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TargetGeranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
LigandBDBM14001
Substrate/CompetitorBiotinylated Peptide Substrate
Meas. Tech.In Vitro FTase Inhibition Assay
IC50 1600±n/a nM
Citation Bell, IM; Gallicchio, SN; Abrams, M; Beese, LS; Beshore, DC; Bhimnathwala, H; Bogusky, MJ; Buser, CA; Culberson, JC; Davide, J; Ellis-Hutchings, M; Fernandes, C; Gibbs, JB; Graham, SL; Hamilton, KA; Hartman, GD; Heimbrook, DC; Homnick, CF; Huber, HE; Huff, JR; Kassahun, K; Koblan, KS; Kohl, NE; Lobell, RB; Lynch, JJ; Robinson, R; Rodrigues, AD; Taylor, JS; Walsh, ES; Williams, TM; Zartman, CB 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. J Med Chem45:2388-409 (2002) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Geranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Name:Geranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:Geranylgeranyl Transferase (GGTase-I)
Type:Protein Complex
Mol. Mass.:n/a
Description:To express recombinant enzyme in E. coli, the cloned human alpha and beta subunits were co-expressed from a plasmid, in which their expression was translationally coupled.
Components:This complex has 2 components.
Component 1
Name:Geranylgeranyl transferase type-1 subunit beta [A2V]
Synonyms:GGTase-I-beta | Geranylgeranyl Transferase (GGTase-I) Chain B | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_HUMAN
Type:Enzyme Subunit
Mol. Mass.:42397.89
Organism:Homo sapiens (Human)
Description:Geranylgeranyl transferase type-1 subunit beta.
Residue:377
Sequence:
MVATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
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Component 2
Name:Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:CAAX farnesyltransferase alpha subunit | FNTA | FNTA_HUMAN | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Geranylgeranyl transferase type I | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha
Type:Enzyme
Mol. Mass.:44392.46
Organism:Homo sapiens (Human)
Description:Recombinant human FTase.
Residue:379
Sequence:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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BDBM14001
Biotinylated Peptide Substrate
Name:Biotinylated Peptide Substrate
Synonyms:biotinylated peptide that represents the C-terminus of the K4B-Ras protein
Type:Peptide
Mol. Mass.:2461.17
Organism:n/a
Description:100 nM [3H]GGPP as co-substrate.
Residue:21
Sequence:
biotinyl-GKKKKKKSKTKCVIM