DGIdb - FDPS Gene Record

FDPS 2224 Druggable Genome

Alternate Names:

2224
FARNESYL DIPHOSPHATE SYNTHASE
FDPS
FPPS
FPS
POROK9
134629
3631
ENSG00000160752
OTTHUMG00000013909
644
P14324
FPP synthase
Geranyltranstransferase
Dimethylallyltranstransferase
(2E,6E)-farnesyl diphosphate synthase
Farnesyl pyrophosphate synthase
KIAA1293
PA28075
FPPS_HUMAN
BE0000776
T86528
NM_002004\|NM_001135821\|NM_001135822\|NM_001242824\|NM_001242825
NP_001995\|NP_001129293\|NP_001129294\|NP_001229753\|NP_001229754

Gene Info:

Target Main Class	Enzymes
Target Subclass	2.5.1.-
Target Class	Enzymes
Target Subclass	EC:2.5.1.10
Target Subclass	EC:2.5.1.-
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	Lanosterol biosynthesis pathway
GuideToPharmacology Gene Category ID	104

(8 More Sources)

Gene Categories: Category Details

DRUGGABLE GENOME
ENZYME

Publications:

Coxon et al., 2005, Phosphonocarboxylate inhibitors of Rab geranylgeranyl transferase disrupt the prenylation and membrane localization of Rab proteins in osteoclasts in vitro and in vivo., Bone
Dunford et al., 2001, Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates., J. Pharmacol. Exp. Ther.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Ortiz-Gómez et al., 2006, Farnesyl diphosphate synthase is a cytosolic enzyme in Leishmania major promastigotes and its overexpression confers resistance to risedronate., Eukaryotic Cell
Russell et al., 2007, Bisphosphonates: an update on mechanisms of action and how these relate to clinical efficacy., Ann. N. Y. Acad. Sci.
Bergstrom et al., 2000, Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase., Arch. Biochem. Biophys.
Gritzalis D et al., 2015, Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase., Bioorg Med Chem Lett
Yokoyama T et al., 2015, Protonation State and Hydration of Bisphosphonate Bound to Farnesyl Pyrophosphate Synthase., J Med Chem
Marini F et al., 2011, Pharmacogenetics of bisphosphonate-associated osteonecrosis of the jaw., Front Biosci (Elite Ed)
Chapurlat et al., 2006, Drug insight: Bisphosphonates for postmenopausal osteoporosis., Nat Clin Pract Endocrinol Metab
Rondeau et al., 2006, Structural basis for the exceptional in vivo efficacy of bisphosphonate drugs., ChemMedChem
Scrima M et al., 2014, Structural evidence of N6-isopentenyladenosine as a new ligand of farnesyl pyrophosphate synthase., J Med Chem
Pérez-Castrillón JL et al., 2014, Polymorphisms of the farnesyl diphosphate synthase gene modulate bone changes in response to atorvastatin., Rheumatol Int
Olmos JM et al., 2012, Common allelic variants of the farnesyl diphosphate synthase gene influence the response of osteoporotic women to bisphosphonates., Pharmacogenomics J
Riebeling et al., 2002, The bisphosphonate pamidronate induces apoptosis in human melanoma cells in vitro., Br. J. Cancer
Zhang et al., 2004, Pamidronate resistance and associated low ras levels in breast cancer cells: a role for combinatorial therapy., Ann. Clin. Lab. Sci.
Notarnicola et al., 2004, Higher farnesyl diphosphate synthase activity in human colorectal cancer inhibition of cellular apoptosis., Oncology
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Miwa A et al., 2012, YM-175 induces apoptosis of human native monocyte-lineage cells via inhibition of prenylation., Am J Hematol

RISEDRONIC ACID FDPS

Interaction Score: 9.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction in vitro assay, inhibition of recombinant human enzyme expressed in E.coli

Details of the Assay for Interaction In vitro inhibition of recombinant human FDPS expressed in E.coli.

