Target

Ligand

Substrate

Meas. Tech.

In Vitro FTase Inhibition Assay

pH

7.5±n/a

Temperature

303.15±n/a K

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 Chem 45:2388-409 (2002) [PubMed]  Article Copy BDB DOI

More Info.:

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Name:

Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha

Synonyms:

Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase

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.

Name:

Protein farnesyltransferase subunit beta

Synonyms:

CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FNTB | FNTB_HUMAN | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Ras proteins prenyltransferase subunit beta | Type I protein geranyl-geranyltransferase subunit alpha

Type:

Enzyme Subunit

Mol. Mass.:

48766.02

Organism:

Homo sapiens (Human)

Description:

Protein farnesyltransferase subunit beta

Residue:

437

Sequence:

MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD

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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:

MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ

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Name:

BDBM14008

Synonyms:

(11R)-32-oxo-25-oxa-8,12,16,18-tetraazahexacyclo[24.3.1.1^{8,11}.1^{20,24}.0^{2,7}.0^{14,18}]dotriaconta-1(30),2,4,6,14,16,20(31),21,23,26,28-undecaene-23-carbonitrile | (23R)-22,23,24,25-Tetrahydro-22-oxo-16H,21H-21,23-ethano-6,10:12,16-dimethenobenz[g]-imidazo[4,3-n][1,9,12,15]oxatriazacycloheneicosine-9-carbonitrile | CHEMBL524862 | Macrocyclic 3-Aminopyrrolidinone analog 42

Type:

Small organic molecule

Emp. Form.:

C28H23N5O2

Mol. Mass.:

461.5145

SMILES:

O=C1[C@H]2CCN1c1ccccc1-c1cccc(Oc3cc(Cn4cncc4CN2)ccc3C#N)c1 |r|

Structure:

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Similarity to this molecule at least:

Name:

K-Ras C-terminus

Synonyms:

K-Ras C-terminus containing PDCVIM

Type:

Other Protein Type

Mol. Mass.:

358.43

Organism:

n/a

Description:

[3H]farnesyl diphosphate (10-500 nM) as co-substrate.

Residue:

3

Sequence:

NA