Reference on EC 2.5.1.58 - protein farnesyltransferase
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REF. 
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Casey, P.J.; Seabra, M.C.
Protein prenyltransferases
J. Biol. Chem.
271
5289-5292
1996
Saccharomyces cerevisiae
Furfine, E.S; Leban, J.J.; Landavazo, A.; Moomaw, J.F.; Casey, P.J.
Protein farnesyltransferase: kinetics of farnesyl pyrophosphate binding and product release
Biochemistry
34
6857-6862
1995
Rattus norvegicus
Long, S.B.; Casey, P.J.; Beese, L.S.
Cocrystal structure of protein farnesyltransferase complexed with a farnesyl diphosphate substrate
Biochemistry
37
9612-9618
1998
Rattus norvegicus
Micali, E.; Chehade, K.A.; Isaacs, R.J.; Andres, D.A.; Spielmann, H.P.
Protein farnesyltransferase isoprenoid substrate discrimination is dependent on isoprene double bonds and branched methyl groups
Biochemistry
40
12254-12265
2001
Rattus norvegicus
Long, S.B.; Casey, P.J.; Beese, L.S.
Reaction path of protein farnesyltransferase at atomic resolution
Nature
419
645-650
2002
Rattus norvegicus
Chen, W.J.; Moomaw, J.F.; Overton, L.; Kost, T.A.; Casey, P.J.
High level expression of mammalian protein farnesyltransferase in a baculovirus system
J. Biol. Chem.
286
9675-9680
1993
Rattus norvegicus
Park, H.W.; Beese, L.S.
Protein farnesyltransferase
Curr. Opin. Struct. Biol.
7
873-880
1997
Saccharomyces cerevisiae, Homo sapiens, Rattus norvegicus
Okolotowicz, K.J.; Lee, W.J.; Hartman, R.F.; Kim, A.Y.; Ottersberg, S.R.; Robinson, D.E., Jr.; Lefler, S.R.; Rose, S.D.
Inactivation of protein farnesyltransferase by active-site-targeted dicarbonyl compounds
Arch. Pharm.
334
194-202
2001
Homo sapiens
Caplin, B.E.; Hettich, L.A.; Marshall, M.S.
Substrate characterization of the Saccharomyces cerevisiae protein farnesyltransferase and type-I protein geranylgeranyltransferase
Biochim. Biophys. Acta
1205
39-48
1994
Saccharomyces cerevisiae
Ibrahim, M.; Azzouz, N.; Gerold, P.; Schwarz, R.T.
Identification and characterisation of Toxoplasma gondii protein farnesyltransferase
Int. J. Parasitol.
31
1489-1497
2001
Homo sapiens, Toxoplasma gondii
Yokoyama, K.; Trobridge, P.; Buckner, F.S.; Van Voorhis, W.C.; Stuart, K.D.; Gelb, M.H.
Protein farnesyltransferase from Trypanosoma brucei. A heterodimer of 61- and 65-kDa subunits as a new target for antiparasite therapeutics
J. Biol. Chem.
273
26497-26505
1998
Rattus norvegicus, Trypanosoma brucei brucei, Trypanosoma brucei brucei EATRO 140
Buckner, F.S.; Yokoyama, K.; Nguyen, L.; Grewal, A.; Erdjument-Bromage, H.; Tempst, P.; Strickland, C.L.; Xiao, L.; Van Voorhis, W.C.; Gelb, M.H.
Cloning, heterologous expression, and distinct substrate specificity of protein farnesyltransferase from Trypanosoma brucei
J. Biol. Chem.
275
21870-21876
2000
Trypanosoma brucei brucei
Buckner, F.S.; Eastman, R.T.; Nepomuceno-Silva, J.L.; Speelmon, E.C.; Myler, P.J.; Van Voorhis, W.C.; Yokoyama, K.
Cloning, heterologous expression, and substrate specificities of protein farnesyltransferases from Trypanosoma cruzi and Leishmania major
Mol. Biochem. Parasitol.
122
181-188
2002
Leishmania amazonensis, Trypanosoma brucei brucei, Leishmania major (Q8WR00), Leishmania major (Q8WR01), Leishmania major, Trypanosoma cruzi (Q8WR02), Trypanosoma cruzi (Q8WR03), Trypanosoma cruzi (Q8WR04), Trypanosoma cruzi, Leishmania amazonensis LV78
Fu, H.W.; Beese, L.S.; Casey, P.J.
Kinetic analysis of zinc ligand mutants of mammalian protein farnesyltransferase
Biochemistry
37
4465-4472
1998
Rattus norvegicus
Huang, C.c.; Hightower, K.E.; Fierke, C.A.
Mechanistic studies of rat protein farnesyltransferase indicate an associative transition state
Biochemistry
39
2593-2602
2000
Rattus norvegicus
Saderholm, M.J.; Hightower, K.E.; Fierke, C.A.
Role of metals in the reaction catalyzed by protein farnesyltransferase
Biochemistry
39
12398-12405
2000
Rattus norvegicus
Pickett, J.S.; Bowers, K.E.; Hartman, H.L.; Fu, H.W.; Embry, A.C.; Casey, P.J.; Fierke, C.A.
Kinetic studies of protein farnesyltransferase mutants establish active substrate conformation
Biochemistry
42
9741-9748
2003
Rattus norvegicus
Gomez, R.; Goodman, L.E.; Tripathy, S.K.; O'Rourke, E.; Manne, V.; Tamanoi, F.
Purified yeast protein farnesyltransferase is structurally and functionally similar to its mammalian counterpart
Biochem. J.
289
25-31
1993
Saccharomyces cerevisiae
Andres, D.A.; Goldstein, J.L.; Ho, Y.K.; Brown, M.S.
Mutational analysis of a-subunit of protein farnesyltransferase. Evidence for a catalytic role
J. Biol. Chem.
268
1383-1390
1993
Rattus norvegicus
Ryu, K.Y.; Baik, Y.J.; Yang, C.H.
Purification and characterization of farnesyl protein transferase from bovine testis
J. Biochem. Mol. Biol.
28
197-203
1995
Bos taurus
-
Qian, D.; Zhou, D.; Ju, R.; Cramer, C.L.; Yang, Z.
Protein farnesyltransferase in plants: molecular characterization and involvement in cell cycle control
Plant Cell
8
2381-2394
1996
Nicotiana tabacum, Pisum sativum
Schmitt, D.; Callan, K.; Gruissem.W.
Molecular and biochemical characterization of tomato farnesyl-protein transferase
Plant Physiol.
112
767-777
1996
Solanum lycopersicum
Dunten, P.; Kammlott, U.; Crowther, R.; Weber, D.; Palermo, R.; Birktoft, J.
Protein farnesyltransferase: Structure and implications for substrate binding
Biochemistry
37
7907-7912
1998
Rattus norvegicus
Roskoski, R.Jr.; Ritchie, P.
Role of the carboxyterminal residue in peptide binding to protein farnesyltransferase and protein geranylgeranyltransferase
Arch. Biochem. Biophys.
356
167-176
1998
Rattus norvegicus
Wu, Z.; Demma, M.; Strickland, C.L.; Syto, R.; Le, H.V.; Windsor, W.T.; Weber, P.C.
High-level expression, purification, kinetic characterization and crystallization of protein farnesyltransferase b-subunit C-terminal mutants
Protein Eng.
12
341-348
1999
Homo sapiens, Rattus norvegicus
Chakrabarti, D.; Da Silva, T.; Barger, J.; Paquette, S.; Patel, H.; Patterson, S.; Allen, C.M.
Protein Farnesyltransferase and protein prenylation in Plasmodium falciparum
J. Biol. Chem.
277
42066-42073
2002
Plasmodium falciparum
Park, H.W.; Boduluri, S.R.; Moomaw, J.F.; Casey, P.J.; Beese, L.S.
Crystal structure of protein farnesyltransferase at 2.25 angstrom resolution
Science
275
1800-1804
1997
Rattus norvegicus
Pais, J.E.; Bowers, K.E.; Stoddard, A.K.; Fierke, C.A.
A continuous fluorescent assay for protein prenyltransferases measuring diphosphate release
Anal. Biochem.
345
302-311
2005
Escherichia coli
Turek-Etienne, T.C.; Strickland, C.L.; Distefano, M.D.
Biochemical and structural studies with prenyl diphosphate analogues provide insights into isoprenoid recognition by protein farnesyl transferase
Biochemistry
42
3716-3724
2003
Saccharomyces cerevisiae
Bowers, K.E.; Fierke, C.A.
Positively charged side chains in protein farnesyltransferase enhance catalysis by stabilizing the formation of the diphosphate leaving group
Biochemistry
43
5256-5265
2004
Rattus norvegicus
Reid, T.S.; Long, S.B.; Beese, L.S.
Crystallographic analysis reveals that anticancer clinical candidate L-778,123 inhibits protein farnesyltransferase and geranylgeranyltransferase-I by different binding modes
Biochemistry
43
9000-9008
2004
Homo sapiens
Reigard, S.A.; Zahn, T.J.; Haworth, K.B.; Hicks, K.A.; Fierke, C.A.; Gibbs, R.A.
Interplay of isoprenoid and peptide substrate specificity in protein farnesyltransferase
Biochemistry
44
11214-11223
2005
Rattus norvegicus
Curtin, M.L.; Florjancic, A.S.; Cohen, J.; Gu, W.Z.; Frost, D.J.; Muchmore, S.W.; Sham, H.L.
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase
Bioorg. Med. Chem. Lett.
13
1367-1371
2003
Rattus norvegicus
Mijimolle, N.; Velasco, J.; Dubus, P.; Guerra, C.; Weinbaum, C.A.; Casey, P.J.; Campuzano, V.; Barbacid, M.
Protein farnesyltransferase in embryogenesis, adult homeostasis, and tumor development
Cancer Cell
7
313-324
2005
Mus musculus
Maurer-Stroh, S.; Washietl, S.; Eisenhaber, F.
Protein prenyltransferases
Genome Biol.
4
212
2003
Homo sapiens
Tobin, D.A.; Pickett, J.S.; Hartman, H.L.; Fierke, C.A.; Penner-Hahn, J.E.
Structural characterization of the zinc site in protein farnesyltransferase
J. Am. Chem. Soc.
125
9962-9969
2003
Rattus norvegicus
Pickett, J.S.; Bowers, K.E.; Fierke, C.A.
Mutagenesis studies of protein farnesyltransferase implicate aspartate beta 352 as a magnesium ligand
J. Biol. Chem.
278
51243-51250
2003
Rattus norvegicus
Kumagai, M.; Makioka, A.; Takeuchi, T.; Nozaki, T.
Molecular cloning and characterization of a protein farnesyltransferase from the enteric protozoan parasite Entamoeba histolytica
J. Biol. Chem.
279
2316-2323
2004
Entamoeba histolytica (Q76L89), Entamoeba histolytica (Q76L90), Entamoeba histolytica
Reid, T.S.; Terry, K.L.; Casey, P.J.; Beese, L.S.
Crystallographic analysis of CaaX prenyltransferases complexed with substrates defines rules of protein substrate selectivity
J. Mol. Biol.
343
417-433
2004
Homo sapiens
Courdavault, V.; Burlat, V.; St-Pierre, B.; Giglioli-Guivarc'h, N.
Characterisation of CaaX-prenyltransferases in Catharanthus roseus: relationships with the expression of genes involved in the early stages of monoterpenoid biosynthetic pathway
Plant Sci.
168
1097-1107
2005
Catharanthus roseus (Q6EZ49), Catharanthus roseus (Q6J6P6)
Hartman, H.L.; Hicks, K.A.; Fierke, C.A.
Peptide specificity of protein prenyltransferases is determined mainly by reactivity rather than binding affinity
Biochemistry
44
15314-15324
2005
Rattus norvegicus
Ryckebusch, A.; Gilleron, P.; Millet, R.; Houssin, R.; Lemoine, A.; Pommery, N.; Grellier, P.; Sergheraert, C.; Henichart, J.P.
Novel N-(4-piperidinyl)benzamide antimalarials with mammalian protein farnesyltransferase inhibitory activity
Chem. Pharm. Bull.
53
1324-1326
2005
Rattus norvegicus
Duckworth, B.P.; Zhang, Z.; Hosokawa, A.; Distefano, M.D.
Selective labeling of proteins by using protein farnesyltransferase
ChemBioChem
8
98-105
2007
Saccharomyces cerevisiae
Eastman, R.T.; White, J.; Hucke, O.; Bauer, K.; Yokoyama, K.; Nallan, L.; Chakrabarti, D.; Verlinde, C.L.; Gelb, M.H.; Rathod, P.K.; Van Voorhis, W.C.
Resistance to a protein farnesyltransferase inhibitor in Plasmodium falciparum
J. Biol. Chem.
280
13554-13559
2005
Plasmodium falciparum
Henriksen, B.S.; Zahn, T.J.; Evanseck, J.D.; Firestine, S.M.; Gibbs, R.A.
