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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50073179
Substrate
n/a
Meas. Tech.
ChEBML_69830
IC50
>65000±n/a nM
Citation
 Cooper, AB; Strickland, CL; Wang, J; Desai, J; Kirschmeier, P; Patton, R; Bishop, WR; Weber, PC; Girijavallabhan, V Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase. Bioorg Med Chem Lett 12:601-5 (2002) [PubMed]  Article 
Target
Name:
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Farnesyltransferase (FTase) | Protein farnesyltransferase | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B
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:
Protein farnesyltransferase subunit beta
Synonyms:
Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase subunit beta | CAAX farnesyltransferase subunit beta | CAAX farnesyltransferase subunit alpha | Ras proteins prenyltransferase subunit alpha | Type I protein geranyl-geranyltransferase subunit alpha | FTase-beta | GGTase-I-alpha | Ras proteins prenyltransferase subunit beta | Protein farnesyltransferase beta subunit | FTase-alpha | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | FNTB_HUMAN | FNTB | Protein farnesyl/geranylgeranyl transferase
Type:
Enzyme Subunit
Mol. Mass.:
48766.02
Organism:
Human
Description:
Protein farnesyltransferase subunit beta
Residue:
437
Sequence:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD
  
Component 2
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Protein Farnesyltransferase (PFT) Chain A | GGTase-I-alpha | FTase-alpha | FTase-1-alpha | Protein farnesyltransferase | Ras proteins prenyltransferase alpha | CAAX farnesyltransferase alpha subunit | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Geranylgeranyl Transferase (GGTase-I) Chain A | FNTA_HUMAN | FNTA | Geranylgeranyl transferase type I | Protein farnesyl/geranylgeranyl transferase
Type:
Enzyme
Mol. Mass.:
44392.46
Organism:
Human
Description:
Recombinant human FTase.
Residue:
379
Sequence:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ
  
Inhibitor
Name:
BDBM50073179
Synonyms:
CHEMBL1172 | Clarinex | Claritin-D | Claritin | SCH-34117 | 8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine | DESLORATADINE | US9333199, DESLORATADINE (Clarinex) | US9138431, DESLORATADINE (Clarinex)
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity: