Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T39797 Target Info
Target Name Frizzled-7 receptor (FZD7)
Synonyms hFz7; FzE3; Fz7; Fz-7; Frizzled7; Frizzled-7
Target Type Clinical trial Target
Gene Name FZD7
Biochemical Class GPCR frizzled
UniProt ID
FZD7_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: 4,5,-IP2 Ligand Info
Structure Description Crystal structure of the syntenin PDZ1 and PDZ2 tandem in complex with the Frizzled 7 C-terminal fragment and PIP2 PDB:4Z33
Method X-ray diffraction Resolution 2.45 Å Mutation No [1]
PDB Sequence
KGETAV
Residue
Distance (Å)
LYS1
3.400
Residue
Distance (Å)
Ligand Name: Nervonic acid Ligand Info
Structure Description Crystal structure of Frizzled 7 CRD in complex with C24 fatty acid PDB:5URV
Method X-ray diffraction Resolution 2.20 Å Mutation No [2]
PDB Sequence
HGFCQPISIP
25
LCTDIAYNQT
35
ILPNLLGHTN
45
QEDAGLEVHQ
55
FYPLVKVQCS
65

PELRFFLCSM
75
YAPVCTVLDQ
85
AIPPCRSLCE
95
RARQGCEALM
105
NKFGFQWPER
115

LRCENFPVHG
125
AGEICVGQ
Residue
Distance (Å)
GLU52
3.641
GLN55
3.590
PHE56
3.345
TYR57
4.964
PRO58
3.558
LEU59
3.707
Residue
Distance (Å)
LYS61
3.884
TYR76
4.123
MET105
3.652
PHE108
3.970
PHE110
3.670
PRO113
3.799
Ligand Name: 3-Cyclohexyl-1-propylsulfonic acid Ligand Info
Structure Description Crystal structure of Frizzled 7 CRD in complex with F7.B Fab PDB:6O3A
Method X-ray diffraction Resolution 2.10 Å Mutation No [3]
PDB Sequence
FCQPISIPLC
57
TDIAYNQTIL
67
PNLLGHTNQE
77
DAGLEVHQFY
87
PLVKVQCSPE
97

LRFFLCSMYA
107
PVCTVLDQAI
117
PPCRSLCERA
127
RQGCEALMNK
137
FGFQWPERLR
147

CENFPVHGAG
157
EICVGQNT
Click to Show 3D Structure of This Binding Site
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Residue
Distance (Å)
GLN85
3.386
PHE86
3.479
MET135
3.554
Residue
Distance (Å)
PHE140
3.857
GLN141
3.910
PRO143
3.737
References  Top
REF 1 Crystal structure of the syntenin PDZ1 and PDZ2 tandem in complex with the Frizzled 7 C-terminal fragment and PIP2
REF 2 Unsaturated fatty acyl recognition by Frizzled receptors mediates dimerization upon Wnt ligand binding. Proc Natl Acad Sci U S A. 2017 Apr 18;114(16):4147-4152.
REF 3 Structure-guided design fine-tunes pharmacokinetics, tolerability, and antitumor profile of multispecific frizzled antibodies. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):6812-6817.

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