Target Information

Target General Infomation
Target ID
T86428
Former ID
TTDR01076
Target Name
Protein farnesyltransferase beta subunit
Gene Name
FNTB
Synonyms
CAAX farnesyltransferase beta subunit; FTase-beta; RAS proteins prenyltransferasebeta; FNTB
Target Type
Discontinued
Disease Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Non-small cell lung cancer [ICD10: C33-C34]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Essential subunit of the farnesyltransferase complex. Catalyzes the transfer of a farnesyl moiety from farnesyl diphosphate to a cysteine at the fourth position from the C- terminus of several proteins having the C-terminal sequence Cys- aliphatic-aliphatic-X.
BioChemical Class
Alkyl aryl transferase
Target Validation
T86428
UniProt ID
P49356
EC Number
EC 2.5.1.58
Sequence
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV
PGFEELKDETSAEPATD
Structure
1JCQ; 1LD7; 1LD8; 1MZC; 1S63; 1SA4; 1TN6; 2F0Y; 2H6F; 2H6G; 2H6H; 2H6I; 2IEJ; 3E37
Drugs and Mode of Action
Drug(s) ABT-100 Drug Info Terminated Solid tumours [1]
ABT-839 Drug Info Terminated Non-small cell lung cancer [2]
B-956 Drug Info Terminated Cancer [3]
BMS-182566 Drug Info Terminated Cancer [4]
BMS-185857 Drug Info Terminated Cancer [5]
CP-663427 Drug Info Terminated Cancer [6]
FUSIDIENOL Drug Info Terminated Discovery agent [7]
L-731735 Drug Info Terminated Cancer [8]
L-739749 Drug Info Terminated Cancer [9]
L-745631 Drug Info Terminated Cancer [10]
MANUMYCIN A Drug Info Terminated Discovery agent [11]
RPR-113829 Drug Info Terminated Discovery agent [12]
RPR-114334 Drug Info Terminated Discovery agent [13]
Sch-207758 Drug Info Terminated Cancer [14]
SCH-44342 Drug Info Terminated Discovery agent [15]
XR-3005 Drug Info Terminated Colorectal cancer [16]
XR-3054 Drug Info Terminated Cancer [17]
Inhibitor (Z)-2-Methyl-3-tetradecyl-but-2-enedioic acid Drug Info [18]
A-313326 Drug Info [19]
ABT-100 Drug Info [20]
ABT-839 Drug Info [19]
ACTINOPLANIC ACID A Drug Info [18]
ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID Drug Info [21]
ARTEMINOLIDE Drug Info [22]
BMS-316810 Drug Info [23]
BMS-404683 Drug Info [24]
CLAVARINONE Drug Info [25]
CP-663427 Drug Info [26]
CYLINDROL A Drug Info [18]
F-12458 Drug Info [27]
FARNESYL Drug Info [21]
FTI 276 Drug Info [28]
FUSIDIENOL Drug Info [22]
GERANYLGERANYL DIPHOSPHATE Drug Info [21]
H-SMGLPCVVM-OH Drug Info [29]
L-731735 Drug Info [18]
L-739749 Drug Info [18]
L-739750 Drug Info [18]
L-745631 Drug Info [18]
LB42908 Drug Info [30]
MANUMYCIN A Drug Info [31]
PB-27 Drug Info [24]
PB-80 Drug Info [24]
PB-81 Drug Info [24]
PD-83176 Drug Info [32]
Prenyl pyrophosphate analogue Drug Info [33]
PREUSSOMERIN Drug Info [18]
Pseudopeptide derivative Drug Info [34]
RPR-113829 Drug Info [35]
RPR-114334 Drug Info [35]
Sch-207758 Drug Info [36]
SCH-44342 Drug Info [18]
XR-3054 Drug Info [17]
Modulator B-956 Drug Info [3]
BMS-182566 Drug Info [37]
BMS-185857 Drug Info [37]
XR-3005 Drug Info [37]
Pathways
KEGG Pathway Terpenoid backbone biosynthesis
Biosynthesis of antibiotics
NetPath Pathway TSH Signaling Pathway
Reactome Inactivation, recovery and regulation of the phototransduction cascade
WikiPathways Visual phototransduction
References
REF 1Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019239)
REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014561)
REF 3Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956. Cancer Res. 1995 Nov 15;55(22):5310-4.
REF 4Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004903)
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004901)
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013446)
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004994)
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002714)
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004259)
REF 10Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007537)
REF 11Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006417)
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008741)
REF 13Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008739)
REF 14Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012642)
REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007534)
REF 16Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005580)
REF 17XR3054, structurally related to limonene, is a novel inhibitor of farnesyl protein transferase. Eur J Cancer. 1999 Jun;35(6):1014-9.
REF 18J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
REF 19Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
REF 20Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection. J Heart Lung Transplant. 2005 Sep;24(9):1403-9.
REF 21The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 22J Med Chem. 2002 Mar 28;45(7):1460-5.Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking.
REF 23Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9.Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
REF 24J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
REF 25J Med Chem. 1998 Nov 5;41(23):4492-501.Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.
REF 26WO patent application no. 2011,0881,26, Treatment of viral infection with prenyltransferase inhibitors.
REF 27Recent progress in protein farnesyltransferase inhibition. IDrugs. 2000 Nov;3(11):1336-45.
REF 28Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. J Biol Chem. 1995 Nov 10;270(45):26802-6.
REF 29Bioorg Med Chem Lett. 2003 Aug 4;13(15):2583-6.Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide.
REF 30A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase). Bioorg Med Chem Lett. 2001 Dec 3;11(23):3069-72.
REF 31Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.A novel metal-chelating inhibitor of protein farnesyltransferase.
REF 32J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase.
REF 33Synthesis and evaluation of benzophenone-based photoaffinity labeling analogs of prenyl pyrophosphates containing stable amide linkages, Bioorg. Med. Chem. Lett. 7(16):2125-2130 (1997).
REF 34Local constrained shifty pseudopeptides inhibitors of rasfarnesyl transferase, Bioorg. Med. Chem. Lett. 5(22):2677-2682 (1995).
REF 35J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase.
REF 36Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase. J Med Chem. 2002 Aug 29;45(18):3854-64.
REF 37US patent application no. 2005,0227,929, Combination therapy comprising a cox-2 inhibitor and an antineoplastic agent.

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