Brand  (β version)

PDB ID: 1SA4

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Ligands
Code Name Style Show Link
FPP Farnesyl diphosphate PoSSuM
JAN 6-[(S)-amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1h)-one PoSSuM
ZN Zinc ion PoSSuM
FRU Beta-D-fructofuranose PoSSuM
GLC Alpha-D-glucopyranose PoSSuM
: Polysaccharide
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Structure summary

Code : 1SA4   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : human protein farnesyltransferase complexed with FPP and R115777
Release Data : 2004-06-08
Compound :
mol_id molecule chains synonym
1 Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit A CAAX farnesyltransferase alpha subunit, Ras proteins prenyltransferase alpha, FTase-alpha, Type I protein geranyl-geranyltransferase alpha subunit, GGTase-I-alpha
ec: 2.5.1.58, 2.5.1.59
mol_id molecule chains synonym
2 Protein farnesyltransferase beta subunit B CAAX farnesyltransferase beta subunit, RAS proteins prenyltransferase beta, FTase-beta
ec: 2.5.1.58
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: FNTA
mol_id organism_scientific organism_common expression_system
2 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: FNTB
Authors : Reid, T.S., Beese, L.S.
Keywords : FTASE, FARNESYLTRANSFERASE, FARNESYL TRANSFERASE, CAAX, RAS, CANCER, TUMOR REGRESSION, R115777, TIPIFARNIB, ZARNESTRA, FTI, CLINICAL CANDIDATE, INHIBITOR, PROTEIN PRENYLATION, LIPID MODIFICATION, TRANSFERASE
Exp. method : X-RAY DIFFRACTION ( 2.10 Å )
Citation :

Crystal Structures of the Anticancer Clinical Candidates R115777 (Tipifarnib) and BMS-214662 Complexed with Protein Farnesyltransferase Suggest a Mechanism of FTI Selectivity.

Reid, T.S.,Beese, L.S.
(2004)  Biochemistry  43 : 6877 - 6884

PubMed: 15170324
DOI: 10.1021/bi049723b

Reaction

Chain : A
UniProt : P49354 (FNTA_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
(2E,6E)-farnesyl diphosphate + L-cysteinyl-[protein] = diphosphate + S-(2E,6E)-farnesyl-L-cysteinyl-[protein] 2.5.1.58 PubMed:12036349, PubMed:12825937, PubMed:16893176, PubMed:19246009, PubMed:8419339, PubMed:8494894
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geranylgeranyl diphosphate + L-cysteinyl-[protein] = diphosphate + S-geranylgeranyl-L-cysteinyl-[protein] 2.5.1.59 PubMed:16893176
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Chain : B
UniProt : P49356 (FNTB_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
(2E,6E)-farnesyl diphosphate + L-cysteinyl-[protein] = diphosphate + S-(2E,6E)-farnesyl-L-cysteinyl-[protein] 2.5.1.58 PubMed:12036349, PubMed:12825937, PubMed:16893176, PubMed:19246009, PubMed:8494894
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