Drug Information

Drug (ID: DG01750) and It's Reported Resistant Information
Name
Alpelisib/Cetuximab/Encorafenib
Synonyms
Alpelisib/Cetuximab/Encorafenib
    Click to Show/Hide
Type(s) of Resistant Mechanism of This Drug
  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
Colorectal cancer [ICD-11: 2B91]
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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 Colorectal cancer [ICD-11: 2B91.1]
 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
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G
G
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H
H
H
430
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H
H
G
G
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E
E
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D
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N
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M
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440
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450
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460
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470
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T
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480
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L
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A
A
490
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500
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510
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520
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530
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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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590
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600
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610
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620
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630
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640
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650
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660
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670
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680
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690
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700
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710
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720
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Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
Cell Pathway Regulation MAPK signaling pathway Inhibition hsa04010
In Vitro Model WiDR cells Colon Homo sapiens (Human) CVCL_2760
VACO432 cells Colon Homo sapiens (Human) CVCL_5402
HROC87 cells Colon Homo sapiens (Human) CVCL_S854
Experiment for
Molecule Alteration		 SDS-PAGE assay; Western blot analysis; chemiluminescent detection assay
Experiment for
Drug Resistance		 CellTiter-Glo luminescent assay; CellTox green assay
Mechanism Description Resistant cells escaped drug treatments through one or more mechanisms leading to biochemical reactivation of the MAPK signaling pathway.
References
Ref 1 Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal CancerCancer Res. 2016 Aug 1;76(15):4504-15. doi: 10.1158/0008-5472.CAN-16-0396. Epub 2016 Jun 16.

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