Computational and conformational evaluation of FTase alternative substrates: insight into a novel enzyme binding pocket
J. Chem. Inf. Model.
45
1047-1052
2005
Homo sapiens
Guida, W.C.; Hamilton, A.D.; Crotty, J.W.; Sebti, S.M.
Protein farnesyltransferase: flexible docking studies on inhibitors using computational modeling
J. Comput. Aided Mol. Des.
19
871-885
2006
Rattus norvegicus
Lane, K.T.; Beese, L.S.
Thematic review series: lipid posttranslational modifications. Structural biology of protein farnesyltransferase and geranylgeranyltransferase type I
J. Lipid Res.
47
681-699
2006
Homo sapiens
Clark, M.K.; Scott, S.A.; Wojtkowiak, J.; Chirco, R.; Mathieu, P.; Reiners, J.J.; Mattingly, R.R.; Borch, R.F.; Gibbs, R.A.
Synthesis, biochemical, and cellular evaluation of farnesyl monophosphate prodrugs as farnesyltransferase inhibitors
J. Med. Chem.
50
3274-3282
2007
Homo sapiens
Eastman, R.T.; White, J.; Hucke, O.; Yokoyama, K.; Verlinde, C.L.; Hast, M.A.; Beese, L.S.; Gelb, M.H.; Rathod, P.K.; Van Voorhis, W.C.
Resistance mutations at the lipid substrate binding site of Plasmodium falciparum protein farnesyltransferase
Mol. Biochem. Parasitol.
152
66-71
2007
Plasmodium falciparum
Ohkanda, J.; Strickland, C.L.; Blaskovich, M.A.; Carrico, D.; Lockman, J.W.; Vogt, A.; Bucher, C.J.; Sun, J.; Qian, Y.; Knowles, D.; Pusateri, E.E.; Sebti, S.M.; Hamilton, A.D.
Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase
Org. Biomol. Chem.
4
482-492
2006
Mus musculus
Courdavault, V.; Thiersault, M.; Courtois, M.; Gantet, P.; Oudin, A.; Doireau, P.; St-Pierre, B.; Giglioli-Guivarch, N.
CaaX-prenyltransferases are essential for expression of genes involved in the early stages of monoterpenoid biosynthetic pathway in Catharanthus roseus cells
Plant Mol. Biol.
57
855-870
2005
Catharanthus roseus (Q6EZ49), Catharanthus roseus
Zeng, Q.; Wang, X.; Running, M.P.
Dual lipid modification of Arabidopsis Ggamma-subunits is required for efficient plasma membrane targeting
Plant Physiol.
143
1119-1131
2007
Arabidopsis thaliana
Sousa, S.F.; Fernandes, P.A.; Ramos, M.J.
Effective tailor-made force field parameterization of the several Zn coordination environments in the puzzling FTase enzyme: opening the door to the full understanding of its elusive catalytic mechanism
Theoret. Chem. Accounts
117
171-181
2007
Rattus norvegicus
-
Cui, G.; Merz, K.M.
Computational studies of the farnesyltransferase ternary complex part II: the conformational activation of farnesyldiphosphate
Biochemistry
46
12375-12381
2007
Homo sapiens
Gilleron, P.; Wlodarczyk, N.; Houssin, R.; Farce, A.; Laconde, G.; Goossens, J.F.; Lemoine, A.; Pommery, N.; Henichart, J.P.; Millet, R.
Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors
Bioorg. Med. Chem. Lett.
17
5465-5471
2007
Homo sapiens
Bolchi, C.; Pallavicini, M.; Rusconi, C.; Diomede, L.; Ferri, N.; Corsini, A.; Fumagalli, L.; Pedretti, A.; Vistoli, G.; Valoti, E.
Peptidomimetic inhibitors of farnesyltransferase with high in vitro activity and significant cellular potency
Bioorg. Med. Chem. Lett.
17
6192-6196
2007
Homo sapiens
Olepu, S.; Suryadevara, P.K.; Rivas, K.; Yokoyama, K.; Verlinde, C.L.; Chakrabarti, D.; Van Voorhis, W.C.; Gelb, M.H.
2-Oxo-tetrahydro-1,8-naphthyridines as selective inhibitors of malarial protein farnesyltransferase and as anti-malarials
Bioorg. Med. Chem. Lett.
18
494-497
2008
Plasmodium falciparum, Rattus norvegicus
Braun, T.; Fenaux, P.
