Multiple conformers in active site of human dihydrofolate reductase F31R/Q35E double mutant suggest structural basis for methotrexate resistance

Journal of Biological Chemistry

Volumn 284, Issue 30, 2009, Pages 20079-20089

  Volpato, Jordan P ^a   Yachnin, Brahm J ^b   Blanchet, Jonathan ^a   Guerrero, Vanessa ^a   Poulin, Lucie ^a   Fossati, Elena ^a   Berghuis, Albert M ^b   Pelletier, Joelle N ^a  

^a UNIVERSITÉ DE MONTRÉAL   (Canada)

^b MCGILL UNIVERSITY   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVE SITE; AMINO ACID SUBSTITUTION; CATALYTIC ACTIVITY; DIHYDROFOLATE REDUCTASE; DOUBLE MUTANTS; DRUG RESISTANCE; LIGAND BINDING; MOLECULAR BASIS; MOLECULAR DOCKING; NATIVE ENZYMES; P-AMINOBENZOIC ACID; STRUCTURAL BASIS; SYNERGISTIC EFFECT; TIGHT BINDING; VAN DER WAALS; WILD-TYPE ENZYMES;

AMINES; AMINO ACIDS; BIOCHEMICAL ENGINEERING; BIOCHEMISTRY; ENZYMES; ORGANIC ACIDS; ORGANIC POLYMERS; VAN DER WAALS FORCES;

CRYSTAL STRUCTURE;

ARGININE; DIHYDROFOLATE REDUCTASE; METHOTREXATE;

AMINO ACID SUBSTITUTION; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING; ENZYME ACTIVE SITE; ENZYME CONFORMATION; ENZYME STRUCTURE; MOLECULAR MECHANICS; MUTANT; PRIORITY JOURNAL; WILD TYPE;

CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; DRUG RESISTANCE; ENZYME INHIBITORS; FOLIC ACID; HUMANS; METHOTREXATE; MODELS, MOLECULAR; POINT MUTATION; PROTEIN BINDING; PROTEIN CONFORMATION; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDROFOLATE DEHYDROGENASE;

EID: 67749106478     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M109.018010     Document Type: Article

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