Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation

ACS Medicinal Chemistry Letters

Volumn 6, Issue 1, 2015, Pages 53-57

  Goodwin, Nicole C ^a,b   Cianchetta, Giovanni ^a   Burgoon, Hugh A ^a   Healy, Jason ^a   Mabon, Ross ^a   Strobel, Eric D ^a   Allen, Jason ^a   Wang, Shuli ^a   Hamman, Brian D ^a   Rawlins, David B ^a  

^a LEXICON PHARMACEUTICALS INC   (United States)

^b NONE   (United States)

Author keywords

allosteric; DFG out; LIM kinase 2; noncompetitive; selective; type III kinase inhibitor

Indexed keywords

ASPARTYLPHENYLALANYLGLYCINE; LIM KINASE 2 TYPE III INHIBITOR; PEPTIDE DERIVATIVE; PROTEIN KINASE INHIBITOR; SULFONAMIDE; UNCLASSIFIED DRUG; AMINO ACID; ASPARTYLPHENYLGLYCINE; LIM KINASE 2 INHIBITOR; PROTEIN SERINE THREONINE KINASE INHIBITOR;

ALKYLATION; ARTICLE; BINDING SITE; CONTROLLED STUDY; DRUG BINDING; DRUG CONFORMATION; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME KINETICS; HINGE REGION; HYDROGEN BOND; HYDROPHOBICITY; IC50; IN VITRO STUDY; PRIORITY JOURNAL; X RAY CRYSTALLOGRAPHY; ENZYME CONFORMATION;

EID: 84920747143     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml500242y     Document Type: Article

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