Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T86350 | Target Info | |||
| Target Name | Erbb3 tyrosine kinase receptor (Erbb-3) | ||||
| Synonyms | Tyrosine kinase-type cell surface receptor HER3; Receptor tyrosine-protein kinase erbB-3; Proto-oncogene-like protein c-ErbB-3; HER3; C-erbB3; C-erbB-3 protein | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | ERBB3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Bosutinib | Ligand Info | |||||
| Structure Description | HER3 pseudokinase domain bound to bosutinib | PDB:6OP9 | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [1] |
| PDB Sequence |
VLARIFKETE
689 LRKLKVLGSG699 VFGTVHKGVW709 IPEGESIKIP719 VCIKVIEDKS729 GRQSFQAVTD 739 HMLAIGSLDH749 AHIVRLLGLC759 PGSSLQLVTQ769 YLPLGSLLDH779 VRQHRGALGP 789 QLLLNWGVQI799 AKGMYYLEEH809 GMVHRNLAAR819 NVLLKSPSQV829 QVADFGVADL 839 LPPDDKQAKT854 PIKWMALESI864 HFGKYTHQSD874 VWSYGVTVWE884 LMTFGAEPYA 894 GLRLAEVPDL904 LEKGERLAQP914 QICTIDVYMV924 MVKCWMIDEN934 IRPTFKELAN 944 EFTRMARDPP954 RYLVIK
|
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|
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LEU696
3.423
GLY697
4.357
VAL704
3.958
CYS721
3.154
ILE722
3.729
LYS723
3.371
VAL753
3.288
LEU766
3.375
VAL767
4.429
THR768
3.023
GLN769
3.518
|
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| Ligand Name: AMP-PNP | Ligand Info | |||||
| Structure Description | Crystal structure of the catalytically inactive kinase domain of the human epidermal growth factor receptor 3 (HER3) | PDB:3KEX | ||||
| Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | No | [2] |
| PDB Sequence |
KVLARIFKET
688 ELRKLKVLGS698 GVFGTVHKGV708 WIPEGESIKI718 PVCIKVIEDK728 SGRQSFQAVT 738 DHMLAIGSLD748 HAHIVRLLGL758 CPGSSLQLVT768 QYLPLGSLLD778 HVRQHRGALG 788 PQLLLNWGVQ798 IAKGMYYLEE808 HGMVHRNLAA818 RNVLLKSPSQ828 VQVADFGVAD 838 LLPPDDKQLL848 TPIKWMALES863 IHFGKYTHQS873 DVWSYGVTVW883 ELMTFGAEPY 893 AGLRLAEVPD903 LLEKGERLAQ913 PQICTIDVYM923 VMVKCWMIDE933 NIRPTFKELA 943 NEFTRMARDP953 PRYLVIKRES963 GPGIAPGPEP973 HG
|
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|
|
LEU696
3.380
GLY697
3.065
SER698
2.898
GLY699
2.888
VAL700
3.035
PHE701
4.817
GLY702
3.614
VAL704
3.085
CYS721
3.563
LYS723
3.484
VAL753
4.334
THR768
3.897
|
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Targetable HER3 functions driving tumorigenic signaling in HER2-amplified cancers. Cell Rep. 2022 Feb 1;38(5):110291. | ||||
| REF 2 | Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3. Proc Natl Acad Sci U S A. 2009 Dec 22;106(51):21608-13. | ||||
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