Farnesyltransferase inhibitors and their potential role in therapy for myelodysplastic syndromes and acute myeloid leukaemia
Br. J. Haematol.
141
576-586
2008
Homo sapiens
Nguyen, U.T.; Cramer, J.; Gomis, J.; Reents, R.; Gutierrez-Rodriguez, M.; Goody, R.S.; Alexandrov, K.; Waldmann, H.
Exploiting the substrate tolerance of farnesyltransferase for site-selective protein derivatization
Chembiochem
8
408-423
2007
Homo sapiens
Equbal, T.; Silakari, O.; Ravikumar, M.
Exploring three-dimensional quantitative structural activity relationship (3D-QSAR) analysis of SCH 66336 (Sarasar) analogues of farnesyltransferase inhibitors
Eur. J. Med. Chem.
43
204-209
2008
Homo sapiens
Hosokawa, A.; Wollack, J.W.; Zhang, Z.; Chen, L.; Barany, G.; Distefano, M.D.
Evaluation of an alkyne-containing analogue of farnesyl diphosphate as a dual substrate for protein-prenyltransferases
Int. J. Pept. Res. Ther.
13
345-354
2007
Saccharomyces cerevisiae
-
Iwasaki, S.; Omura, S.
Search for protein farnesyltransferase inhibitors of microbial origin: our strategy and results as well as the results obtained by other groups
J. Antibiot.
60
1-12
2007
Homo sapiens
Puntambekar, D.S.; Giridhar, R.; Yadav, M.R.
Inhibition of farnesyltransferase: a rational approach to treat cancer?
J. Enzyme Inhib. Med. Chem.
22
127-140
2007
Homo sapiens
Bendale, P.; Olepu, S.; Suryadevara, P.K.; Bulbule, V.; Rivas, K.; Nallan, L.; Smart, B.; Yokoyama, K.; Ankala, S.; Pendyala, P.R.; Floyd, D.; Lombardo, L.J.; Williams, D.K.; Buckner, F.S.; Chakrabarti, D.; Verlinde, C.L.; Van Voorhis, W.C.; Gelb, M.H.
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials
J. Med. Chem.
50
4585-4605
2007
Plasmodium falciparum, Rattus norvegicus
Labadie, G.R.; Viswanathan, R.; Poulter, C.D.
Farnesyl diphosphate analogues with omega-bioorthogonal azide and alkyne functional groups for protein farnesyl transferase-catalyzed ligation reactions
J. Org. Chem.
72
9291-9297
2007
Saccharomyces cerevisiae
Kim, S.J.; Kwon, B.; Kim, S.; Baek, N.; Yang, J.H.; Lee, J.J.; Lee, S.I.; Kwon, Y.; Park, H.W.; Lee, J.H.; Park, J.; Kim, D.K.
Farnesyl protein transferase inhibitory components of Lithospermum erythrorhizon
Nat. Prod. Sci.
13
328-331
2007
Homo sapiens, Rattus norvegicus
-
de Figueiredo, R.M.; Coudray, L.; Dubois, J.
Synthesis and biological evaluation of potential bisubstrate inhibitors of protein farnesyltransferase. Design and synthesis of functionalized imidazoles
Org. Biomol. Chem.
5
3299-3309
2007
Saccharomyces cerevisiae
Hougland, J.L.; Lamphear, C.L.; Scott, S.A.; Gibbs, R.A.; Fierke, C.A.
Context-dependent substrate recognition by protein farnesyltransferase
Biochemistry
48
1691-1701
2009
Rattus norvegicus
Sousa, S.F.; Fernandes, P.A.; Ramos, M.J.
Molecular dynamics simulations on the critical states of the farnesyltransferase enzyme
Bioorg. Med. Chem.
17
3369-3378
2009
Rattus norvegicus
Duez, S.; Coudray, L.; Mouray, E.; Grellier, P.; Dubois, J.
Towards the synthesis of bisubstrate inhibitors of protein farnesyltransferase: Synthesis and biological evaluation of new farnesylpyrophosphate analogues
Bioorg. Med. Chem.
18
543-556
2010
Saccharomyces cerevisiae, Homo sapiens, Plasmodium falciparum, Trypanosoma brucei
DeGraw, A.J.; Hast, M.A.; Xu, J.; Mullen, D.; Beese, L.S.; Barany, G.; Distefano, M.D.
Caged protein prenyltransferase substrates: tools for understanding protein prenylation
Chem. Biol. Drug Des.
