Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T58454 | Target Info | |||
| Target Name | Fibroblast growth factor receptor 2 (FGFR2) | ||||
| Synonyms | Keratinocyte growth factor receptor 2; Keratinocyte growth factor receptor; KSAM; KGFR; K-sam; FGFR-2; FGF-2 receptor; CD332; BEK | ||||
| Target Type | Successful Target | ||||
| Gene Name | FGFR2 | ||||
| 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: 6V6Q Crystal Structure of Monophosphorylated FGF Receptor 2 isoform IIIb with PTR657 | ||||||
| Method | X-ray diffraction | Resolution | 2.46 Å | Mutation | Yes | [1] |
| PDB Sequence |
FELPEDPKWE
475 FPRDKLTLGK485 PLGEGCFGQV495 VMAEAVGIDK505 DKPKEAVTVA515 VKMLKDDATE 525 KDLSDLVSEM535 EMMKMIGKHK545 NIINLLGACT555 QDGPLFVIVE565 FASKGNLREF 575 LRARRPPQMT599 FKDLVSCTFQ609 LARGMEFLAS619 QKCIHRDLAA629 RNVLVTENNV 639 MKIADFGLAR649 DINNIDFKKT660 TNGRLPVKWM670 APEALFDRVY680 THQSDVWSFG 690 VLMWEIFTLG700 GSPYPGIPVE710 ELFKLLKEGH720 RMDKPANCTN730 ELFMMMRDCW 740 HAVPSQRPTF750 KQLVEDLDRI760 LTLTT
|
|||||
|
|
LEU487
2.847
GLY488
3.212
GLU489
4.254
GLY490
3.173
CYS491
3.701
PHE492
4.083
GLY493
4.143
VAL495
3.679
ALA515
3.130
LYS517
4.538
ILE548
4.446
|
|||||
| PDB ID: 2PVF Crystal Structure of Tyrosine Phosphorylated Activated FGF Receptor 2 (FGFR2) Kinase Domain in Complex with ATP Analog and Substrate Peptide | ||||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | Yes | [2] |
| PDB Sequence |
ELPEDPKWEF
476 PRDKLTLGKP486 LGEGAFGQVV496 MAEAVGIDKD506 KPVTVAVKML519 KDDATEKDLS 529 DLVSEMEMMK539 MIGKHKNIIN549 LLGACTQDGP559 LYVIVEYASK569 GNLREYLRAR 579 RPPGMESYQM598 TFKDLVSCTY608 QLARGMEYLA618 SQKCIHRDLA628 ARNVLVTENN 638 VMKIADFGLA648 RDINNIDKKT660 TNGRLPVKWM670 APEALFDRVY680 THQSDVWSFG 690 VLMWEIFTLG700 GSPYPGIPVE710 ELFKLLKEGH720 RMDKPANCTN730 ELYMMMRDCW 740 HAVPSQRPTF750 KQLVEDLDRI760 LTLTT
|
|||||
|
|
LEU487
3.596
GLY488
3.529
GLU489
4.775
GLY490
2.957
ALA491
3.172
PHE492
3.007
GLY493
2.971
VAL495
3.641
ALA515
3.269
LYS517
2.715
GLU534
4.836
ILE548
4.418
|
|||||
| PDB ID: 3CLY Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domains Trapped in Trans-Phosphorylation Reaction | ||||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | Yes | [3] |
| PDB Sequence |
LPEDPKWEFP
1477 RDKLTLGKPL1487 GEGAFGQVVM1497 AEAVGIDKDK1507 PKEAVTVAVK1517 MLKDDATEKD 1527 LSDLVSEMEM1537 MKMIGKHKNI1547 INLLGACTQD1557 GPLYVIVEYA1567 SKGNLREYLR 1577 ARREEQMTFK1601 DLVSCTYQLA1611 RGMEYLASQK1621 CIHRDLAARN1631 VLVTENNVMK 1641 IADFGLARDI1651 NNIDKKTTNG1663 RLPVKWMAPE1673 ALFDRVYTHQ1683 SDVWSFGVLM 1693 WEIFTLGGSP1703 YPGIPVEELF1713 KLLKEGHRMD1723 KPANCTNELY1733 MMMRDCWHAV 1743 PSQRPTFKQL1753 VEDLDRILTL1763 TTNEEYLDL
|
|||||
|
|
LEU1487
3.540
GLY1488
3.395
GLU1489
4.984
ALA1491
4.096
GLN1494
3.097
VAL1495
3.595
ALA1515
3.223
LYS1517
2.619
GLU1534
4.479
ILE1548
4.469
VAL1564
3.417
|
|||||
| PDB ID: 5EG3 Crystal Structure of the Activated FGF Receptor 2 (FGFR2) Kinase Domain in complex with the cSH2 domain of Phospholipase C gamma (PLCgamma) | ||||||
| Method | X-ray diffraction | Resolution | 2.61 Å | Mutation | Yes | [4] |
| PDB Sequence |
FELPEDPKWE
