Proteins > Folylpolyglutamate synthase, mitochondrial
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Folylpolyglutamate synthase, mitochondrial
A folylpolyglutamate synthase, mitochondrial that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q05932]
Synonyms
EC 6.3.2.17;
Folylpoly-gamma-glutamate synthetase;
FPGS;
Tetrahydrofolylpolyglutamate synthase;
Tetrahydrofolate synthase
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 9 (50.00) | 18.2507 |
| 2000's | 9 (50.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (8)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| methotrexate | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
Drugs with Other Measurements
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
Design and synthesis of histidine analogues of folic acid and methotrexate as potential folylpolyglutamate synthetase inhibitors.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Benzoyl ring halogenated classical 2-amino-6-methyl-3,4-dihydro-4-oxo-5-substituted thiobenzoyl-7H-pyrrolo[2,3-d]pyrimidine antifolates as inhibitors of thymidylate synthase and as antitumor agents.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Synthesis of N-[4-[1-ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid as an antifolate.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Synthesis and biological activities of tricyclic conformationally restricted tetrahydropyrido annulated furo[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Novel 2,4-diamino-5-substituted-pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolate inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Thienyl and thiazolyl acyclic analogues of 5-deazatetrahydrofolic acid.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Synthesis and biological activity of open-chain analogues of 5,6,7,8-tetrahydrofolic acid--potential antitumor agents.Journal of medicinal chemistry, , Apr-17, Volume: 35, Issue:8, 1992
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| tetrahydrofolylpolyglutamate synthase activity | molecular function | Catalysis of the reaction: ATP + tetrahydrofolyl-(Glu)(n) + L-glutamate = ADP + phosphate + tetrahydrofolyl-(Glu)(n+1). [EC:6.3.2.17] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| mitochondrial inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai] |
| mitochondrial matrix | cellular component | The gel-like material, with considerable fine structure, that lies in the matrix space, or lumen, of a mitochondrion. It contains the enzymes of the tricarboxylic acid cycle and, in some organisms, the enzymes concerned with fatty acid oxidation. [GOC:as, ISBN:0198506732] |
| 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] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| 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] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| liver development | biological process | The process whose specific outcome is the progression of the liver over time, from its formation to the mature structure. The liver is an exocrine gland which secretes bile and functions in metabolism of protein and carbohydrate and fat, synthesizes substances involved in the clotting of the blood, synthesizes vitamin A, detoxifies poisonous substances, stores glycogen, and breaks down worn-out erythrocytes. [GOC:add, ISBN:068340007X] |
| nucleobase-containing compound metabolic process | biological process | Any cellular metabolic process involving nucleobases, nucleosides, nucleotides and nucleic acids. [GOC:ai] |
| glutamate metabolic process | biological process | The chemical reactions and pathways involving glutamate, the anion of 2-aminopentanedioic acid. [GOC:go_curators] |
| one-carbon metabolic process | biological process | The chemical reactions and pathways involving the transfer of one-carbon units in various oxidation states. [GOC:hjd, GOC:mah, GOC:pde] |
| folic acid-containing compound metabolic process | biological process | The chemical reactions and pathways involving a folic acid-containing compound, i.e. any of a group of heterocyclic compounds based on the pteroic acid skeleton conjugated with one or more L-glutamic acid or L-glutamate units. [GOC:ai, GOC:mah] |
| animal organ regeneration | biological process | The regrowth of a lost or destroyed animal organ. [GOC:mah] |
| folic acid metabolic process | biological process | The chemical reactions and pathways involving folic acid, pteroylglutamic acid. Folic acid is widely distributed as a member of the vitamin B complex and is essential for the synthesis of purine and pyrimidines. [ISBN:0198506732] |
| tetrahydrofolylpolyglutamate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of tetrahydrofolylpolyglutamate, a folate derivative comprising tetrahydrofolate attached to a chain of glutamate residues. [GOC:ai] |