Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T91331 | Target Info | |||
| Target Name | Fibroblast growth factor receptor 3 (FGFR3) | ||||
| Synonyms | JTK4; FGFR-3; CD333 | ||||
| Target Type | Successful Target | ||||
| Gene Name | FGFR3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | L-betagamma-meATP | Ligand Info | |||
| Canonical SMILES | C1=NC(=C2C(=N1)N(C=N2)C3C(C(C(O3)COP(=O)(O)OP(=O)(CP(=O)(O)O)O)O)O)N | ||||
| InChI | 1S/C11H18N5O12P3/c12-9-6-10(14-2-13-9)16(3-15-6)11-8(18)7(17)5(27-11)1-26-31(24,25)28-30(22,23)4-29(19,20)21/h2-3,5,7-8,11,17-18H,1,4H2,(H,22,23)(H,24,25)(H2,12,13,14)(H2,19,20,21)/t5-,7-,8-,11-/m1/s1 | ||||
| InChIKey | UFZTZBNSLXELAL-IOSLPCCCSA-N | ||||
| PubChem Compound ID | 91532 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 4K33 Crystal Structure of FGF Receptor 3 (FGFR3) Kinase Domain Harboring the K650E Mutation, a Gain-of-Function Mutation Responsible for Thanatophoric Dysplasia Type II and Spermatocytic Seminoma | ||||||
| Method | X-ray diffraction | Resolution | 2.34 Å | Mutation | Yes | [1] |
| PDB Sequence |
LPADPKWELS
468 RARLTLGKPL478 GEGAFGQVVM488 AEAIGIDKDR498 AAKPVTVAVK508 MLKDDATDKD 518 LSDLVSEMEM528 MKMIGKHKNI538 INLLGACTQG548 GPLYVLVEYA558 AKGNLREFLR 568 ARRPPGLDYS578 FDTSEQLTFK592 DLVSCAYQVA602 RGMEYLASQK612 CIHRDLAARN 622 VLVTEDNVMK632 IADFGLARDV642 HNLDYYKETT652 NGRLPVKWMA662 PEALFDRVYT 672 HQSDVWSFGV682 LLWEIFTLGG692 SPYPGIPVEE702 LFKLLKEGHR712 MDKPANCTHD 722 LYMIMRECWH732 AAPSQRPTFK742 QLVEDLDRVL752 TVT
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LEU478
3.552
GLY479
3.490
GLU480
3.954
GLY481
3.470
ALA482
3.110
PHE483
2.669
GLY484
2.675
VAL486
3.543
ALA506
3.356
LYS508
2.790
GLU525
4.760
ILE539
3.996
|
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| PDB ID: 6PNX Crystal Structure of an Asymmetric Dimer of FGF Receptor 3 Kinases Trapped in A-loop Tyrosine Transphosphorylation Reaction | ||||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | Yes | [2] |
| PDB Sequence |
ELELPADPKW
465 ELSRARLTLG475 KPLGEGAFGQ485 VVMAEAIGID495 KDRAAKPVTV505 AVKMLKDDAT 515 DKDLSDLVSE525 MEMMKMIGKH535 KNIINLLGAC545 TQGGPLYVLV555 EYAAKGNLRE 565 FLRARRPPPE586 EQLTFKDLVS596 CAYQVARGME606 YLASQKCIHR616 DLAARNVLVT 626 EDNVMKIADF636 GLARDVHNLD646 YYKKTTNGRL656 PVKWMAPEAL666 FDEVYTHQSD 676 VWSFGVLLWE686 IFTLGGSPYP696 GIPVEELFKL706 LKEGHRMDKP716 ANCTHDLYMI 726 MRECWHAAPS736 QRPTFKQLVE746 DLDRVLTVTS756 T
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural mimicry of a-loop tyrosine phosphorylation by a pathogenic FGF receptor 3 mutation. Structure. 2013 Oct 8;21(10):1889-96. | ||||
| REF 2 | Molecular basis for receptor tyrosine kinase A-loop tyrosine transphosphorylation. Nat Chem Biol. 2020 Mar;16(3):267-277. | ||||
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