72
171-181
2008
Saccharomyces cerevisiae
Hast, M.A.; Fletcher, S.; Cummings, C.G.; Pusateri, E.E.; Blaskovich, M.A.; Rivas, K.; Gelb, M.H.; Van Voorhis, W.C.; Sebti, S.M.; Hamilton, A.D.; Beese, L.S.
Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase
Chem. Biol.
16
181-192
2009
Homo sapiens, Plasmodium falciparum, Rattus norvegicus
Subramanian, T.; Liu, S.; Troutman, J.M.; Andres, D.A.; Spielmann, H.P.
Protein farnesyltransferase-catalyzed isoprenoid transfer to peptide depends on lipid size and shape, not hydrophobicity
ChemBioChem
9
2872-2882
2008
Rattus norvegicus
Gupta, M.K.; Prabhakar, Y.S.
QSAR study on tetrahydroquinoline analogues as plasmodium protein farnesyltransferase inhibitors: a comparison of rationales of malarial and mammalian enzyme inhibitory activities for selectivity
Eur. J. Med. Chem.
43
2751-2767
2008
Plasmodium falciparum, Rattus norvegicus (Q02293), Rattus norvegicus (Q04631)
Zhou, J.; Vos, C.C.; Gjyrezi, A.; Yoshida, M.; Khuri, F.R.; Tamanoi, F.; Giannakakou, P.
The protein farnesyltransferase regulates HDAC6 activity in a microtubule-dependent manner
J. Biol. Chem.
284
9648-9655
2009
Homo sapiens (P49354), Homo sapiens
Coudray, L.; de Figueiredo, R.M.; Duez, S.; Cortial, S.; Dubois, J.
Synthesis of imidazole-containing analogues of farnesyl pyrophosphate and evaluation of their biological activity on protein farnesyltransferase
J. Enzyme Inhib. Med. Chem.
24
972-985
2009
Saccharomyces cerevisiae, Homo sapiens, Plasmodium falciparum
Pinel, B.; Dubois, J.; Seraphin, D.; Richomme, P.
Semisynthesis of alpha-methyl-gamma-lactones and in vitro evaluation of their activity on protein farnesyltransferase
J. Enzyme Inhib. Med. Chem.
25
172-179
2010
Saccharomyces cerevisiae
Yang, S.H.; Chang, S.Y.; Andres, D.A.; Spielmann, H.P.; Young, S.G.; Fong, L.G.
Assessing the efficacy of protein farnesyltransferase inhibitors in mouse models of progeria
J. Lipid Res.
51
400-405
2010
Mus musculus
Lethu, S.; Ginisty, M.; Bosc, D.; Dubois, J.
Discovery of a new class of protein farnesyltransferase inhibitors in the arylthiophene series
J. Med. Chem.
52
6205-6208
2009
Saccharomyces cerevisiae
DeGraw, A.J.; Keiser, M.J.; Ochocki, J.D.; Shoichet, B.K.; Distefano, M.D.
Prediction and evaluation of protein farnesyltransferase inhibition by commercial drugs
J. Med. Chem.
53
2464-2471
2010
Rattus norvegicus
Hougland, J.L.; Hicks, K.A.; Hartman, H.L.; Kelly, R.A.; Watt, T.J.; Fierke, C.A.
Identification of novel peptide substrates for protein farnesyltransferase reveals two substrate classes with distinct sequence selectivities
J. Mol. Biol.
395
176-190
2010
Rattus norvegicus
Long, C.; Marcourt, L.; Raux, R.; David, B.; Gau, C.; Menendez, C.; Gao, M.; Laroche, M.F.; Schambel, P.; Delaude, C.; Ausseil, F.; Lavaud, C.; Massiot, G.
Meroterpenes from Dichrostachys cinerea inhibit protein farnesyl transferase activity
J. Nat. Prod.
72
1804-1815
2009
Rattus norvegicus
Wang, Y.; Beaith, M.; Chalifoux, M.; Ying, J.; Uchacz, T.; Sarvas, C.; Griffiths, R.; Kuzma, M.; Wan, J.; Huang, Y.
Shoot-specific down-regulation of protein farnesyltransferase (alpha-subunit) for yield protection against drought in canola
Mol. Plant
2
191-200
2009
Brassica napus
Subramanian, T.; Pais, J.E.; Liu, S.; Troutman, J.M.; Suzuki, Y.; Leela Subramanian, K.; Fierke, C.A.; Andres, D.A.; Spielmann, H.P.
