Drug Information

Drug (ID: DG01895) and It's Reported Resistant Information
Name
ERBB2 TKIs
Synonyms
ERBB2 TKIs
    Click to Show/Hide
Type(s) of Resistant Mechanism of This Drug
  ADTT: Aberration of the Drug's Therapeutic Target
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Click to Show/Hide the Resistance Disease of This Class
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.S310F (c.929C>T)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 3.09  Å
PDB: 3WLW
Mutant Type Structure Method: Electron microscopy Resolution: 3.09  Å
PDB: 7MN6
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.33
TM score: 0.96205
Amino acid change:
S310F
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
T
M
Q
E
V
L
C
A
T
A
G
L
T
C
D
R
M
W
10
|
K
G
L
L
R
L
L
L
P
A
A
L
S
L
P
P
E
P
T
G
20
|
H
A
L
A
D
S
M
T
L
Q
R
V
H
C
L
T
Y
G
Q
T
30
|
G
D
C
M
Q
K
V
L
V
R
Q
L
G
P
N
A
L
S
E
P
40
|
L
E
T
T
Y
H
L
L
P
D
T
M
N
L
A
R
S
H
L
L
50
|
S
Y
F
Q
L
G
Q
C
D
Q
I
V
Q
V
E
Q
V
G
Q
N
60
|
G
L
Y
E
V
L
L
T
I
Y
A
L
H
P
N
T
Q
N
V
A
70
|
R
S
Q
L
V
S
P
F
L
L
Q
Q
R
D
L
I
R
Q
I
E
80
|
V
V
R
Q
G
G
T
Y
Q
V
L
L
F
I
E
A
D
H
N
N
90
|
Y
Q
A
V
L
R
A
Q
V
V
L
P
D
L
N
Q
G
R
D
L
100
|
P
R
L
I
N
V
N
R
T
G
T
T
P
Q
V
L
T
F
G
E
110
|
A
D
S
N
P
Y
G
A
G
L
L
A
R
V
E
L
L
D
Q
N
120
|
L
G
R
D
S
P
L
L
T
N
E
N
I
T
L
T
K
P
G
V
130
|
G
T
V
G
L
A
I
S
Q
P
R
G
N
G
P
L
Q
R
L
E
140
|
C
L
Y
Q
Q
L
D
R
T
S
I
L
L
T
W
E
K
I
D
L
150
|
I
K
F
G
H
G
K
V
N
L
N
I
Q
Q
L
R
A
N
L
P
160
|
T
Q
L
L
I
C
D
Y
T
Q
N
D
R
T
S
I
R
L
A
W
170
|
C
K
H
D
P
I
C
F
S
H
P
K
M
N
C
N
K
Q
G
L
180
|
S
A
R
L
C
T
W
L
G
I
E
D
S
T
S
N
E
R
D
S
190
|
C
R
Q
A
S
C
L
H
T
P
R
C
T
S
V
P
C
M
A
C
200
|
G
K
G
G
C
S
A
R
R
C
C
W
K
G
G
E
P
S
L
S
210
|
P
E
T
D
D
C
C
Q
C
S
H
L
E
T
Q
R
C
T
A
V
220
|
A
C
G
A
C
G
T
G
G
C
P
A
K
R
H
C
S
K
D
G
230
|
C
P
L
L
A
P
C
T
L
D
H
C
F
C
N
H
H
E
S
Q
240
|
G
C
I
A
C
A
E
G
L
C
H
T
C
G
P
P
A
K
L
H
250
|
V
S
T
D
Y
C
N
L
T
A
D
C
T
L
F
H
E
F
S
N
260
|
M
H
P
S
N
G
P
I
E
C
G
E
R
L
Y
H
T
C
F
P
270
|
G
A
A
L
S
V
C
T
V
Y
T
N
A
T
C
D
P
T
Y
F
280
|
N
E
Y
S
L
M
S
P
T
N
D
P
V
E
G
G
S
R
C
Y
290
|
T
T
L
F
V
G
C
A
P
S
L
C
H
V
N
T
Q
A
E
C
300
|
V
P
T
Y
A
N
E
Y
D
L
G
S
T
T
Q
D
R
V
C
