9, Issue 9, 2014, Pages

  Gatfield, John ^a   Grandjean, Celia Mueller ^a   Bur, Daniel ^a   Bolli, Martin H ^a   Nayler, Oliver ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

AMBRISENTAN; BOSENTAN; ENDOTHELIN; ENDOTHELIN RECEPTOR; ENDOTHELIN RECEPTOR A; MACITENTAN; MUTANT PROTEIN; UNCLASSIFIED DRUG; ENDOTHELIN RECEPTOR ANTAGONIST; PROTEIN BINDING; PYRIMIDINE DERIVATIVE; SULFONAMIDE;

AQUEOUS SOLUTION; ARTICLE; BINDING KINETICS; BINDING SITE; CHEMICAL REACTION KINETICS; CONFORMATION; DISSOCIATION; DRUG ACTIVITY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; HUMAN; HUMAN CELL; HYDROPHOBICITY; MOLECULAR MODEL; POINT MUTATION; PROTON NUCLEAR MAGNETIC RESONANCE; SITE DIRECTED MUTAGENESIS; CELL LINE; CHEMICAL STRUCTURE; CHEMISTRY; ENZYME ACTIVE SITE; GENETICS; IC50; KINETICS; METABOLISM; MUTATION; PROTEIN CONFORMATION;

BINDING SITES; CATALYTIC DOMAIN; CELL LINE; ENDOTHELIN RECEPTOR ANTAGONISTS; HUMANS; INHIBITORY CONCENTRATION 50; KINETICS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MUTAGENESIS, SITE-DIRECTED; MUTATION; PROTEIN BINDING; PROTEIN CONFORMATION; PYRIMIDINES; RECEPTORS, ENDOTHELIN; SULFONAMIDES;

EID: 84907151744     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0107809     Document Type: Article

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