Disease Information

General Information of the Disease (ID: DIS00372)
Name
Anal canal cancer
ICD
ICD-11: 2C00
Type(s) of Resistant Mechanism of This Disease
  ADTT: Aberration of the Drug's Therapeutic Target
Drug Resistance Data Categorized by Drug
Clinical Trial Drug(s)
1 drug(s) in total
Click to Show/Hide the Full List of Drugs
BAY1125976
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: RAC-alpha serine/threonine-protein kinase (AKT1) [1]
Sensitive Disease Anal canal cancer [ICD-11: 2C00.0]
Sensitive Drug BAY1125976
 Drug Info 
Molecule Alteration Missense mutation
p.E17K (c.49G>A)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 1.65  Å
PDB: 1UNP
Mutant Type Structure Method: X-ray diffraction Resolution: 1.94  Å
PDB: 2UZR
   Download The Information of Sequence       Download The Structure File   
RMSD: 0.26
TM score: 0.99569
Amino acid change:
E17K
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
0
|
-
S
M
M
S
S
D
D
V
V
A
A
I
I
V
V
K
K
E
E
10
|
G
G
W
W
L
L
H
H
K
K
R
R
G
G
E
K
Y
Y
I
I
20
|
K
K
T
T
W
W
R
R
P
P
R
R
Y
Y
F
F
L
L
L
L
30
|
K
K
N
N
D
D
G
G
T
T
F
F
I
I
G
G
Y
Y
K
K
40
|
E
E
R
R
P
P
Q
Q
D
D
V
V
D
D
Q
Q
R
R
E
E
50
|
A
A
P
P
L
L
N
N
N
N
F
F
S
S
V
V
A
A
Q
Q
60
|
C
C
Q
Q
L
L
M
M
K
K
T
T
E
E
R
R
P
P
R
R
70
|
P
P
N
N
T
T
F
F
I
I
I
I
R
R
C
C
L
L
Q
Q
80
|
W
W
T
T
T
T
V
V
I
I
E
E
R
R
T
T
F
F
H
H
90
|
V
V
E
E
T
T
P
P
E
E
E
E
R
R
E
E
E
E
W
W
100
|
T
T
T
T
A
A
I
I
Q
Q
T
T
V
V
A
A
D
D
G
G
110
|
L
L
K
K
K
K
Q
Q
E
E
E
E
E
E
E
E
M
M
D
D
120
|
F
F
R
R
-
S
-
G
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model LNCaP cells Prostate Homo sapiens (Human) CVCL_0395
MDA-MB-231 cells Breast Homo sapiens (Human) CVCL_0062
Hela cells Cervix uteri Homo sapiens (Human) CVCL_0030
NCI-H460 cells Lung Homo sapiens (Human) CVCL_0459
MDA-MB-453 cells Breast Homo sapiens (Human) CVCL_0418
MDA-MB-468 cells Breast Homo sapiens (Human) CVCL_0419
HCC70 cells Breast Homo sapiens (Human) CVCL_1270
A2058 cells Skin Homo sapiens (Human) CVCL_1059
Caco2 cells Colon Homo sapiens (Human) CVCL_0025
MCF-7 cells Breast Homo sapiens (Human) CVCL_0031
ZR75-1 cells Breast Homo sapiens (Human) CVCL_0588
DU-145 cells Prostate Homo sapiens (Human) CVCL_0105
NCI-60 cells N.A. Homo sapiens (Human) N.A.
EVSA-T cells Ascites Homo sapiens (Human) CVCL_1207
KU-19 cells Blood Bos taurus (Bovine) CVCL_VN09
T47D cells Pleural effusion Homo sapiens (Human) CVCL_0553
CAL-120 cells Pleural effusion Homo sapiens (Human) CVCL_1104
BT-549 cells Breast Homo sapiens (Human) CVCL_1092
BT-474 cells Breast Homo sapiens (Human) CVCL_0179
BT-20 cells Mammary gland Homo sapiens (Human) CVCL_0178
B16F10 cells Skin Mus musculus (Mouse) CVCL_0159
In Vivo Model Female NMRI (nu/nu) mouse xenograft model Mus musculus
Mechanism Description The missense mutation p.E17K (c.49G>A) in gene AKT1 cause the sensitivity of BAY1125976 by aberration of the drug's therapeutic target
References
Ref 1 BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse modelsInt J Cancer. 2017 Jan 15;140(2):449-459. doi: 10.1002/ijc.30457. Epub 2016 Oct 20.

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