Drug Information

Drug (ID: DG01887) and It's Reported Resistant Information
Name
Hormone therapy
Synonyms
Hormone therapy
    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]
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
Breast cancer [ICD-11: 2C60]
Click to Show/Hide
Drug Resistance Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Estrogen receptor alpha (ESR1) [1]
Resistant Disease Breast adenocarcinoma [ICD-11: 2C60.1]
 Disease Info 
Molecule Alteration Missense mutation
p.Y537S (c.1610A>C)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 1.60  Å
PDB: 2IOG
Mutant Type Structure Method: X-ray diffraction Resolution: 1.50  Å
PDB: 5DXE
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.7
TM score: 0.91757
Amino acid change:
Y537S
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
-
M
-
D
-
P
-
M
-
I
-
K
300
|
-
R
-
S
-
K
-
K
-
N
-
S
-
L
-
A
-
L
S
S
310
|
L
L
T
T
A
A
D
D
Q
Q
M
M
V
V
S
S
A
A
L
L
320
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L
L
D
D
A
A
E
E
P
P
P
P
I
I
L
L
Y
Y
S
S
330
|
E
E
Y
Y
D
D
P
P
T
T
R
R
P
P
F
F
S
S
E
E
340
|
A
A
S
S
M
M
M
M
G
G
L
L
L
L
T
T
N
N
L
L
350
|
A
A
D
D
R
R
E
E
L
L
V
V
H
H
M
M
I
I
N
N
360
|
W
W
A
A
K
K
R
R
V
V
P
P
G
G
F
F
V
V
D
D
370
|
L
L
T
T
L
L
H
H
D
D
Q
Q
V
V
H
H
L
L
L
L
380
|
E
E
C
-
A
A
W
W
L
L
E
E
I
I
L
L
M
M
I
I
390
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G
G
L
L
V
V
W
W
R
R
S
S
M
M
E
E
H
H
P
P
400
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G
G
K
K
L
L
L
L
F
F
A
A
P
P
N
N
L
L
L
L
410
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L
L
D
D
R
R
N
N
Q
Q
G
G
K
K
C
-
V
V
E
E
420
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G
G
M
M
V
V
E
E
I
I
F
F
D
D
M
M
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L
L
430
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A
A
T
T
S
S
S
S
R
R
F
F
R
R
M
M
M
M
N
N
440
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L
L
Q
Q
G
G
E
E
E
E
F
F
V
V
C
C
L
L
K
K
450
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S
S
I
I
I
I
L
L
L
L
N
N
S
S
G
G
V
V
Y
Y
460
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T
T
F
F
L
L
S
S
S
S
T
T
L
L
K
K
S
S
L
L
470
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E
E
E
E
K
K
D
D
H
H
I
I
H
H
R
R
V
V
L
L
480
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D
D
K
K
I
I
T
T
D
D
T
T
L
L
I
I
H
H
L
L
490
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M
M
A
A
K
K
A
A
G
G
L
L
T
T
L
L
Q
Q
Q
Q
500
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Q
Q
H
H
Q
Q
R
R
L
L
A
A
Q
Q
L
L
L
L
L
L
510
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I
I
L
L
S
S
H
H
I
I
R
R
H
H
M
M
S
S
N
N
520
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K
K
G
G
M
M
E
E
H
H
L
L
Y
Y
S
S
M
M
K
K
530
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C
-
K
K
N
N
V
V
V
V
P
P
L
L
Y
S
D
D
L
L
540
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L
L
L
L
E
E
M
M
L
L
D
D
A
A
H
H
R
R
L
L
550
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H
H
A
A
P
P
T
T
S
S
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
In Vitro Model MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
ZR75-1 cells Breast Homo sapiens (Human) CVCL_0588
MDA-MB-361 cells Breast Homo sapiens (Human) CVCL_0620
MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
SkBR3 MCF7 cells Breast Homo sapiens (Human) N.A.
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
Ishikawa cells Endometrium Homo sapiens (Human) CVCL_2529
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
In Vivo Model Nu/Nu athymic BALB/c female mouse model Mus musculus
Experiment for
Molecule Alteration		 IMPACT assay; Western blot analysis; Luciferase assays; Microarrays assay
Experiment for
Drug Resistance		 MSKCC assay
Key Molecule: Estrogen receptor alpha (ESR1) [1]
Resistant Disease Breast adenocarcinoma [ICD-11: 2C60.1]
 Disease Info 
Molecule Alteration Missense mutation
p.D538G (c.1613A>G)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 1.60  Å
PDB: 2IOG
Mutant Type Structure Method: X-ray diffraction Resolution: 1.90  Å
PDB: 4PXM
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.86
TM score: 0.90649
Amino acid change:
D538G
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
-
V
-
D
-
L
-
G
-
T
-
E
290
|
-
N
-
L
-
Y
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F
-
Q
-
S
-
N
-
A
-
M
-
K
300
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-
R
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S
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K
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K
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N
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S
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L
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A
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L
S
S
310
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L
L
T
T
A
A
D
D
Q
Q
M
M
V
V
S
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A
A
L
L
320
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L
L
D
D
A
A
E
E
P
P
P
P
I
I
L
L
Y
Y
S
S
330
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E
E
Y
Y
D
D
P
P
T
T
R
R
P
P
F
F
S
S
E
E
340
