Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T35465 | Target Info | |||
| Target Name | Solute carrier family 19 member 1 (SLC19A1) | ||||
| Synonyms |
Reduced folate carrier protein; RFC1; RFC; Placental folate transporter; Intestinal folate carrier 1; IFC-1; Folate transporter 1; FOLT; FLOT1
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| Target Type | Successful Target | ||||
| Gene Name | SLC19A1 | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Dihydrofolate reductase (DHFR) | Successful Target | ||||
| UniProt ID | DYR_HUMAN | |||||
| Gene Name | DHFR | |||||
| Synonyms |
DYR; DHFRP1
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| Representative Drug(s) | Methotrexate | Drug Info | Ki = 0.00034 nM | [1] | ||
| Co-Target Name | Folate receptor alpha (FOLR1) | Successful Target | ||||
| UniProt ID | FOLR1_HUMAN | |||||
| Gene Name | FOLR1 | |||||
| Synonyms |
Ovarian tumorassociated antigen MOv18; KB cells FBP; Folate receptor, adult; Folate receptor 1; FRalpha; FOLR1; Adult folatebinding protein
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| Representative Drug(s) | Methotrexate | Drug Info | IC50 = 114 nM | [2] | ||
| Co-Target Name | Proton-coupled folate transporter (SLC46A1) | Successful Target | ||||
| UniProt ID | PCFT_HUMAN | |||||
| Gene Name | SLC46A1 | |||||
| Synonyms |
Solute carrier family 46 member 1; PCFT/HCP1; PCFT; Heme carrier protein 1; HCP1; G21
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| Representative Drug(s) | Methotrexate | Drug Info | IC50 = 120.5 nM | [3] | ||
| Co-Target Name | Folate receptor beta (FOLR2) | Literature-reported Target | ||||
| UniProt ID | FOLR2_HUMAN | |||||
| Gene Name | FOLR2 | |||||
| Synonyms |
Placental folate-binding protein; Folate receptor, fetal/placental; Folate receptor type-beta; Folate receptor 2; FR-beta; FOLR2
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| Representative Drug(s) | Methotrexate | Drug Info | IC50 = 106 nM | [2] | ||
| Co-Target Name | Thymidylate synthase (TYMS) | Literature-reported Target | ||||
| UniProt ID | TYSY_HUMAN | |||||
| Gene Name | TYMS | |||||
| Synonyms |
TSase; TS
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| Representative Drug(s) | Methotrexate | Drug Info | Ki = 600 nM | [1] | ||
| Co-Target Name | Thymidylate synthase/GAR transformylase/AICAR transformylase (TYMS/GAR/TATIC) | Co-Target | ||||
| UniProt ID | TYSY_HUMAN; PUR2_HUMAN; PUR9_HUMAN | |||||
| Gene Name | TYMS; GART; ATIC | |||||
| Synonyms |
Tsase; PRGS; PURH
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| Representative Drug(s) | Methotrexate | Drug Info | IC50 = 10 nM | [4] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-based selectivity optimization of piperidine-pteridine derivatives as potent Leishmania pteridine reductase inhibitors. J Med Chem. 2012 Oct 11;55(19):8318-29. | ||||
| REF 2 | Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor alpha and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis. J Med Chem. 2018 Mar 8;61(5):2027-40. | ||||
| REF 3 | Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors alpha and beta and the proton-coupled folate transporter. J Med Chem. 2014 Oct 9;57(19):8152-66. | ||||
| REF 4 | Novel 6-substituted benzoyl and non-benzoyl straight chain pyrrolo[2,3-d]pyrimidines as potential antitumor agents with multitargeted inhibition of TS, GARFTase and AICARFTase. Eur J Med Chem. 2017 Oct 20;139:531-541. | ||||
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