Proteins > Protein farnesyltransferase subunit beta
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Protein farnesyltransferase subunit beta
A protein farnesyltransferase subunit beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P49356]
Synonyms
FTase-beta;
EC 2.5.1.58;
CAAX farnesyltransferase subunit beta;
Ras proteins prenyltransferase subunit beta
Research
Bioassay Publications (53)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 12 (22.64) | 18.2507 |
| 2000's | 27 (50.94) | 29.6817 |
| 2010's | 14 (26.42) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (29)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| l 778,123 | Homo sapiens (human) | EC50 | 0.0920 | 1 | 1 |
| farnesyl pyrophosphate | Homo sapiens (human) | Kd | 0.0020 | 1 | 1 |
| a 228839 | Homo sapiens (human) | EC50 | 0.0160 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| farnesyl pyrophosphate | Homo sapiens (human) | Km | 0.0735 | 2 | 2 |
Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Ras farnesyltransferase: a new therapeutic target.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.MedChemComm, , Volume: 4, Issue:3, 2013
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 14, Issue:23, 2004
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 inhibitorJournal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Analogs of 4-(3-bromo-8-methyl-10-methoxy-6,11-dihydro-5H-benzo[5,6]-cyclo hepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N-oxide as inhibitors of farnesyl protein transferase.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.Journal of medicinal chemistry, , Jul-15, Volume: 42, Issue:14, 1999
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
(+)-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-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.MedChemComm, , Volume: 4, Issue:3, 2013
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.MedChemComm, , Volume: 4, Issue:3, 2013
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.Bioorganic & medicinal chemistry letters, , Feb-26, Volume: 11, Issue:4, 2001
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Chemical and biological explorations of the electrophilic reactivity of the bioactive marine natural product halenaquinone with biomimetic nucleophiles.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia.Bioorganic & medicinal chemistry, , Aug-15, Volume: 18, Issue:16, 2010
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.MedChemComm, , Volume: 4, Issue:3, 2013
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.Journal of enzyme inhibition and medicinal chemistry, , Volume: 28, Issue:1, 2013
Chemical and biological explorations of the electrophilic reactivity of the bioactive marine natural product halenaquinone with biomimetic nucleophiles.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity.Bioorganic & medicinal chemistry letters, , Mar-26, Volume: 11, Issue:6, 2001
3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-19, Volume: 11, Issue:22, 2001
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 9, Issue:8, 1999
Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.MedChemComm, , Volume: 4, Issue:3, 2013
Synthesis of acyloxymethyl ester prodrugs of the transferable protein farnesyl transferase substrate farnesyl methylenediphosphonate.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
Grignard-mediated synthesis and preliminary biological evaluation of novel 3-substituted farnesyl diphosphate analogues.Bioorganic & medicinal chemistry letters, , Aug-07, Volume: 10, Issue:15, 2000
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators.Journal of medicinal chemistry, , Jul-11, Volume: 56, Issue:13, 2013
Synthesis and biological evaluation of new phenothiazine derivatives bearing a pyrazole unit as protein farnesyltransferase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Novel indolizine derivatives with unprecedented inhibitory activity on human farnesyltransferase.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Towards the synthesis of bisubstrate inhibitors of protein farnesyltransferase: Synthesis and biological evaluation of new farnesylpyrophosphate analogues.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Ras farnesyltransferase: a new therapeutic target.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
A novel metal-chelating inhibitor of protein farnesyltransferase.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.Bioorganic & medicinal chemistry letters, , Sep-22, Volume: 8, Issue:18, 1998
(+)-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-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compJournal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein farnesyltransferase activity | molecular function | Catalysis of the reaction: farnesyl diphosphate + protein-cysteine = S-farnesyl protein + diphosphate. [EC:2.5.1.58, PMID:8621375] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| microtubule associated complex | cellular component | Any multimeric complex connected to a microtubule. [GOC:jl] |
| protein farnesyltransferase complex | cellular component | A protein complex that possesses protein farnesyltransferase activity. [GOC:mah] |
Involved In
This protein is involved in 2 target(s):
| Target | Category | Definition |
|---|
| lipid metabolic process | biological process | The chemical reactions and pathways involving lipids, compounds soluble in an organic solvent but not, or sparingly, in an aqueous solvent. Includes fatty acids; neutral fats, other fatty-acid esters, and soaps; long-chain (fatty) alcohols and waxes; sphingoids and other long-chain bases; glycolipids, phospholipids and sphingolipids; and carotenes, polyprenols, sterols, terpenes and other isoprenoids. [GOC:ma] |
| protein farnesylation | biological process | The covalent attachment of a farnesyl group to a protein. [GOC:jl] |