G
310
|
E
F
K
C
C
T
S
L
K
V
P
C
C
P
A
L
R
H
V
N
320
|
C
Q
Y
E
G
V
L
T
G
A
M
E
E
D
H
G
L
T
R
Q
330
|
E
R
V
C
R
E
A
K
V
C
T
S
S
K
A
P
N
C
I
A
340
|
Q
R
E
V
F
C
A
Y
G
G
C
L
K
G
K
M
I
E
F
H
350
|
G
L
S
R
L
E
A
V
F
R
L
A
P
V
E
T
S
S
F
A
360
|
D
N
G
I
D
Q
P
E
A
F
S
A
N
G
T
C
A
K
P
K
370
|
L
I
Q
F
P
G
E
S
Q
L
L
A
Q
F
V
L
F
P
E
E
380
|
T
S
L
F
E
D
E
G
I
D
T
P
G
A
Y
S
L
N
Y
T
390
|
I
A
S
P
A
L
W
Q
P
P
D
E
S
Q
L
L
P
Q
D
V
400
|
L
F
S
E
V
T
F
L
Q
E
N
E
L
I
Q
T
V
G
I
Y
410
|
R
L
G
Y
R
I
I
S
L
A
H
W
N
P
G
D
A
S
Y
L
420
|
S
P
L
D
T
L
L
S
Q
V
G
F
L
Q
G
N
I
L
S
Q
430
|
W
V
L
I
G
R
L
G
R
R
S
I
L
L
R
H
E
N
L
G
440
|
G
A
S
Y
G
S
L
L
A
T
L
L
I
Q
H
G
H
L
N
G
450
|
T
I
H
S
L
W
C
L
F
G
V
L
H
R
T
S
V
L
P
R
460
|
W
E
D
L
Q
G
L
S
F
G
R
L
N
A
P
L
H
I
Q
H
470
|
A
H
L
N
L
T
H
H
T
L
A
C
N
F
R
V
P
H
E
T
480
|
D
V
E
P
C
W
V
D
G
Q
E
L
G
F
L
R
A
N
C
P
490
|
H
H
Q
Q
L
A
C
L
A
L
R
H
G
T
H
A
C
N
W
R
500
|
G
P
P
E
G
D
P
E
T
C
Q
V
C
G
V
E
N
G
C
L
510
|
S
A
Q
C
F
H
L
Q
R
L
G
C
Q
A
E
R
C
G
V
H
520
|
E
C
E
W
C
G
R
P
V
G
L
P
Q
T
G
Q
L
C
P
V
530
|
R
N
E
C
Y
S
V
Q
N
F
A
L
R
R
H
G
C
Q
L
E
540
|
P
C
C
V
H
E
P
E
E
C
C
R
Q
V
P
L
Q
Q
N
G
550
|
G
L
S
P
V
R
T
E
C
Y
F
V
G
N
P
A
E
R
A
H
560
|
D
C
Q
L
C
P
V
C
A
H
-
P
-
E
-
C
-
Q
-
P
570
|
-
Q
-
N
-
G
-
S
-
V
-
T
-
C
-
F
-
G
-
P
580
|
-
E
-
A
-
D
-
Q
-
C
-
V
-
A
-
C
-
A
-
H
590
|
-
Y
-
K
-
D
-
P
-
P
-
F
-
C
-
V
-
A
-
R
600
|
-
C
-
P
-
S
-
G
-
V
-
K
-
P
-
D
-
L
-
S
610
|
-
Y
-
M
-
P
-
I
-
W
-
K
-
F
-
P
-
D
-
E
620
|
-
E
-
G
-
A
-
C
-
Q
-
P
-
C
-
P
-
I
-
N
630
|
-
C
-
T
-
H
-
S
-
C
-
V
-
D
-
L
-
D
-
D
640
|
-
K
-
G
-
C
-
P
-
A
-
E
-
Q
-
R
-
A
-
S
650
|
-
P
-
L
-
T
-
S
-
I
-
I
-
S
-
A
-
V
-
V
660
|
-
G
-
I
-
L
-
L
-
V
-
V
-
V
-
L
-
G
-
V
670
|
-
V
-
F
-
G
-
I
-
L
-
I
-
K
-
R
-
R
-
Q
680
|
-
Q
-
K
-
I
-
R
-
K
-
Y
-
T
-
M
-
R
-
R
690
|
-
L
-
L
-
Q
-
E
-
T
-
E
-
L
-
V
-
E
-
P
700
|
-
L
-
T
-
P
-
S
-
G
-
A
-
M
-
P
-
N
-
Q
710
|
-
A
-
Q
-
M
-
R
-
I
-
L
-
K
-
E
-
T
-
E
720
|
-
L
-
R
-
K
-
V
-
K
-
V
-
L
-
G
-
S
-
G
730
|
-
A
-
F
-
G
-
T
-
V
-
Y
-
K
-
G
-
I
-
W
740
|
-
I
-
P
-
D
-
G
-
E
-
N
-
V
-
K
-
I
-
P
750
|
-
V
-
A
-
I
-
K
-
V
-
L
-
R
-
E
-
N
-
T
760
|
-
S
-
P
-
K
-
A
-
N
-
K
-
E
-
I
-
L
-
D
770