475 FPRDKLTLGK485 PLGEGAFGQV495 VMAEAVGIDK505 DKPKEAVTVA515 VKMLKDDATE 525 KDLSDLVSEM535 EMMKMIGKHK545 NIINLLGACT555 QDGPLYVIVA565 YASKGNLREY 575 LRARRPPGNR592 VPEEQMTFKD602 LVSCTYQLAR612 GMEYLASQKC622 IHRDLAARNV 632 LVTENNVMKI642 ADFGLARDIN652 NIDFFKETTN662 GRLPVKWMAP672 EALFDRVYTH 682 QSDVWSFGVL692 MWEIFTLGGS702 PYPGIPVEEL712 FKLLKEGHRM722 DKPANCTNEL 732 YMMMRDCWHA742 VPSQRPTFKQ752 LVEDLDRILT762 LTTNEELDLS773 Q |
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:488 or .A:489 or .A:490 or .A:495 or .A:515 or .A:517 or .A:534 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:574 or .A:626 or .A:630 or .A:631 or .A:633 or .A:644 or .A:664; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU487
3.652
GLY488
3.623
GLU489
4.468
GLY490
3.886
VAL495
3.794
ALA515
3.395
LYS517
2.864
GLU534
4.138
ILE548
4.203
VAL564
3.454
ALA565
2.760
|
|||||
| PDB ID: 4J99 Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Gain-of-Function K659T Mutation. | ||||||
| Method | X-ray diffraction | Resolution | 1.85 Å | Mutation | Yes | [5] |
| PDB Sequence |
YELPEDPKWE
475 FPRDKLTLGK485 PLGEGAFGQV495 VMAEAVGIDK505 DKPKEAVTVA515 VKMLKDDATE 525 KDLSDLVSEM535 EMMKMIGKHK545 NIINLLGACT555 QDGPLYVIVE565 YASKGNLREY 575 LRARRPQMTF600 KDLVSCTYQL610 ARGMEYLASQ620 KCIHRDLAAR630 NVLVTENNVM 640 KIADFGLARD650 INDYYKTNGR664 LPVKWMAPEA674 LFDRVYTHQS684 DVWSFGVLMW 694 EIFTLGGSPY704 PGIPVEELFK714 LLKEGHRMDK724 PANCTNELYM734 MMRDCWHAVP 744 SQRPTFKQLV754 EDLDRILTLT764
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:488 or .A:489 or .A:490 or .A:491 or .A:493 or .A:494 or .A:495 or .A:515 or .A:517 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:568 or .A:570 or .A:571 or .A:626 or .A:630 or .A:631 or .A:633 or .A:644; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU487
3.685
GLY488
2.623
GLU489
3.407
GLY490
3.328
ALA491
3.252
GLY493
4.866
GLN494
4.860
VAL495
3.029
ALA515
2.894
LYS517
3.452
ILE548
3.396
VAL564
2.761
|
|||||
| PDB ID: 2PVY Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic K659N Mutation Responsible for an Unclassified Craniosynostosis Syndrome. | ||||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | Yes | [2] |
| PDB Sequence |
ELPEDPKWEF
476 PRDKLTLGKP486 LQVVMAEAVG502 IDKDKPKEAV512 TVAVKMLKDD522 ATEKDLSDLV 532 SEMEMMKMIG542 KHKNIINLLG552 ACTQDGPLYV562 IVEYASKGNL572 REYLRARRPP 582 GMDINRVPEE596 QMTFKDLVSC606 TYQLARGMEY616 LASQKCIHRD626 LAARNVLVTE 636 NNVMKIADFG646 LARDINNIDY656 YKNTTNGRLP666 VKWMAPEALF676 DRVYTHQSDV 686 WSFGVLMWEI696 FTLGGSPYPG706 IPVEELFKLL716 KEGHRMDKPA726 NCTNELYMMM 736 RDCWHAVPSQ746 RPTFKQLVED756 LDRILTLT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:495 or .A:515 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:574 or .A:633; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| PDB ID: 2PY3 Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic E565G Mutation Responsible for Pfeiffer Syndrome | ||||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | Yes | [2] |
| PDB Sequence |
LPEDPKWEFP
477 RDKLTLGKPL487 FGQVVMAEAV501 GIDKDKPKEA511 VTVAVKMLKD521 DATEKDLSDL 531 VSEMEMMKMI541 GKHKNIINLL551 GACTQDGPLY561 VIVGYASKGN571 LREYLRARRP 581 EEQMTFKDLV604 SCTYQLARGM614 EYLASQKCIH624 RDLAARNVLV634 TENNVMKIAD 644 FGLARDINNI654 DYYKKTTNGR664 LPVKWMAPEA674 LFDRVYTHQS684 DVWSFGVLMW 694 EIFTLGGSPY704 PGIPVEELFK714 LLKEGHRMDK724 PANCTNELYM734 MMRDCWHAVP 744 SQRPTFKQLV754 EDLDRILTLT764 TN
