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TargetGeranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT)
LigandBDBM50134315
Substrate/Competitorn/a
Meas. Tech.ChEMBL_71960
IC50 17000±n/a nM
Citation Vigushin DMBrooke GWillows DCoombes RCMoody CJ Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I. Bioorg Med Chem Lett 13:3661-3 (2003) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT)
Name:Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT)
Synonyms:Geranylgeranyl transferase type I | Geranylgeranyl transferase type I beta/Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of EBI is 70196
Components:This complex has 2 components.
Component 1
Name:Geranylgeranyl transferase type I
Synonyms:CAAX farnesyltransferase alpha subunit | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | 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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Component 2
Name:Geranylgeranyl transferase type I
Synonyms:GGTase-I-beta | Geranylgeranyl transferase type I beta subunit | Geranylgeranyl transferase type I subunit beta | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | Protein farnesyl/geranylgeranyl transferase | Type I protein geranyl-geranyltransferase subunit beta
Type:n/a
Mol. Mass.:42369.84
Organism:Homo sapiens (Human)
Description:n/a
Residue:377
Sequence:
MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
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BDBM50134315
n/a
NameBDBM50134315
Synonyms:7-hydroxy-11-hydroxymethyl-12-methyl-14,15-dithia-9,12-diazatetracyclo[9.2.2.01,9.03,8]pentadeca-3,5-diene-10,13-dione | CHEMBL331627 | GLIOTOXIN
TypeSmall organic molecule
Emp. Form.C13H14N2O4S2
Mol. Mass.326.391
SMILESCN1C(=O)[C@]23CC4=CC=C[C@H](O)[C@H]4N2C(=O)[C@@]1(CO)SS3 |r,c:8,t:6,THB:12:13:1.2:19.20,15:14:1.2:19.20|
Structure
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