|
-
E
-
A
-
Y
-
V
-
M
-
A
-
G
-
V
-
D
-
S
780
|
-
P
-
Y
-
V
-
S
-
R
-
L
-
L
-
G
-
I
-
C
790
|
-
L
-
T
-
S
-
T
-
V
-
Q
-
L
-
V
-
T
-
Q
800
|
-
L
-
M
-
P
-
Y
-
G
-
C
-
L
-
L
-
D
-
H
810
|
-
V
-
R
-
E
-
N
-
R
-
G
-
R
-
L
-
G
-
S
820
|
-
Q
-
D
-
L
-
L
-
N
-
W
-
C
-
M
-
Q
-
I
830
|
-
A
-
K
-
G
-
M
-
S
-
Y
-
L
-
E
-
D
-
V
840
|
-
R
-
L
-
V
-
H
-
R
-
D
-
L
-
A
-
A
-
R
850
|
-
N
-
V
-
L
-
V
-
K
-
S
-
P
-
N
-
H
-
V
860
|
-
K
-
I
-
T
-
D
-
F
-
G
-
L
-
A
-
R
-
L
870
|
-
L
-
D
-
I
-
D
-
E
-
T
-
E
-
Y
-
H
-
A
880
|
-
D
-
G
-
G
-
K
-
V
-
P
-
I
-
K
-
W
-
M
890
|
-
A
-
L
-
E
-
S
-
I
-
L
-
R
-
R
-
R
-
F
900
|
-
T
-
H
-
Q
-
S
-
D
-
V
-
W
-
S
-
Y
-
G
910
|
-
V
-
T
-
V
-
W
-
E
-
L
-
M
-
T
-
F
-
G
920
|
-
A
-
K
-
P
-
Y
-
D
-
G
-
I
-
P
-
A
-
R
930
|
-
E
-
I
-
P
-
D
-
L
-
L
-
E
-
K
-
G
-
E
940
|
-
R
-
L
-
P
-
Q
-
P
-
P
-
I
-
C
-
T
-
I
950
|
-
D
-
V
-
Y
-
M
-
I
-
M
-
V
-
K
-
C
-
W
960
|
-
M
-
I
-
D
-
S
-
E
-
C
-
R
-
P
-
R
-
F
970
|
-
R
-
E
-
L
-
V
-
S
-
E
-
F
-
S
-
R
-
M
980
|
-
A
-
R
-
D
-
P
-
Q
-
R
-
F
-
V
-
V
-
I
990
|
-
Q
-
N
-
E
-
D
-
L
-
G
-
P
-
A
-
S
-
P
1000
|
-
L
-
D
-
S
-
T
-
F
-
Y
-
R
-
S
-
L
-
L
1010
|
-
E
-
D
-
D
-
D
-
M
-
G
-
D
-
L
-
V
-
D
1020
|
-
A
-
E
-
E
-
Y
-
L
-
V
-
P
-
Q
-
Q
-
G
1030
|
-
G
-
G
-
S
-
L
-
E
-
V
-
L
-
F
-
Q
-
G
1040
|
-
P
-
S
-
S
-
P
-
S
-
G
-
S
-
S
-
M
-
K
1050
|
-
I
-
E
-
E
-
G
-
K
-
L
-
V
-
I
-
W
-
I
1060
|
-
N
-
G
-
D
-
K
-
G
-
Y
-
N
-
G
-
L
-
A
1070
|
-
E
-
V
-
G
-
K
-
K
-
F
-
E
-
K
-
D
-
T
1080
|
-
G
-
I
-
K
-
V
-
T
-
V
-
E
-
H
-
P
-
D
1090
|
-
K
-
L
-
E
-
E
-
K
-
F
-
P
-
Q
-
V
-
A
1100
|
-
A
-
T
-
G
-
D
-
G
-
P
-
D
-
I
-
I
-
F
1110
|
-
W
-
A
-
H
-
D
-
R
-
F
-
G
-
G
-
Y
-
A
1120
|
-
Q
-
S
-
G
-
L
-
L
-
A
-
E
-
I
-
T
-
P
1130
|
-
D
-
K
-
A
-
F
-
Q
-
D
-
K
-
L
-
Y
-
P
1140
|
-
F
-
T
-
W
-
D
-
A
-
V
-
R
-
Y
-
N
-
G
1150
|
-
K
-
L
-
I
-
A
-
Y
-
P
-
I
-
A
-
V
-
E
1160
|
-
A
-
L
-
S
-
L
-
I
-
Y
-
N
-
K
-
D
-
L
1170
|
-
L
-
P
-
N
-
P
-
P
-
K
-
T
-
W
-
E
-
E
1180
|
-
I
-
P
-
A
-
L
-
D
-
K
-
E
-
L
-
K
-
A
1190
|
-
K
-
G
-
K
-
S
-
A
-
L
-
M
-
F
-
N
-
L
1200
|
-
Q
-
E
-
P
-
Y
-
F
-
T
-
W
-
P
-
L
-
I
1210
|
-
A
-
A
-
D
-
G
-
G
-
Y
-
A
-
F
-
K
-
Y
1220
|
-
E
-
N
-
G
-
K
-
Y
-
D
-
I