Farnesyl diphosphate analogues with aryl moieties are efficient alternate substrates for protein farnesyltransferase
Biochemistry
51
8307-8319
2012
Rattus norvegicus
Baciu-Atudosie, L.; Ghinet, A.; Farce, A.; Dubois, J.; Belei, D.; Bicu, E.
Synthesis and biological evaluation of new phenothiazine derivatives bearing a pyrazole unit as protein farnesyltransferase inhibitors
Bioorg. Med. Chem. Lett.
22
6896-6902
2012
Homo sapiens
Qiao, Y.; Gao, J.; Qiu, Y.; Wu, L.; Guo, F.; Lo, K.K.; Li, D.
Design, synthesis, and characterization of piperazinedione-based dual protein inhibitors for both farnesyltransferase and geranylgeranyltransferase-I
Eur. J. Med. Chem.
46
2264-2273
2011
Rattus norvegicus
Yang, Y.; Wang, B.; Ucisik, M.N.; Cui, G.; Fierke, C.A.; Merz, K.M.
Insights into the mechanistic dichotomy of the protein farnesyltransferase peptide substrates CVIM and CVLS
J. Am. Chem. Soc.
134
820-823
2012
Rattus norvegicus (Q04631)
Hast, M.A.; Nichols, C.B.; Armstrong, S.M.; Kelly, S.M.; Hellinga, H.W.; Alspaugh, J.A.; Beese, L.S.
Structures of Cryptococcus neoformans protein farnesyltransferase reveal strategies for developing inhibitors that target fungal pathogens
J. Biol. Chem.
286
35149-35162
2011
Cryptococcus neoformans, Cryptococcus neoformans B-3501A
Hougland, J.L.; Gangopadhyay, S.A.; Fierke, C.A.
Expansion of protein farnesyltransferase specificity using "tunable" active site interactions: development of bioengineered prenylation pathways
J. Biol. Chem.
287
38090-38100
2012
Homo sapiens
Lethu, S.; Bosc, D.; Mouray, E.; Grellier, P.; Dubois, J.
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis
J. Enzyme Inhib. Med. Chem.
28
163-171
2013
Saccharomyces cerevisiae, Homo sapiens, Trypanosoma brucei
Wang, Y.C.; Dozier, J.K.; Beese, L.S.; Distefano, M.D.
Rapid analysis of protein farnesyltransferase substrate specificity using peptide libraries and isoprenoid diphosphate analogues
ACS Chem. Biol.
9
1726-1735
2014
Saccharomyces cerevisiae (P29703 AND P22007), Saccharomyces cerevisiae, Rattus norvegicus (Q04631 AND Q02293), Rattus norvegicus, Candida albicans (Q9Y765)
Kubala, M.H.; Norwood, S.J.; Gomez, G.A.; Jones, A.; Johnston, W.; Yap, A.S.; Mureev, S.; Alexandrov, K.
Mammalian farnesyltransferase alpha subunit regulates vacuolar protein sorting-associated protein 4A (Vps4A)-dependent intracellular trafficking through recycling endosomes
Biochem. Biophys. Res. Commun.
468
580-586
2015
Saccharomyces cerevisiae (P29703), Rattus norvegicus (Q04631)
Abuhaie, C.M.; Ghinet, A.; Farce, A.; Dubois, J.; Rigo, B.; Bicu, E.
Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors
Bioorg. Med. Chem. Lett.
23
5887-5892
2013
Homo sapiens
Jennings, B.C.; Danowitz, A.M.; Wang, Y.C.; Gibbs, R.A.; Distefano, M.D.; Fierke, C.A.
Analogs of farnesyl diphosphate alter CaaX substrate specificity and reactions rates of protein farnesyltransferase
Bioorg. Med. Chem. Lett.
26
1333-1336
2016
Rattus norvegicus (Q04631 AND Q02293)
Shen, M.; Pan, P.; Li, Y.; Li, D.; Yu, H.; Hou, T.
Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling
Drug Discov. Today
20
267-276
2015
Homo sapiens (P49354), Homo sapiens (P49356), Rattus norvegicus (Q02293), Rattus norvegicus (Q04631)
Bosc, D.; Mouray, E.; Cojean, S.; Franco, C.H.; Loiseau, P.M.; Freitas-Junior, L.H.; Moraes, C.B.; Grellier, P.; Dubois, J.
