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Ligands
Code Name Style Show Link
336 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-B]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide
FPP Farnesyl diphosphate
ZN Zinc ion
Non-standard Residues
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Glycosylation
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Code : 1O5M   PDBj   RCSB PDB   PDBe
Header : transferase/transferase inhibitor
Title : Structure of FPT bound to the inhibitor SCH66336
Release Data : 2003-10-21
Compound :
mol_id molecule chains synonym
1 Protein farnesyltransferase alpha subunit A CAAX farnesyltransferase alpha subunit, RAS proteins prenyltransferase alpha, FTase-alpha
ec: 2.5.1.-
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.-
Source :
mol_id organism_scientific organism_common expression_system
1 Rattus norvegicus  (taxid:10116) Norway rat Escherichia coli  (taxid:562)
gene: FNTA
mol_id organism_scientific organism_common expression_system
2 Rattus norvegicus  (taxid:10116) Norway rat Escherichia coli  (taxid:562)
gene: FNTB
Authors : Strickland, C.L., Weber, P.C., Ganguly, A.K.
Keywords : Protein Inhibitor Complex, transferase-transferase inhibitor COMPLEX
Exp. method : X-RAY DIFFRACTION ( 2.3 Å )
Citation :

Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure-Activity Relationships

Strickland, C.L.,Weber, P.C.,Windsor, W.T.  et al.
(1999)  J.Med.Chem.  42 : 2125 - 2135

PubMed: 10377218
DOI: 10.1021/jm990030g

Chain : A
UniProt : Q04631 (FNTA_RAT)
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:12657282, PubMed:18844669, PubMed:19219049, PubMed:22963166
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geranylgeranyl diphosphate + L-cysteinyl-[protein] = diphosphate + S-geranylgeranyl-L-cysteinyl-[protein] 2.5.1.59 PubMed:14609943, PubMed:19219049
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Chain : B
UniProt : Q02293 (FNTB_RAT)
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:10673434, PubMed:18844669, PubMed:19219049, PubMed:19246009, PubMed:22963166
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