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:492 or .A:493 or .A:494 or .A:495 or .A:515 or .A:517 or .A:534 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:626 or .A:630 or .A:631 or .A:633 or .A:644; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU487
3.644
PHE492
4.077
GLY493
3.765
GLN494
4.191
VAL495
3.620
ALA515
3.234
LYS517
2.653
GLU534
4.655
ILE548
4.197
VAL564
3.522
|
|||||
| PDB ID: 5UGX Crystal Structure of the Tyrosine Kinase Domain of FGF Receptor 2 Harboring a E565A/D650V double Gain-of-Function Mutation | ||||||
| Method | X-ray diffraction | Resolution | 2.35 Å | Mutation | Yes | [6] |
| PDB Sequence |
LPEDPKWEFP
477 RDKLTLGKPL487 GEGAFGQVVM497 AEAVGIDKDK507 PKEAVTVAVK517 MLKDDATEKD 527 LSDLVSEMEM537 MKMIGKHKNI547 INLLGACTQD557 GPLYVIVAYA567 SKGNLREYLR 577 ARRPPGMINR592 VPEEQMTFKD602 LVSCTYQLAR612 GMEYLASQKC622 IHRDLAARNV 632 LVTENNVMKI642 ADFGLARVTN662 GRLPVKWMAP672 EALFDRVYTH682 QSDVWSFGVL 692 MWEIFTLGGS702 PYPGIPVEEL712 FKLLKEGHRM722 DKPANCTNEL732 YMMMRDCWHA 742 VPSQRPTFKQ752 LVEDLDRILT762 LT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .B:487 or .B:488 or .B:489 or .B:490 or .B:491 or .B:492 or .B:493 or .B:495 or .B:515 or .B:517 or .B:534 or .B:548 or .B:564 or .B:565 or .B:566 or .B:567 or .B:570 or .B:571 or .B:630 or .B:631 or .B:633 or .B:644; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU487
3.811
GLY488
3.342
GLU489
4.292
GLY490
2.996
ALA491
2.572
PHE492
2.283
GLY493
3.101
VAL495
3.850
ALA515
3.243
LYS517
3.138
GLU534
4.817
|
|||||
| PDB ID: 4J95 Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic K659N Mutation Responsible for an Unclassified Craniosynostosis Syndrome in Space Group C2. | ||||||
| Method | X-ray diffraction | Resolution | 2.38 Å | Mutation | Yes | [5] |
| PDB Sequence |
ELPEDPKWEF
476 PRDKLTLGKP486 LGEGAFGQVV496 MAEAVGIDKD506 KPKEAVTVAV516 KMLKDDATEK 526 DLSDLVSEME536 MMKMIGKHKN546 IINLLGACTQ556 DGPLYVIVEY566 ASKGNLREYL 576 RARRPQMTFK601 DLVSCTYQLA611 RGMEYLASQK621 CIHRDLAARN631 VLVTENNVMK 641 IADFGLARDI651 YYKNTTNGRL665 PVKWMAPEAL675 FDRVYTHQSD685 VWSFGVLMWE 695 IFTLGGSPYP705 GIPVEELFKL715 LKEGHRMDKP725 ANCTNELYMM735 MRDCWHAVPS 745 QRPTFKQLVE755 DLDRILTLT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:488 or .A:489 or .A:490 or .A:491 or .A:495 or .A:515 or .A:517 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:630 or .A:631 or .A:633 or .A:644; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| PDB ID: 2PWL Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic N549H Mutation Responsible for Crouzon Syndrome. | ||||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [2] |
| PDB Sequence |
ELPEDPKWEF
476 PRDKLTLGKP486 LGEGAFGQVV496 MAEAVGIDKD506 KPKEAVTVAV516 KMLKDDATEK 526 DLSDLVSEME536 MMKMIGKHKN546 IIHLLGACTQ556 DGPLYVIVEY566 ASKGNLREYL 576 RARRPEQMTF600 KDLVSCTYQL610 ARGMEYLASQ620 KCIHRDLAAR630 NVLVTENNVM 640 KIADFGLARD650 INNIDYYKKT660 TNGRLPVKWM670 APEALFDRVY680 THQSDVWSFG 690 VLMWEIFTLG700 GSPYPGIPVE710 ELFKLLKEGH720 RMDKPANCTN730 ELYMMMRDCW 740 HAVPSQRPTF750 KQLVEDLDRI760 LTLT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:488 or .A:489 or .A:490 or .A:491 or .A:492 or .A:493 or .A:495 or .A:515 or .A:517 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:630 or .A:631 or .A:633 or .A:644; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU487