Highly improved antiparasitic activity after introduction of an N-benzylimidazole moiety on protein farnesyltransferase inhibitors
Eur. J. Med. Chem.
109
173-186
2016
Homo sapiens, Trypanosoma brucei
Soni, R.; Sharma, D.; Patel, S.; Sharma, B.; Bhatt, T.K.
Structure-based binding between protein farnesyl transferase and PRL-PTP of malaria parasite: an interaction study of prenylation process in Plasmodium
J. Biomol. Struct. Dyn.
34
2667-2678
2016
Plasmodium falciparum
Bosc, D.; Mouray, E.; Grellier, P.; Cojean, S.; Loiseau, P.; Dubois, J.
Introduction of methionine mimics on 3-arylthiophene: Influence on protein farnesyltransferase inhibition and on antiparasitic activity
MedChemComm
4
1034-1041
2013
Homo sapiens, Trypanosoma brucei
-
Mabanglo, M.F.; Hast, M.A.; Lubock, N.B.; Hellinga, H.W.; Beese, L.S.
Crystal structures of the fungal pathogen Aspergillus fumigatus protein farnesyltransferase complexed with substrates and inhibitors reveal features for antifungal drug design
Protein Sci.
23
289-301
2014
Aspergillus fumigatus
Zhang, C.; Gao, F.; Wu, W.; Qiu, W.X.; Zhang, L.; Li, R.; Zhuang, Z.N.; Yu, W.; Cheng, H.; Zhang, X.Z.
Enzyme-driven membrane-targeted chimeric peptide for enhanced tumor photodynamic immunotherapy
ACS Nano
13
11249-11262
2019
Mus musculus (Q61239 and Q8K2I1)
Lucescu, L.; Ghinet, A.; Shova, S.; Magnez, R.; Thuru, X.; Farce, A.; Rigo, B.; Belei, D.; Dubois, J.; Bicu, E.
Exploring isoxazoles and pyrrolidinones decorated with the 4,6-dimethoxy-1,3,5-triazine unit as human farnesyltransferase inhibitors
Arch. Pharm.
352
e1800227
2019
Homo sapiens (P49354 and P49356)
Ashok, S.; Hildebrandt, E.R.; Ruiz, C.S.; Hardgrove, D.S.; Coreno, D.W.; Schmidt, W.K.; Hougland, J.L.
Protein farnesyltransferase catalyzes unanticipated farnesylation and geranylgeranylation of shortened target sequences
Biochemistry
59
1149-1162
2020
Rattus norvegicus (Q04631 AND Q02293)
Hagemann, A.; Mueller, G.; Manthey, I.; Bachmann, H.S.
Exploring the putative self-binding property of the human farnesyltransferase alpha-subunit
FEBS Lett.
591
3637-3648
2017
Homo sapiens (P49354 and P49356), Homo sapiens, Rattus norvegicus (Q04631 AND Q02293)
Zhang, Y.; Auger, S.; Schaefer, J.V.; Plueckthun, A.; Distefano, M.D.
Site-selective enzymatic labeling of designed ankyrin repeat proteins using protein farnesyltransferase
Methods Mol. Biol.
2033
207-219
2019
Saccharomyces cerevisiae (P29703 AND P22007), Saccharomyces cerevisiae
Aboelfotoh Hendy, A.; Xing, J.; Chen, X.; Chen, X.L.
The farnesyltransferase beta-subunit RAM1 regulates localization of RAS proteins and appressorium-mediated infection in Magnaporthe oryzae
Mol. Plant Pathol.
20
1264-1278
2019
Pyricularia oryzae (G4MY67), Pyricularia oryzae ATCC MYA-4617 (G4MY67)
Wu, J.R.; Wang, L.C.; Lin, Y.R.; Weng, C.P.; Yeh, C.H.; Wu, S.J.
The Arabidopsis heat-intolerant 5 (hit5)/enhanced response to aba 1 (era1) mutant reveals the crucial role of protein farnesylation in plant responses to heat stress
New Phytol.
213
1181-1193
2017
Arabidopsis thaliana (Q38920)
Su, P.; Gao, L.; Liu, S.; Guan, H.; Wang, J.; Zhang, Y.; Zhao, Y.; Hu, T.; Tu, L.; Zhou, J.; Ma, B.; Liu, X.; Huang, L.; Gao, W.
Probing the function of protein farnesyltransferase in Tripterygium wilfordii
Plant Cell Rep.
38
211-220
2019
Tripterygium wilfordii
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