Direct Interaction? True

PMIDs:
16006204 11160603 11752352 16835450 18056045 10620343 25630225 26314394

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD

RIBOPRINE FDPS

Interaction Score: 5.68

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25184810

Sources:
DTC
IBANDRONIC ACID FDPS

Interaction Score: 5.68

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name ibandronate, R484,Boniva, Bonviva, Bondronat

Novel drug target Established target

PMIDs:
16932286 16892359 11752352 11160603

Sources:
DrugBank TdgClinicalTrial TEND TTD
PAMIDRONIC ACID FDPS

Interaction Score: 5.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12177810 11160603 15487700 11752352 15713990 10620343

Sources:
TdgClinicalTrial TEND TTD
DIMETHYLALLYL DIPHOSPHATE FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
MINODRONIC ACID FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11160603

Sources:
DrugBank
ISOPENTENYLPYROPHOSPHATE FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
GERANYL DIPHOSPHATE FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
IBANDRONATE SODIUM FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PAMIDRONATE DISODIUM FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RISEDRONATE SODIUM FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL294192 FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ALENDRONATE SODIUM FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
(CYCLOHEXYLAMINO)METHYLENEDIPHOSPHONIC ACID FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of human recombinant FPPS expressed in Escherichia coli BL21

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ZOLEDRONIC ACID FDPS

Interaction Score: 2.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

Trial Name Zoledronic

PMIDs:
21196316

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD
INCADRONIC ACID FDPS

Interaction Score: 1.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
23044853

Sources:
DrugBank
ALENDRONIC ACID FDPS

Interaction Score: 1.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In vitro inhibition of recombinant human protein expressed in E coli.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
FARNESYL DIPHOSPHATE FDPS

Interaction Score: 0.81

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
TIPIFARNIB FDPS

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ATORVASTATIN FDPS

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24311107 21151198

Sources:
PharmGKB

Ensembl: ENSG00000160752
- Version: 101_38
Alternate Names:

FDPS Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P14324
- Version: January-2014
Alternate Names:

FDPS Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.5.1.10

Target Subclass EC:2.5.1.-

Publications:
TEND: P14324
- Version: 01-August-2011
Alternate Names:

FDPS Gene Symbol

P14324 Uniprot Accession

ENSG00000160752 Ensembl Gene Id

Gene Info:

Target Main Class Enzymes

Target Subclass 2.5.1.-

Publications:
GuideToPharmacology: 2224
- Version: 29-September-2020
Alternate Names:

3631 HUGO Gene ID

3631 HUGO Gene Symbol

farnesyl diphosphate synthase HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Lanosterol biosynthesis pathway

GuideToPharmacology Gene Category ID 104

Gene Categories:

ENZYME

Publications:

PharmGKB: FDPS

Version: 18-August-2020

Alternate Names:

PA28075 PharmGKB ID

Gene Info:

Publications:

Marini F et al., 2011, Pharmacogenetics of bisphosphonate-associated osteonecrosis of the jaw., Front Biosci (Elite Ed)

Marini F et al., 2008, Modulatory effect of farnesyl pyrophosphate synthase (FDPS) rs2297480 polymorphism on the response to long-term amino-bisphosphonate treatment in postmenopausal osteoporosis., Curr Med Res Opin

Olmos JM et al., 2012, Common allelic variants of the farnesyl diphosphate synthase gene influence the response of osteoporotic women to bisphosphonates., Pharmacogenomics J

DrugBank: BE0000776

Version: 5.1.7

Alternate Names:

FDPS DrugBank Gene Name

P14324 UniProt Accession

2224 Entrez Gene Id

Gene Info:

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Bergstrom et al., 2000, Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase., Arch. Biochem. Biophys.

Notarnicola et al., 2004, Higher farnesyl diphosphate synthase activity in human colorectal cancer inhibition of cellular apoptosis., Oncology

DTC: FDPS

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Yokoyama T et al., 2015, Protonation State and Hydration of Bisphosphonate Bound to Farnesyl Pyrophosphate Synthase., J Med Chem

Gritzalis D et al., 2015, Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase., Bioorg Med Chem Lett

Scrima M et al., 2014, Structural evidence of N6-isopentenyladenosine as a new ligand of farnesyl pyrophosphate synthase., J Med Chem

HingoraniCasas: ENSG00000160752
- Version: 31-May-2017
Alternate Names:

ENSG00000160752 Gene Symbol

FDPS Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: FPS
- Version: chembl_23
Alternate Names:

