Drug (ID: DG01894) and It's Reported Resistant Information
Name
IDH2 inhibitors
Synonyms
IDH2 inhibitors
    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
Acute myeloid leukemia [ICD-11: 2A60]
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: Isocitrate dehydrogenase NADP 2 (IDH2) [1]
Sensitive Disease Acute myeloid leukemia [ICD-11: 2A60.0]
Molecule Alteration Missense mutation
p.R172K (c.515G>A)
Wild Type Structure Method: X-ray diffraction Resolution: 1.93  Å
PDB: 5GIS
Mutant Type Structure Method: X-ray diffraction Resolution: 2.10  Å
PDB: 5SVN
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.13
TM score: 0.29352
Amino acid change:
R172K
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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Experimental Note Identified from the Human Clinical Data
Key Molecule: Isocitrate dehydrogenase NADP 2 (IDH2) [1]
Sensitive Disease Acute myeloid leukemia [ICD-11: 2A60.0]
Molecule Alteration Missense mutation
p.R140Q (c.419G>A)
Wild Type Structure Method: X-ray diffraction Resolution: 2.10  Å
PDB: 5SVN
Mutant Type Structure Method: X-ray diffraction Resolution: 1.54  Å
PDB: 5I95
   Download The Information of Sequence       Download The Structure File   
RMSD: 0.33
TM score: 0.99798
Amino acid change:
R140Q
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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H
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Experimental Note Identified from the Human Clinical Data
References
Ref 1 Abstract CT103: Clinical safety and efficacy of pembrolizumab (MK-3475) in patients with malignant pleural mesothelioma: Preliminary results from KEYNOTE-0280.

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