Target General Infomation
Target ID
T86528
Former ID
TTDI02575
Target Name
Geranyltranstransferase
Gene Name
GGPS1
Synonyms
(2E,6E)farnesyl diphosphate synthase; Dimethylallyltranstransferase; Farnesyl diphosphate synthase; Farnesyltranstransferase; GGPP synthase; GGPPSase; Geranylgeranyl diphosphate synthase; Geranylgeranyl pyrophosphate synthase; GGPS1
Target Type
Research
Disease Bone disease [ICD10: M00-M99]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Catalyzes the trans-addition of the three molecules of IPP onto DMAPP to form geranylgeranyl pyrophosphate, an important precursor of carotenoids and geranylated proteins.
BioChemical Class
Alkyl aryl transferase
UniProt ID
EC Number
EC 2.5.1.10
Sequence
MEKTQETVQRILLEPYKYLLQLPGKQVRTKLSQAFNHWLKVPEDKLQIIIEVTEMLHNAS
LLIDDIEDNSKLRRGFPVAHSIYGIPSVINSANYVYFLGLEKVLTLDHPDAVKLFTRQLL
ELHQGQGLDIYWRDNYTCPTEEEYKAMVLQKTGGLFGLAVGLMQLFSDYKEDLKPLLNTL
GLFFQIRDDYANLHSKEYSENKSFCEDLTEGKFSFPTIHAIWSRPESTQVQNILRQRTEN
IDIKKYCVHYLEDVGSFEYTRNTLKELEAKAYKQIDARGGNPELVALVKHLSKMFKEENE
Inhibitor (2E, 6E)-farnesylbisphosphonate Drug Info [529074]
3-azageranylgeranyl diphosphate Drug Info [526333]
BPH-252 Drug Info [529700]
BPH-608 Drug Info [528871]
BPH-628 Drug Info [529700]
BPH-629 Drug Info [528871]
BPH-675 Drug Info [528871]
BPH-676 Drug Info [528871]
BPH-715 Drug Info [529700]
BPH-742 Drug Info [529700]
compound 11 Drug Info [529700]
compound 12 Drug Info [526333]
compound 14 Drug Info [529700]
compound 16 Drug Info [529700]
compound 19 Drug Info [529700]
compound 47 Drug Info [529700]
compound 51 Drug Info [529700]
CT-10 Drug Info [543909]
digeranyl bisphosphonate Drug Info [529700]
minodronic acid Drug Info [529700]
PG-1014491 Drug Info [543909]
Pathways
BioCyc Pathway Superpathway of geranylgeranyldiphosphate biosynthesis I (via mevalonate)
Superpathway of cholesterol biosynthesis
Trans, trans-farnesyl diphosphate biosynthesis
Geranylgeranyldiphosphate biosynthesis
KEGG Pathway Terpenoid backbone biosynthesis
Metabolic pathways
Biosynthesis of antibiotics
PANTHER Pathway Cholesterol biosynthesis
PathWhiz Pathway Steroid Biosynthesis
Reactome Cholesterol biosynthesis
Activation of gene expression by SREBF (SREBP)
WikiPathways Activation of Gene Expression by SREBP (SREBF)
References
Ref 526333Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents. J Med Chem. 2002 May 23;45(11):2185-96.
Ref 528871Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases. Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7. Epub 2007 May 29.
Ref 529074Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors. Bioorg Med Chem. 2008 Jan 1;16(1):390-9. Epub 2007 Sep 18.
Ref 529700Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation. J Med Chem. 2008 Sep 25;51(18):5594-607.
Ref 543909(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 643).

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