-
K
-
D
-
V
1230
|
-
G
-
V
-
D
-
N
-
A
-
G
-
A
-
K
-
A
-
G
1240
|
-
L
-
T
-
F
-
L
-
V
-
D
-
L
-
I
-
K
-
N
1250
|
-
K
-
H
-
M
-
N
-
A
-
D
-
T
-
D
-
Y
-
S
1260
|
-
I
-
A
-
E
-
A
-
A
-
F
-
N
-
K
-
G
-
E
1270
|
-
T
-
A
-
M
-
T
-
I
-
N
-
G
-
P
-
W
-
A
1280
|
-
W
-
S
-
N
-
I
-
D
-
T
-
S
-
K
-
V
-
N
1290
|
-
Y
-
G
-
V
-
T
-
V
-
L
-
P
-
T
-
F
-
K
1300
|
-
G
-
Q
-
P
-
S
-
K
-
P
-
F
-
V
-
G
-
V
1310
|
-
L
-
S
-
A
-
G
-
I
-
N
-
A
-
A
-
S
-
P
1320
|
-
N
-
K
-
E
-
L
-
A
-
K
-
E
-
F
-
L
-
E
1330
|
-
N
-
Y
-
L
-
L
-
T
-
D
-
E
-
G
-
L
-
E
1340
|
-
A
-
V
-
N
-
K
-
D
-
K
-
P
-
L
-
G
-
A
1350
|
-
V
-
A
-
L
-
K
-
S
-
Y
-
E
-
E
-
E
-
L
1360
|
-
A
-
K
-
D
-
P
-
R
-
I
-
A
-
A
-
T
-
M
1370
|
-
E
-
N
-
A
-
Q
-
K
-
G
-
E
-
I
-
M
-
P
1380
|
-
N
-
I
-
P
-
Q
-
M
-
S
-
A
-
F
-
W
-
Y
1390
|
-
A
-
V
-
R
-
T
-
A
-
V
-
I
-
N
-
A
-
A
1400
|
-
S
-
G
-
R
-
Q
-
T
-
V
-
D
-
E
-
A
-
L
1410
|
-
K
-
D
-
A
-
Q
-
T
-
N
-
S
-
S
-
S
-
S
1420
|
-
G
-
P
-
S
-
S
-
P
-
S
-
A
-
W
-
S
-
H
1430
|
-
P
-
Q
-
F
-
E
-
K
-
G
-
G
-
G
-
S
-
G
1440
|
-
G
-
G
-
S
-
G
-
G
-
S
-
S
-
A
-
W
-
S
1450
|
-
H
-
P
-
Q
-
F
-
E
-
K
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.S310F (c.929C>T) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.G309E (c.926G>A)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.G309E (c.926G>A) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.S310Y (c.929C>A)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.S310Y (c.929C>A) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.C311R (c.931T>C)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.C311R (c.931T>C) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.E321G (c.962A>G)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.E321G (c.962A>G) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
References
Ref 1 Functional analysis of receptor tyrosine kinase mutations in lung cancer identifies oncogenic extracellular domain mutations of ERBB2Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14476-81. doi: 10.1073/pnas.1203201109. Epub 2012 Aug 20.

If you find any error in data or bug in web service, please kindly report it to Dr. Sun and Dr. Yu.