Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T19229 Target Info
Target Name Proton-coupled folate transporter (SLC46A1)
Synonyms
Solute carrier family 46 member 1; PCFT/HCP1; PCFT; Heme carrier protein 1; HCP1; G21
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Target Type Successful Target
Gene Name SLC46A1
UniProt ID
PCFT_HUMAN
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 Solute carrier family 19 member 1 (SLC19A1) Successful Target
UniProt ID S19A1_HUMAN
Gene Name 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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Representative Drug(s) Methotrexate Drug Info IC50 = 12 nM [2]
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 [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 [3]
Co-Target Name Nuclear receptor coactivator 3 (NCOA3) Literature-reported Target
UniProt ID NCOA3_HUMAN
Gene Name NCOA3
Synonyms
bHLHe42; Thyroid hormone receptor activator molecule 1; TRAM1; TRAM-1; Steroid receptor coactivator protein 3; SRC-3; Receptor-associated coactivator 3; RAC3; RAC-3; PCIP; NCoA-3; Class E basic helix-loop-helix protein 42; CBP-interacting protein; Amplified in breast cancer-1 protein; Amplified in breast cancer 1 protein; AIB1 (SRC-3); AIB1; AIB-1; ACTR
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Representative Drug(s) Methotrexate Drug Info IC50 = 210.97 nM [4]
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 [5]
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 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 3 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 4 PubChem BioAssay: 2017 update. Nucleic Acids Res. 2017 Jan 4;45(D1):D955-D963.
REF 5 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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