3.460
GLY488
3.165
GLU489
4.227
GLY490
3.207
ALA491
2.665
PHE492
4.846
GLY493
4.337
VAL495
3.423
ALA515
3.375
LYS517
3.618
ILE548
4.190
|
|||||
| PDB ID: 2PZ5 Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic N549T Mutation Responsible for Pfeiffer Syndrome | ||||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [2] |
| PDB Sequence |
LPEDPKWEFP
477 RDKLTLGKPL487 QVVMAEAVGI503 DKDKPKEAVT513 VAVKMLKDDA523 TEKDLSDLVS 533 EMEMMKMIGK543 HKNIITLLGA553 CTQDGPLYVI563 VEYASKGNLR573 EYLRARRPEE 596 QMTFKDLVSC606 TYQLARGMEY616 LASQKCIHRD626 LAARNVLVTE636 NNVMKIADFG 646 LARDINNIDY656 YKKTTNGRLP666 VKWMAPEALF676 DRVYTHQSDV686 WSFGVLMWEI 696 FTLGGSPYPG706 IPVEELFKLL716 KEGHRMDKPA726 NCTNELYMMM736 RDCWHAVPSQ 746 RPTFKQLVED756 LDRILTLTTN766
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:494 or .A:495 or .A:515 or .A:517 or .A:534 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:626 or .A:630 or .A:631 or .A:633 or .A:644; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| PDB ID: 2PZP Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic K526E Mutation Responsible for Crouzon Syndrome | ||||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [2] |
| PDB Sequence |
LPEDPKWEFP
477 RDKLTLGKPL487 QVVMAEAVGI503 DKDKPKEAVT513 VAVKMLKDDA523 TEEDLSDLVS 533 EMEMMKMIGK543 HKNIINLLGA553 CTQDGPLYVI563 VEYASKGNLR573 EYLRARRPEE 596 QMTFKDLVSC606 TYQLARGMEY616 LASQKCIHRD626 LAARNVLVTE636 NNVMKIADFG 646 LARDINNIDY656 YKKTTNGRLP666 VKWMAPEALF676 DRVYTHQSDV686 WSFGVLMWEI 696 FTLGGSPYPG706 IPVEELFKLL716 KEGHRMDKPA726 NCTNELYMMM736 RDCWHAVPSQ 746 RPTFKQLVED756 LDRILTLTTN766
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:494 or .A:495 or .A:515 or .A:517 or .A:534 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:630 or .A:631 or .A:633 or .A:644; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| PDB ID: 4J97 Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic Gain-of-Function K659E Mutation Identified in Endometrial Cancer. | ||||||
| Method | X-ray diffraction | Resolution | 2.55 Å | Mutation | Yes | [5] |
| PDB Sequence |
LPEDPKWEFP
477 RDKLTLGKPL487 GEGQVVMAEA500 VGIDKPKEAV512 TVAVKMLKDD522 ATEKDLSDLV 532 SEMEMMKMIG542 KHKNIINLLG552 ACTQDGPLYV562 IVEYASKGNL572 REYLRARRPP 582 GPEEQMTFKD602 LVSCTYQLAR612 GMEYLASQKC622 IHRDLAARNV632 LVTENNVMKI 642 ADFGLARDIN652 NIDYYKETTN662 GRLPVKWMAP672 EALFDRVYTH682 QSDVWSFGVL 692 MWEIFTLGGS702 PYPGIPVEEL712 FKLLKEGHRM722 DKPANCTNEL732 YMMMRDCWHA 742 VPSQRPTFKQ752 LVEDLDRILT762 LT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:488 or .A:489 or .A:493 or .A:495 or .A:515 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:574 or .A:633; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| PDB ID: 2Q0B Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic E565A Mutation Responsible for Pfeiffer Syndrome | ||||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | Yes | [2] |
| PDB Sequence |
