Target Information
Target General Infomation | |||||
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Target ID |
T86428
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Former ID |
TTDR01076
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Target Name |
Protein farnesyltransferase beta subunit
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Gene Name |
FNTB
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Synonyms |
CAAX farnesyltransferase beta subunit; FTase-beta; RAS proteins prenyltransferasebeta; FNTB
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Target Type |
Discontinued
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Disease | Cancer [ICD9: 140-229; ICD10: C00-C96] | ||||
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
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.
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BioChemical Class |
Alkyl aryl transferase
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Target Validation |
T86428
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UniProt ID | |||||
EC Number |
EC 2.5.1.58
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Sequence |
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV PGFEELKDETSAEPATD |
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Structure |
1JCQ; 1LD7; 1LD8; 1MZC; 1S63; 1SA4; 1TN6; 2F0Y; 2H6F; 2H6G; 2H6H; 2H6I; 2IEJ; 3E37
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Drugs and Mode of Action | |||||
Drug(s) | ABT-100 | Drug Info | Terminated | Solid tumours | [547784] |
ABT-839 | Drug Info | Terminated | Non-small cell lung cancer | [547261] | |
B-956 | Drug Info | Terminated | Cancer | [533645] | |
BMS-182566 | Drug Info | Terminated | Cancer | [545819] | |
BMS-185857 | Drug Info | Terminated | Cancer | [545818] | |
CP-663427 | Drug Info | Terminated | Cancer | [547153] | |
FUSIDIENOL | Drug Info | Terminated | Discovery agent | [545839] | |
L-731735 | Drug Info | Terminated | Cancer | [545288] | |
L-739749 | Drug Info | Terminated | Cancer | [545701] | |
L-745631 | Drug Info | Terminated | Cancer | [546335] | |
MANUMYCIN A | Drug Info | Terminated | Discovery agent | [546113] | |
RPR-113829 | Drug Info | Terminated | Discovery agent | [546523] | |
RPR-114334 | Drug Info | Terminated | Discovery agent | [546522] | |
Sch-207758 | Drug Info | Terminated | Cancer | [547062] | |
SCH-44342 | Drug Info | Terminated | Discovery agent | [546334] | |
XR-3005 | Drug Info | Terminated | Colorectal cancer | [545970] | |
XR-3054 | Drug Info | Terminated | Cancer | [525621] | |
Inhibitor | (Z)-2-Methyl-3-tetradecyl-but-2-enedioic acid | Drug Info | [534466] | ||
A-313326 | Drug Info | [527321] | |||
ABT-100 | Drug Info | [527723] | |||
ABT-839 | Drug Info | [527321] | |||
ACTINOPLANIC ACID A | Drug Info | [534466] | |||
ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID | Drug Info | [551374] | |||
ARTEMINOLIDE | Drug Info | [526296] | |||
BMS-316810 | Drug Info | [527491] | |||
BMS-404683 | Drug Info | [527568] | |||
CLAVARINONE | Drug Info | [534739] | |||
CP-663427 | Drug Info | [550155] | |||
CYLINDROL A | Drug Info | [534466] | |||
F-12458 | Drug Info | [527662] | |||
FARNESYL | Drug Info | [551374] | |||
FTI 276 | Drug Info | [533648] | |||
FUSIDIENOL | Drug Info | [526296] | |||
GERANYLGERANYL DIPHOSPHATE | Drug Info | [551374] | |||
H-SMGLPCVVM-OH | Drug Info | [526670] | |||
L-731735 | Drug Info | [534466] | |||
L-739749 | Drug Info | [534466] | |||
L-739750 | Drug Info | [534466] | |||
L-745631 | Drug Info | [534466] | |||
LB42908 | Drug Info | [526198] | |||
MANUMYCIN A | Drug Info | [526603] | |||
PB-27 | Drug Info | [527568] | |||
PB-80 | Drug Info | [527568] | |||
PB-81 | Drug Info | [527568] | |||
PD-83176 | Drug Info | [534307] | |||
Prenyl pyrophosphate analogue | Drug Info | [551324] | |||
PREUSSOMERIN | Drug Info | [534466] | |||
Pseudopeptide derivative | Drug Info | [551289] | |||
RPR-113829 | Drug Info | [534405] | |||
RPR-114334 | Drug Info | [534405] | |||
Sch-207758 | Drug Info | [526408] | |||
SCH-44342 | Drug Info | [534466] | |||
XR-3054 | Drug Info | [525621] | |||
Modulator | B-956 | Drug Info | [533645] | ||
BMS-182566 | Drug Info | [550890] | |||
BMS-185857 | Drug Info | [550890] | |||
XR-3005 | Drug Info | [550890] | |||
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 525621 | XR3054, structurally related to limonene, is a novel inhibitor of farnesyl protein transferase. Eur J Cancer. 1999 Jun;35(6):1014-9. | ||||
Ref 533645 | Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956. Cancer Res. 1995 Nov 15;55(22):5310-4. | ||||
Ref 545288 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002714) | ||||
Ref 545701 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004259) | ||||
Ref 545818 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004901) | ||||
Ref 545819 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004903) | ||||
Ref 545839 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004994) | ||||
Ref 545970 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005580) | ||||
Ref 546113 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006417) | ||||
Ref 546334 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007534) | ||||
Ref 546335 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007537) | ||||
Ref 546522 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008739) | ||||
Ref 546523 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008741) | ||||
Ref 547062 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012642) | ||||
Ref 547153 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013446) | ||||
Ref 525621 | XR3054, structurally related to limonene, is a novel inhibitor of farnesyl protein transferase. Eur J Cancer. 1999 Jun;35(6):1014-9. | ||||
Ref 526198 | A 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 526296 | J 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 526408 | Exploring 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 526603 | Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.A novel metal-chelating inhibitor of protein farnesyltransferase. | ||||
Ref 526670 | Bioorg 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 527321 | Bioorg 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 527491 | Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9.Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors. | ||||
Ref 527568 | J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. | ||||
Ref 527662 | Recent progress in protein farnesyltransferase inhibition. IDrugs. 2000 Nov;3(11):1336-45. | ||||
Ref 527723 | Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection. J Heart Lung Transplant. 2005 Sep;24(9):1403-9. | ||||
Ref 533645 | Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956. Cancer Res. 1995 Nov 15;55(22):5310-4. | ||||
Ref 533648 | Ras 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 534307 | J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. | ||||
Ref 534405 | J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. | ||||
Ref 534739 | J 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 550155 | WO patent application no. 2011,0881,26, Treatment of viral infection with prenyltransferase inhibitors. | ||||
Ref 550890 | US patent application no. 2005,0227,929, Combination therapy comprising a cox-2 inhibitor and an antineoplastic agent. | ||||
Ref 551289 | Local constrained shifty pseudopeptides inhibitors of rasfarnesyl transferase, Bioorg. Med. Chem. Lett. 5(22):2677-2682 (1995). |
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