Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T83386 | Target Info | |||
| Target Name | Folate receptor alpha (FOLR1) | ||||
| Synonyms | Ovarian tumorassociated antigen MOv18; KB cells FBP; Folate receptor, adult; Folate receptor 1; FRalpha; FOLR1; Adult folatebinding protein | ||||
| Target Type | Successful Target | ||||
| Gene Name | FOLR1 | ||||
| Biochemical Class | Folate receptor | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Folic acid | Ligand Info | |||||
| Structure Description | Crystal structure of human folate receptor alpha in complex with folic acid | PDB:4LRH | ||||
| Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | No | [1] |
| PDB Sequence |
RTELLNVCMN
17 AKHHKEKPGP27 EDKLHEQCRP37 WRKNACCSTN47 TSQEAHKDVS57 YLYRFNWNHC 67 GEMAPACKRH77 FIQDTCLYEC87 SPNLGPWIQQ97 VDQSWRKERV107 LNVPLCKEDC 117 EQWWEDCRTS127 YTCKSNWHKG137 WNWTSGFNKC147 AVGAACQPFH157 FYFPTPTVLC 167 NEIWTHSYKV177 SNYSRGSGRC187 IQMWFDPAQG197 NPNEEVARFY207 AAAMSGT |
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| Ligand Name: N-(4-{[2-(2-Amino-4-Oxo-4,7-Dihydro-3h-Pyrrolo[2,3-D]pyrimidin-6-Yl)ethyl]amino}benzene-1-Carbonyl)-L-Glutamic Acid | Ligand Info | |||||
| Structure Description | Crystal structure of human folate receptor alpha in complex with novel antifolate AGF183 | PDB:5IZQ | ||||
| Method | X-ray diffraction | Resolution | 3.60 Å | Mutation | No | [2] |
| PDB Sequence |
RTELLNVCMN
17 AKHHKEKPGP27 EDKLHEQCRP37 WRKNACCSTN47 TSQEAHKDVS57 YLYRFNWNHC 67 GEMAPACKRH77 FIQDTCLYEC87 SPNLGPWIQQ97 VDQSWRKERV107 LNVPLCKEDC 117 EQWWEDCRTS127 YTCKSNWHKG137 WNWTSGFNKC147 AVGAACQPFH157 FYFPTPTVLC 167 NEIWTHSYKV177 SNYSRGSGRC187 IQMWFDPAQG197 NPNEEVARFY207 AAAMSGT |
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural basis for molecular recognition of folic acid by folate receptors. Nature. 2013 Aug 22;500(7463):486-9. | ||||
| REF 2 | Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor Alpha and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis. J Med Chem. 2016 Sep 8;59(17):7856-76. | ||||
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