Brand  (β version)

PDB ID: 1LD7

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Ligands
Code Name Style Show Link
FPP Farnesyl diphosphate PoSSuM
U66 (20s)-19,20,22,23-tetrahydro-19-oxo-5h,21h-18,20-ethano-12,14-etheno-6,10-methenobenz[D]imidazo[4,3-L][1,6,9,13]oxatria zacyclonoadecosine-9-carbonitrile PoSSuM
ZN Zinc ion PoSSuM
FRU Beta-D-fructofuranose PoSSuM
GLC Alpha-D-glucopyranose PoSSuM
: Polysaccharide
Non-standard Residues
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Structure summary

Code : 1LD7   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : Co-crystal structure of Human Farnesyltransferase with farnesyldiphosphate and inhibitor compound 66
Release Data : 2002-06-19
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 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
mol_id organism_scientific organism_common expression_system
2 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
Authors : Taylor, J.S., Terry, K.L., Beese, L.S.
Keywords : alpha-alpha barrel, inhibitor, ftase, pftase, fpp, caax, ras, TRANSFERASE
Exp. method : X-RAY DIFFRACTION ( 2.00 Å )
Citation :

3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.

Bell, I.M.,Gallicchio, S.N.,Abrams, M.  et al.
(2002)  J.Med.Chem.  45 : 2388 - 2409

PubMed: 12036349
DOI: 10.1021/jm010531d

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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