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A
A
S
S
M
M
M
M
G
G
L
L
L
L
T
T
N
N
L
L
350
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A
A
D
D
R
R
E
E
L
L
V
V
H
H
M
M
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I
N
N
360
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W
W
A
A
K
K
R
R
V
V
P
P
G
G
F
F
V
V
D
D
370
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L
L
T
T
L
L
H
H
D
D
Q
Q
V
V
H
H
L
L
L
L
380
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E
E
C
C
A
A
W
W
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L
E
E
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I
L
L
M
M
I
I
390
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G
G
L
L
V
V
W
W
R
R
S
S
M
M
E
E
H
H
P
P
400
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G
G
K
K
L
L
L
L
F
F
A
A
P
P
N
N
L
L
L
L
410
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L
L
D
D
R
R
N
N
Q
Q
G
G
K
K
C
C
V
V
E
E
420
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G
G
M
M
V
V
E
E
I
I
F
F
D
D
M
M
L
L
L
L
430
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A
A
T
T
S
S
S
S
R
R
F
F
R
R
M
M
M
M
N
N
440
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L
L
Q
Q
G
G
E
E
E
E
F
F
V
V
C
C
L
L
K
K
450
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S
S
I
I
I
I
L
L
L
L
N
N
S
S
G
G
V
V
Y
Y
460
|
T
T
F
F
L
L
S
S
S
S
T
T
L
L
K
K
S
S
L
L
470
|
E
E
E
E
K
K
D
D
H
H
I
I
H
H
R
R
V
V
L
L
480
|
D
D
K
K
I
I
T
T
D
D
T
T
L
L
I
I
H
H
L
L
490
|
M
M
A
A
K
K
A
A
G
G
L
L
T
T
L
L
Q
Q
Q
Q
500
|
Q
Q
H
H
Q
Q
R
R
L
L
A
A
Q
Q
L
L
L
L
L
L
510
|
I
I
L
L
S
S
H
H
I
I
R
R
H
H
M
M
S
S
N
N
520
|
K
K
G
G
M
M
E
E
H
H
L
L
Y
Y
S
S
M
M
K
K
530
|
C
C
K
K
N
N
V
V
V
V
P
P
L
L
Y
Y
D
G
L
L
540
|
L
L
L
L
E
E
M
M
L
L
D
D
A
A
H
H
R
R
L
L
550
|
H
H
A
A
P
P
T
T
S
S
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
In Vitro Model MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
ZR75-1 cells Breast Homo sapiens (Human) CVCL_0588
MDA-MB-361 cells Breast Homo sapiens (Human) CVCL_0620
MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
SkBR3 MCF7 cells Breast Homo sapiens (Human) N.A.
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
Ishikawa cells Endometrium Homo sapiens (Human) CVCL_2529
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
In Vivo Model Nu/Nu athymic BALB/c female mouse model Mus musculus
Experiment for
Molecule Alteration		 IMPACT assay; Western blot analysis; Luciferase assays; Microarrays assay
Experiment for
Drug Resistance		 MSKCC assay
Key Molecule: Estrogen receptor alpha (ESR1) [1]
Resistant Disease Breast adenocarcinoma [ICD-11: 2C60.1]
 Disease Info 
Molecule Alteration Missense mutation
p.L536Q (c.1607_1608delTCinsAA)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
ZR75-1 cells Breast Homo sapiens (Human) CVCL_0588
MDA-MB-361 cells Breast Homo sapiens (Human) CVCL_0620
MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
SkBR3 MCF7 cells Breast Homo sapiens (Human) N.A.
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
Ishikawa cells Endometrium Homo sapiens (Human) CVCL_2529
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
In Vivo Model Nu/Nu athymic BALB/c female mouse model Mus musculus
Experiment for
Molecule Alteration		 IMPACT assay; Western blot analysis; Luciferase assays; Microarrays assay
Experiment for
Drug Resistance		 MSKCC assay
Key Molecule: Estrogen receptor alpha (ESR1) [1]
Resistant Disease Breast adenocarcinoma [ICD-11: 2C60.1]
 Disease Info 
Molecule Alteration Missense mutation
p.Y537N (c.1609T>A)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
ZR75-1 cells Breast Homo sapiens (Human) CVCL_0588
MDA-MB-361 cells Breast Homo sapiens (Human) CVCL_0620
MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
SkBR3 MCF7 cells Breast Homo sapiens (Human) N.A.
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
Ishikawa cells Endometrium Homo sapiens (Human) CVCL_2529
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
In Vivo Model Nu/Nu athymic BALB/c female mouse model Mus musculus
Experiment for
Molecule Alteration		 IMPACT assay; Western blot analysis; Luciferase assays; Microarrays assay
Experiment for
Drug Resistance		 MSKCC assay
Key Molecule: Estrogen receptor alpha (ESR1) [1]
Resistant Disease Breast adenocarcinoma [ICD-11: 2C60.1]
 Disease Info 
Molecule Alteration Missense mutation
p.Y537C (c.1610A>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
ZR75-1 cells Breast Homo sapiens (Human) CVCL_0588
MDA-MB-361 cells Breast Homo sapiens (Human) CVCL_0620
MDA-MB-231cells Breast Homo sapiens (Human) CVCL_0062
SkBR3 MCF7 cells Breast Homo sapiens (Human) N.A.
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
Ishikawa cells Endometrium Homo sapiens (Human) CVCL_2529
MCF Tet-On cells Pleural effusion Homo sapiens (Human) CVCL_V332
In Vivo Model Nu/Nu athymic BALB/c female mouse model Mus musculus
Experiment for
Molecule Alteration		 IMPACT assay; Western blot analysis; Luciferase assays; Microarrays assay
Experiment for
Drug Resistance		 MSKCC assay
References
Ref 1 ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nat Genet. 2013 Dec;45(12):1439-45. doi: 10.1038/ng.2822. Epub 2013 Nov 3.

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