Proteins > Proton-coupled folate transporter
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Proton-coupled folate transporter
A proton-coupled folate transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q96NT5]
Synonyms
G21;
Heme carrier protein 1;
PCFT/HCP1;
Solute carrier family 46 member 1
Research
Bioassay Publications (8)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 8 (100.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (4)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| pemetrexed | Homo sapiens (human) | K | 0.1570 | 2 | 2 |
Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors α and β and the proton-coupled folate transporter.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors α and β and the proton-coupled folate transporter.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Fluorine-Substituted Pyrrolo[2,3- d]Pyrimidine Analogues with Tumor Targeting via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide BiosynthesiJournal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents.Journal of medicinal chemistry, , Feb-12, Volume: 58, Issue:3, 2015
6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors α and β and the proton-coupled folate transporter.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Synthesis and biological activity of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl regioisomers as inhibitors of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporterJournal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reducJournal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Enables
This protein enables 8 target(s):
| Target | Category | Definition |
|---|
| folic acid binding | molecular function | Binding to 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. [GOC:jl, ISBN:0198506732] |
| folic acid transmembrane transporter activity | molecular function | Enables the transfer of folic acid (pteroylglutamic acid) from one side of a membrane to the other. Folic acid is widely distributed as a member of the vitamin B complex and is essential for the synthesis of purine and pyrimidines. [GOC:ai] |
| proton transmembrane transporter activity | molecular function | Enables the transfer of a proton from one side of a membrane to the other. [GOC:ai] |
| heme transmembrane transporter activity | molecular function | Enables the transfer of heme from one side of a membrane to the other. [PMID:29549126] |
| symporter activity | molecular function | Enables the active transport of a solute across a membrane by a mechanism whereby two or more species are transported together in the same direction in a tightly coupled process not directly linked to a form of energy other than chemiosmotic energy. [GOC:mtg_transport, ISBN:0815340729, PMID:10839820] |
| methotrexate transmembrane transporter activity | molecular function | Enables the transfer of methotrexate, 4-amino-10-methylformic acid from one side of a membrane to the other. Methotrexate is a folic acid analogue and a potent competitive inhibitor of dihydrofolate reductase. [GOC:ai] |
| folic acid:proton symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: folic acid(out) + H+(out) = folic acid(in) + H+(in). The main folic acid symporter is the Proton-Coupled Folate Transporter (PCFT/SLC46A1), which has similar affinity for transport of reduced folates (5-methyl THF, 5-formyl THF) and folic acid. [PMID:24745983] |
| transmembrane transporter activity | molecular function | Enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:jid, GOC:mtg_transport, ISBN:0815340729] |
Located In
This protein is located in 8 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] |
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| endosome membrane | cellular component | The lipid bilayer surrounding an endosome. [GOC:mah] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| brush border membrane | cellular component | The portion of the plasma membrane surrounding the brush border. [GOC:mah] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
Involved In
This protein is involved in 11 target(s):
| Target | Category | Definition |
|---|
| intracellular iron ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of iron ions within a cell. [GOC:ai, GOC:mah] |
| folic acid transport | biological process | The directed movement of folic acid (pteroylglutamic acid) into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Folic acid is widely distributed as a member of the vitamin B complex and is essential for the synthesis of purine and pyrimidines. [GOC:ai] |
| heme transport | biological process | The directed movement of heme, any compound of iron complexed in a porphyrin (tetrapyrrole) ring, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| heme metabolic process | biological process | The chemical reactions and pathways involving heme, any compound of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:jl, ISBN:0124325653] |
| 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] |
| methotrexate transport | biological process | The directed movement of methotrexate, 4-amino-10-methylformic acid, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Methotrexate is a folic acid analogue and a potent competitive inhibitor of dihydrofolate reductase. [GOC:ai] |
| intestinal folate absorption | biological process | Uptake of folic into the blood by absorption from the small intestine. [GOC:BHF, GOC:dos, GOC:hal, PMID:19762432] |
| folate transmembrane transport | biological process | The process in which a folic acid, or one of its derivatives (dihydrofolate, tetrahydrofolate, methylene-tetrahydrofolate or methyl-tetrahydrofolate) is transported across a membrane. [PMID:24745983] |
| proton transmembrane transport | biological process | The directed movement of a proton across a membrane. [GO_REF:0000069, GOC:pr, GOC:TermGenie] |
| folate import across plasma membrane | biological process | The directed movement of folic acid from outside of a cell, across the plasma membrane and into the cytosol. [GO_REF:0000075, GOC:BHF, GOC:hal, GOC:TermGenie, PMID:19762432] |
| transmembrane transport | biological process | The process in which a solute is transported across a lipid bilayer, from one side of a membrane to the other. [GOC:dph, GOC:jid] |