Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity

Biochemistry

Volumn 43, Issue 22, 2004, Pages 6877-6884

  Reid, T Scott ^a   Beese, Lorena S ^a  

^a DUKE UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CRYSTAL STRUCTURE; DRUG PRODUCTS; ENZYMES; LIPIDS; TUMORS;

MALIGNANCIES; MOLECULAR MECHANISMS;

BIOCHEMISTRY;

3 BENZYL 7 CYANO 2,3,4,5 TETRAHYDRO 1 (1H IMIDAZOL 4 YLMETHYL) 4 (2 THIENYLSULFONYL) 1H 1,4 BENZODIAZEPINE; ANTINEOPLASTIC AGENT; ANTIPARASITIC AGENT; PROTEIN FARNESYLTRANSFERASE; PROTEIN FARNESYLTRANSFERASE INHIBITOR; TIPIFARNIB;

AMEBIASIS; ARTICLE; BINDING SITE; BREAST CANCER; CHAGAS DISEASE; CRYSTAL STRUCTURE; DRUG SELECTIVITY; DRUG STRUCTURE; DYSENTERY; ENTAMOEBA HISTOLYTICA; ENZYME INHIBITION; HEMATOPOIETIC SYSTEM TUMOR; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; MALARIA; NONHUMAN; PARASITOSIS; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; STRUCTURE ANALYSIS; TRYPANOSOMA; TRYPANOSOMIASIS;

ALKYL AND ARYL TRANSFERASES; ANIMALS; BENZODIAZEPINES; CRYSTALLIZATION; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; HUMANS; IMIDAZOLES; QUINOLONES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

ENTAMOEBA; ENTAMOEBA HISTOLYTICA; MAMMALIA; PLASMODIUM FALCIPARUM; TRYPANOSOMA;

EID: 2642568535     PISSN: 00062960     EISSN: None     Source Type: Journal    
DOI: 10.1021/bi049723b     Document Type: Article

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