LPEDPKWEFP
477 RDKLTLGKPL487 GQVVMAEAVG502 IDKDKPKEAV512 TVAVKMLKDD522 ATEKDLSDLV 532 SEMEMMKMIG542 KHKNIINLLG552 ACTQDGPLYV562 IVAYASKGNL572 REYLRARRPE 595 EQMTFKDLVS605 CTYQLARGME615 YLASQKCIHR625 DLAARNVLVT635 ENNVMKIADF 645 GLARDINNID655 YYKKTTNGRL665 PVKWMAPEAL675 FDRVYTHQSD685 VWSFGVLMWE 695 IFTLGGSPYP705 GIPVEELFKL715 LKEGHRMDKP725 ANCTNELYMM735 MRDCWHAVPS 745 QRPTFKQLVE755 DLDRILTLTT765
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:495 or .A:515 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:633; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| PDB ID: 5UHN Crystal Structure of the Tyrosine Kinase Domain of FGF Receptor 2 harboring a N549H/E565A Double Gain-of-Function Mutation | ||||||
| Method | X-ray diffraction | Resolution | 2.91 Å | Mutation | Yes | [6] |
| PDB Sequence |
PEDPKWEFPR
478 DKLTLGKPLG488 EGAFGQVVMA498 EAVGIDKDKP508 KEAVTVAVKM518 LKDDATEKDL 528 SDLVSEMEMM538 KMIGKHKNII548 HLLGACTQDG558 PLYVIVAYAS568 KGNLREYLRA 578 RREEQMTFKD602 LVSCTYQLAR612 GMEYLASQKC622 IHRDLAARNV632 LVTENNVMKI 642 ADFGLARDIN652 NIDYYKKTTN662 GRLPVKWMAP672 EALFDRVYTH682 QSDVWSFGVL 692 MWEIFTLGGS702 PYPGIPVEEL712 FKLLKEGHRM722 DKPANCTNEL732 YMMMRDCWHA 742 VPSQRPTFKQ752 LVEDLDRILT762 LT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:488 or .A:489 or .A:490 or .A:491 or .A:495 or .A:515 or .A:517 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:571 or .A:630 or .A:631 or .A:633 or .A:644; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| PDB ID: 2PZR Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic K641R Mutation Responsible for Pfeiffer Syndrome | ||||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | Yes | [2] |
| PDB Sequence |
LPEDPKWEFP
477 RDKLTLGKPL487 QVVMAEAVGI503 DKDKPKEAVT513 VAVKMLKDDA523 TEKDLSDLVS 533 EMEMMKMIGK543 HKNIINLLGA553 CTQDGPLYVI563 VEYASKGNLR573 EYLRARRPPE 595 EQMTFKDLVS605 CTYQLARGME615 YLASQKCIHR625 DLAARNVLVT635 ENNVMRIADF 645 GLARDINNID655 YYKKTTNGRL665 PVKWMAPEAL675 FDRVYTHQSD685 VWSFGVLMWE 695 IFTLGGSPYP705 GIPVEELFKL715 LKEGHRMDKP725 ANCTNELYMM735 MRDCWHAVPS 745 QRPTFKQLVE755 DLDRILTLTT765
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:487 or .A:495 or .A:515 or .A:548 or .A:564 or .A:565 or .A:566 or .A:567 or .A:570 or .A:633; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Crystal Structure of Monophosphorylated FGF Receptor 2 isoform IIIb with PTR657 | ||||
| REF 2 | A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases. Mol Cell. 2007 Sep 7;27(5):717-30. | ||||
| REF 3 | A crystallographic snapshot of tyrosine trans-phosphorylation in action. Proc Natl Acad Sci U S A. 2008 Dec 16;105(50):19660-5. | ||||
| REF 4 | Two FGF Receptor Kinase Molecules Act in Concert to Recruit and Transphosphorylate Phospholipase CGamma. Mol Cell. 2016 Jan 7;61(1):98-110. | ||||
| REF 5 | Cracking the molecular origin of intrinsic tyrosine kinase activity through analysis of pathogenic gain-of-function mutations. Cell Rep. 2013 Jul 25;4(2):376-84. | ||||
| REF 6 | Elucidation of a four-site allosteric network in fibroblast growth factor receptor tyrosine kinases. Elife. 2017 Feb 6;6:e21137. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.