Drug Information

Drug (ID: DG01864) and It's Reported Resistant Information
Name
PI3K pathway inhibitors
Synonyms
PI3K pathway inhibitors
    Click to Show/Hide
Drug Resistance Disease(s)
Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
Breast cancer [ICD-11: 2C60]
[1]
Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
Breast cancer [ICD-11: 2C60]
[2]
Type(s) of Resistant Mechanism of This Drug due to Structure Alteration
  UAPP: Unusual Activation of Pro-survival Pathway
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
Head and neck cancer [ICD-11: 2D42]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: RAC-alpha serine/threonine-protein kinase (AKT1) [3]
Sensitive Disease Head and neck cancer [ICD-11: 2D42.0]
 Disease 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
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0
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-
S
M
M
S
S
D
D
V
V
A
A
I
I
V
V
K
K
E
E
10
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G
G
W
W
L
L
H
H
K
K
R
R
G
G
E
K
Y
Y
I
I
20
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K
K
T
T
W
W
R
R
P
P
R
R
Y
Y
F
F
L
L
L
L
30
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K
K
N
N
D
D
G
G
T
T
F
F
I
I
G
G
Y
Y
K
K
40
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E
E
R
R
P
P
Q
Q
D
D
V
V
D
D
Q
Q
R
R
E
E
50
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A
A
P
P
L
L
N
N
N
N
F
F
S
S
V
V
A
A
Q
Q
60
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C
C
Q
Q
L
L
M
M
K
K
T
T
E
E
R
R
P
P
R
R
70
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P
P
N
N
T
T
F
F
I
I
I
I
R
R
C
C
L
L
Q
Q
80
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W
W
T
T
T
T
V
V
I
I
E
E
R
R
T
T
F
F
H
H
90
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V
V
E
E
T
T
P
P
E
E
E
E
R
R
E
E
E
E
W
W
100
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T
T
T
T
A
A
I
I
Q
Q
T
T
V
V
A
A
D
D
G
G
110
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L
L
K
K
K
K
Q
Q
E
E
E
E
E
E
E
E
M
M
D
D
120
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F
F
R
R
-
S
-
G
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
Mechanism Description The missense mutation p.E17K (c.49G>A) in gene AKT1 cause the sensitivity of PI3K pathway inhibitors by aberration of the drug's therapeutic target
References
Ref 1 Acquired PIK3CA amplification causes resistance to selective phosphoinositide 3-kinase inhibitors in breast cancerOncogenesis. 2013 Dec 23;2(12):e83. doi: 10.1038/oncsis.2013.46.
Ref 2 Activating Mutations in PIK3CB Confer Resistance to PI3K Inhibition and Define a Novel Oncogenic Role for p110BetaCancer Res. 2016 Mar 1;76(5):1193-203. doi: 10.1158/0008-5472.CAN-15-2201. Epub 2016 Jan 12.
Ref 3 Incorporation of Next-Generation Sequencing into Routine Clinical Care to Direct Treatment of Head and Neck Squamous Cell CarcinomaClin Cancer Res. 2016 Jun 15;22(12):2939-49. doi: 10.1158/1078-0432.CCR-15-2314. Epub 2016 Jan 13.

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