Drug (ID: DG00212) and It's Reported Resistant Information
Name
Genistein
Synonyms
Bonistein; GEN; Genestein; Genisteol; Genisterin; Prunetol; Sophoricol; Differenol A; G 6649; G10000; IN1327; NPI 031L; STO514; TNP00151; GENISTEIN (ENDOCRINE DISRUPTER); Lactoferrin-genistein; PTI G4660 (Genistein); PTI-G4660; SIPI 807-1; C.I. 75610; SIPI-9764-I; ENDOCRINE DISRUPTOR (GENISTEIN) (SEE ALSO GENISTEIN (446-72-0)); 4 inverted exclamation marka,5,7-Trihydroxyisoflavone; ,5,7-Trihydroxyisoflavone; 4',5, 7-Trihydroxyisoflavone; 4',5,7-Trihydroxy isoflavone; 4',5,7-Trihydroxyisoflavone; 4,5,7-Trihydroxyiso-flavone; 4,6,7-Trihydroxyisoflavone; 5,7,4'-Trihydroxyisoflavone; 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4-benzopyrone; 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one; 5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one; 5,7-dihydroxy-3-(4-hydroxyphenyl)chromen-4-one
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Indication
In total 2 Indication(s)
Menopausal disorder [ICD-11: GA30]
Phase 2/3
[1]
Prostate cancer [ICD-11: 2C82]
Phase 2
[1]
Structure
Target Estrogen receptor beta (ESR2) ESR2_HUMAN [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
C15H10O5
IsoSMILES
C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
InChI
1S/C15H10O5/c16-9-3-1-8(2-4-9)11-7-20-13-6-10(17)5-12(18)14(13)15(11)19/h1-7,16-18H
InChIKey
TZBJGXHYKVUXJN-UHFFFAOYSA-N
PubChem CID
5280961
ChEBI ID
CHEBI:28088
TTD Drug ID
D0L4FS
VARIDT ID
DR00641
INTEDE ID
DR0768
DrugBank ID
DB01645
Type(s) of Resistant Mechanism of This Drug
  EADR: Epigenetic Alteration of DNA, RNA or Protein
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
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Prostate cancer [ICD-11: 2C82]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Epigenetic Alteration of DNA, RNA or Protein (EADR) Click to Show/Hide
Key Molecule: HOX transcript antisense RNA (HOTAIR) [1]
Molecule Alteration Expression
Down-regulation
Sensitive Disease Prostate cancer [ICD-11: 2C82.0]
Experimental Note Revealed Based on the Cell Line Data
Cell Pathway Regulation Cell apoptosis Activation hsa04210
Cell migration Inhibition hsa04670
Cell proliferation Inhibition hsa05200
In Vitro Model DU-145 cells Prostate Homo sapiens (Human) CVCL_0105
LNCaP cells Prostate Homo sapiens (Human) CVCL_0395
PC3 cells Prostate Homo sapiens (Human) CVCL_0035
RWPE-1 cells Prostate Homo sapiens (Human) CVCL_3791
In Vivo Model Nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration
qRT-PCR
Experiment for
Drug Resistance
MTS assay
Mechanism Description Knockdown (siRNA) of HOTAIR decreased PCa cell proliferation, migration and invasion and induced apoptosis and cell cycle arrest. miR-34a was also up-regulated by genistein and may directly target HOTAIR in both PC3 and DU145 PCa cells.
Key Molecule: hsa-mir-34 [1]
Molecule Alteration Expression
Up-regulation
Sensitive Disease Prostate cancer [ICD-11: 2C82.0]
Experimental Note Revealed Based on the Cell Line Data
Cell Pathway Regulation Cell apoptosis Activation hsa04210
Cell migration Inhibition hsa04670
Cell proliferation Inhibition hsa05200
In Vitro Model DU-145 cells Prostate Homo sapiens (Human) CVCL_0105
LNCaP cells Prostate Homo sapiens (Human) CVCL_0395
PC3 cells Prostate Homo sapiens (Human) CVCL_0035
RWPE-1 cells Prostate Homo sapiens (Human) CVCL_3791
In Vivo Model Nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration
Dual-luciferase reporter assays
Experiment for
Drug Resistance
MTS assay
Mechanism Description Knockdown (siRNA) of HOTAIR decreased PCa cell proliferation, migration and invasion and induced apoptosis and cell cycle arrest. miR-34a was also up-regulated by genistein and may directly target HOTAIR in both PC3 and DU145 PCa cells.
References
Ref 1 Genistein inhibits prostate cancer cell growth by targeting miR-34a and oncogenic HOTAIR. PLoS One. 2013 Aug 1;8(8):e70372. doi: 10.1371/journal.pone.0070372. Print 2013.

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