Drug Information

Drug (ID: DG01910) and It's Reported Resistant Information
Name
BI-2536
Synonyms
BI2536
    Click to Show/Hide
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
Brain cancer [ICD-11: 2A00]
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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: Serine/threonine-protein kinase B-raf (BRAF) [1]
Sensitive Disease FGFR-tacc positive glioblastoma [ICD-11: 2A00.01]
 Disease Info 
Molecule Alteration Missense mutation
p.V600E (c.1799T>A)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.55  Å
PDB: 4E26
Mutant Type Structure Method: X-ray diffraction Resolution: 3.20  Å
PDB: 4G9R
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.53
TM score: 0.95765
Amino acid change:
V600E
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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420
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M
M
D
D
R
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G
G
S
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H
H
H
H
H
H
H
H
H
H
430
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H
H
G
G
S
S
E
E
D
D
R
R
N
N
R
R
M
M
K
K
440
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T
T
L
L
G
G
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R
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D
D
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D
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D
D
450
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W
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E
E
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D
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460
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G
G
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I
I
G
G
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G
G
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F
F
G
G
470
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Y
Y
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G
D
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480
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A
A
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N
V
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A
A
490
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P
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P
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L
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A
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F
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500
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E
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L
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R
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510
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H
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N
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M
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Y
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520
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L
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530
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C
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E
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540
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550
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560
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570
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580
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D
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590
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V
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G
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F
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G
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L
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600
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V
E
K
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W
W
S
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S
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610
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F
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L
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G
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620
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630
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Y
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640
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Y
Y
A
A
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F
G
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L
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650
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M
M
T
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G
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Y
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N
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660
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N
N
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670
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680
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A
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690
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700
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710
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I
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L
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A
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I
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E
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L
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720
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S
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Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
In Vitro Model GBM cells Brain Homo sapiens (Human) N.A.
In Vivo Model Athymic mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 qPCR
Experiment for
Drug Resistance		 Alamar blue proliferation assay
References
Ref 1 Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating CellsCancer Res. 2015 Dec 15;75(24):5355-66. doi: 10.1158/0008-5472.CAN-14-3689. Epub 2015 Nov 16.

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