Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T53524 | Target Info | |||
| Target Name | Platelet-derived growth factor receptor alpha (PDGFRA) | ||||
| Synonyms | RHEPDGFRA; Platelet-derived growth factor receptor 2; Platelet-derived growth factor alpha receptor; PDGFR2; PDGFR-alpha; PDGFR-2; PDGF-R-alpha; CD140a antigen; CD140a; CD140 antigen-like family member A; Alpha-type platelet-derived growth factor receptor; Alpha platelet-derived growth factor receptor | ||||
| Target Type | Successful Target | ||||
| Gene Name | PDGFRA | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Imatinib | Ligand Info | |||||
| Structure Description | Crystal structure of PDGFRA in complex with imatinib by co-crystallization | PDB:6JOL | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [1] |
| PDB Sequence |
DSRWEFPRDG
592 LVLGRVLGSG602 AFGKVVEGTA612 YGLSRSQPVM622 KVAVKMLKPT632 ARSSEKQALM 642 SELKIMTHLG652 PHLNIVNLLG662 ACTKSGPIYI672 ITEYCFYGDL682 VNYLHKNRDS 692 FLTLLDLLSF798 TYQVARGMEF808 LASKNCVHRD818 LAARNVLLAQ828 GKIVKICDFG 838 LARDIMHDSN848 YVSKGSTFLP858 VKWMAPESIF868 DNLYTTLSDV878 WSYGILLWEI 888 FSLGGTPYPG898 MMVDSTFYNK908 IKSGYRMAKP918 DHATSEVYEI928 MVKCWNSEPE 938 KRPSFYHLSE948 IVENLLPGQ
|
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LEU599
3.864
VAL607
3.918
ALA625
3.536
VAL626
3.935
LYS627
3.506
GLU644
2.995
ILE647
4.278
MET648
3.455
LEU651
4.775
VAL658
3.304
ILE672
3.710
ILE673
4.977
THR674
2.999
|
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| Ligand Name: Sunitinib | Ligand Info | |||||
| Structure Description | Crystal structure of PDGFRA in complex with sunitinib by soaking | PDB:6JOK | ||||
| Method | X-ray diffraction | Resolution | 3.80 Å | Mutation | No | [2] |
| PDB Sequence |
EIRWRVIESI
565 SPDGHEYIYV575 DPMQLPYDSR585 WEFPRDGLVL595 GRVLGSGAFG605 KVVEGTAYGL 615 SRSQPVMKVA625 VKMLKPTARS635 SEKQALMSEL645 KIMTHLGPHL655 NIVNLLGACT 665 KSGPIYIITE675 YCFYGDLVNY685 LHKNRDSFLS695 HEVKNLLSDD785 NSEGLTLLDL 795 LSFTYQVARG805 MEFLASKNCV815 HRDLAARNVL825 LAQGKIVKIC835 DFGLARDIMH 845 DSNYVSKGST855 FLPVKWMAPE865 SIFDNLYTTL875 SDVWSYGILL885 WEIFSLGGTP 895 YPGMMVDSTF905 YNKIKSGYRM915 AKPDHATSEV925 YEIMVKCWNS935 EPEKRPSFYH 945 LSEIVENLLP955 GQYKKSYEKI965 HLDFLKSD
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| Ligand Name: CP-868596 | Ligand Info | |||||
| Structure Description | Crystal structure of PDGFRA T674I in complex with crenolanib by soaking | PDB:6JOJ | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | No | [3] |
| PDB Sequence |
RYEIRWRVIE
563 SISPDGHEYI573 YVDPMQLPYD583 SRWEFPRDGL593 VLGRVLGSGA603 FGKVVEGTAY 613 GLSRSQPVMK623 VAVKMLKPTA633 RSSEKQALMS643 ELKIMTHLGP653 HLNIVNLLGA 663 CTKSGPIYII673 TEYCFYGDLV683 NYLHKNRDSF693 LSVKNLLSDD785 NSEGLTLLDL 795 LSFTYQVARG805 MEFLASKNCV815 HRDLAARNVL825 LAQGKIVKIC835 DFGLARDIMH 845 DSNYVSKGST855 FLPVKWMAPE865 SIFDNLYTTL875 SDVWSYGILL885 WEIFSLGGTP 895 YPGMMVDSTF905 YNKIKSGYRM915 AKPDHATSEV925 YEIMVKCWNS935 EPEKRPSFYH 945 LSEIVENLLP955 GQYKKSYEKI965 HLDFLKSD
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .6T2 or .6T22 or .6T23 or :36T2;style chemicals stick;color identity;select .A:599 or .A:600 or .A:607 or .A:625 or .A:627 or .A:658 or .A:674 or .A:675 or .A:676 or .A:677 or .A:678 or .A:679 or .A:680 or .A:681 or .A:825 or .A:835 or .A:836 or .A:837 or .A:838 or .A:840 or .A:841; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU599
3.668
GLY600
4.257
VAL607
4.071
ALA625
3.440
LYS627
3.283
VAL658
4.256
THR674
3.752
GLU675
3.614
TYR676
3.326
CYS677
2.852
PHE678
2.528
|
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: PDGFRalpha kinase inhibitor 1 | Ligand Info | |||||
| Structure Description | Crystal structure of PDGFRA in Complex with WQ-C-159 | PDB:5GRN | ||||
| Method | X-ray diffraction | Resolution | 1.77 Å | Mutation | No | [4] |
| PDB Sequence |
DSRWEFPRDG
592 LVLGRVLGSG602 AFGKVVEGTA612 YGLSRSQPVM622 KVAVKMLKPT632 ARSSEKQALM 642 SELKIMTHLG652 PHLNIVNLLG662 ACTKSGPIYI672 ITEYCFYGDL682 VNYLHKNRDS 692 FLSNSEGLTL792 LDLLSFTYQV802 ARGMEFLASK812 NCVHRDLAAR822 NVLLAQGKIV 832 KICDFGLARD842 IMHDSNYVSK852 GSTFLPVKWM862 APESIFDNLY872 TTLSDVWSYG 882 ILLWEIFSLG892 GTPYPGMMVD902 STFYNKIKSG912 YRMAKPDHAT922 SEVYEIMVKC 932 WNSEPEKRPS942 FYHLSEIVEN952 LLPGQY
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .748 or .7482 or .7483 or :3748;style chemicals stick;color identity;select .A:599 or .A:607 or .A:625 or .A:626 or .A:627 or .A:644 or .A:647 or .A:648 or .A:651 or .A:657 or .A:658 or .A:672 or .A:673 or .A:674 or .A:675 or .A:676 or .A:677 or .A:680 or .A:809 or .A:814 or .A:815 or .A:816 or .A:817 or .A:825 or .A:834 or .A:835 or .A:836 or .A:837; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU599
3.692
VAL607
3.849
ALA625
3.489
VAL626
3.953
LYS627
3.453
GLU644
3.098
ILE647
3.716
MET648
3.465
LEU651
3.857
ILE657
3.863
VAL658
3.770
ILE672
3.675
ILE673
4.800
THR674
2.905
|
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Crystal structure of PDGFRA in complex with imatinib by co-crystallization | ||||
| REF 2 | Crystal structure of PDGFRA in complex with sunitinib by soaking | ||||
| REF 3 | Crystal structure of PDGFRA in complex with crenolanib by soaking | ||||
| REF 4 | Crystal Structure of PDGFRA in Complex with WQ-C-159 | ||||
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