KIAA1293 GENE_SYMBOL

FDPS GENE_SYMBOL

Farnesyl pyrophosphate synthase UNIPROT

Gene Info:

Publications:
Pharos: FDPS
- Version: 03-September-2020
Alternate Names:

Farnesyl pyrophosphate synthase Gene Name

P14324 UniProt ID

Gene Info:

Gene Categories:

ENZYME

Publications:
Tempus: FDPS
- Version: 11-November-2018
Alternate Names:

FDPS Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
TTD: Geranyltranstransferase
- Version: 2020.06.01
Alternate Names:

FDPS TTD Gene Abbreviation

T86528 TTD Target ID

Gene Info:

Publications:

Details of the Assay for Interaction	in vitro assay, inhibition of recombinant human enzyme expressed in E.coli
Details of the Assay for Interaction	<i>In vitro</i> inhibition of recombinant human FDPS expressed in <i>E.coli</i>.
Direct Interaction?	True

Trial Name	ibandronate, R484,Boniva, Bonviva, Bondronat
Novel drug target	Established target

Mechanism of Interaction	Farnesyl diphosphate synthase inhibitor
Direct Interaction	yes

Details of the Assay for Interaction	Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

FDPS	Gene Symbol
P14324	Uniprot Accession
ENSG00000160752	Ensembl Gene Id

3631	HUGO Gene ID
3631	HUGO Gene Symbol
farnesyl diphosphate synthase	HUGO Gene Name

FDPS	DrugBank Gene Name
P14324	UniProt Accession
2224	Entrez Gene Id

KIAA1293	GENE_SYMBOL
FDPS	GENE_SYMBOL
Farnesyl pyrophosphate synthase	UNIPROT

FDPS Gene Record

FDPS 2224 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction in vitro assay, inhibition of recombinant human enzyme expressed in E.coli Details of the Assay for Interaction <i>In vitro</i> inhibition of recombinant human FDPS expressed in <i>E.coli</i>. Direct Interaction? True

PMIDs: 16006204 11160603 11752352 16835450 18056045 10620343 25630225 26314394

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25184810

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name ibandronate, R484,Boniva, Bonviva, Bondronat Novel drug target Established target

PMIDs: 16932286 16892359 11752352 11160603

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12177810 11160603 15487700 11752352 15713990 10620343

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 11160603

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Farnesyl diphosphate synthase inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Farnesyl diphosphate synthase inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Farnesyl diphosphate synthase inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Farnesyl diphosphate synthase inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Farnesyl diphosphate synthase inhibitor Direct Interaction yes Trial Name Zoledronic

PMIDs: 21196316

Sources: TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 23044853

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction <i>In vitro</i> inhibition of recombinant human protein expressed in <i>E coli</i>. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction in vitro assay, inhibition of recombinant human enzyme expressed in E.coli

Details of the Assay for Interaction <i>In vitro</i> inhibition of recombinant human FDPS expressed in <i>E.coli</i>.

Direct Interaction? True

PMIDs:
16006204 11160603 11752352 16835450 18056045 10620343 25630225 26314394

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
25184810

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name ibandronate, R484,Boniva, Bonviva, Bondronat

Novel drug target Established target

PMIDs:
16932286 16892359 11752352 11160603

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12177810 11160603 15487700 11752352 15713990 10620343

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
11160603

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of human recombinant FPPS expressed in Escherichia coli BL21

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Farnesyl diphosphate synthase inhibitor

Direct Interaction yes

Trial Name Zoledronic

PMIDs:
21196316

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
23044853

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction <i>In vitro</i> inhibition of recombinant human protein expressed in <i>E coli</i>.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
24311107 21151198

Sources:
PharmGKB

Alternate Names:

FDPS Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

FDPS Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.5.1.10

Target Subclass EC:2.5.1.-

Alternate Names:

FDPS Gene Symbol

P14324 Uniprot Accession

ENSG00000160752 Ensembl Gene Id

Gene Info:

Target Main Class Enzymes

Target Subclass 2.5.1.-

Alternate Names:

3631 HUGO Gene ID

3631 HUGO Gene Symbol

farnesyl diphosphate synthase HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Lanosterol biosynthesis pathway

GuideToPharmacology Gene Category ID 104

Gene Categories:

ENZYME