Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTRMGQNU)

• DOT Name: Axin-2 (AXIN2)
• Synonyms: Axin-like protein; Axil; Axis inhibition protein 2; Conductin
• Gene Name: AXIN2
• Related Disease:
  Adult glioblastoma
  Glioblastoma multiforme
  Glioma
  Oligodontia-cancer predisposition syndrome
  Adenoma
  Advanced cancer
  Bone osteosarcoma
  Breast carcinoma
  Breast neoplasm
  Carcinoma
  Carcinoma of esophagus
  Carcinoma of liver and intrahepatic biliary tract
  Clear cell renal carcinoma
  Colon carcinoma
  Colonic neoplasm
  Colorectal neoplasm
  Ectodermal dysplasia
  Esophageal cancer
  Gastric neoplasm
  Hepatocellular carcinoma
  Intestinal neoplasm
  Liver cancer
  Melanoma
  Neoplasm
  Neoplasm of esophagus
  Osteosarcoma
  Prostate cancer
  Prostate carcinoma
  Renal cell carcinoma
  Cleft palate
  Isolated cleft palate
  Lung cancer
  Lung carcinoma
  Metastatic malignant neoplasm
  Triple negative breast cancer
  Tooth agenesis
  Colon cancer
  Craniosynostosis
  Dilated cardiomyopathy
  Dilated cardiomyopathy 1A
  Endometrial carcinoma
  Epithelial ovarian cancer
  Gastric cancer
  Myocardial ischemia
  Neuroblastoma
  Ovarian cancer
  Ovarian neoplasm
  Parkinson disease
  Tooth agenesis, selective, 1
• UniProt ID: AXIN2_HUMAN
• PDB ID: 8HEO
• Pfam ID: PF16646 ; PF08833 ; PF00778 ; PF00615
• Sequence:
  MSSAMLVTCLPDPSSSFREDAPRPPVPGEEGETPPCQPGVGKGQVTKPMPVSSNTRRNED
  GLGEPEGRASPDSPLTRWTKSLHSLLGDQDGAYLFRTFLEREKCVDTLDFWFACNGFRQM
  NLKDTKTLRVAKAIYKRYIENNSIVSKQLKPATKTYIRDGIKKQQIDSIMFDQAQTEIQS
  VMEENAYQMFLTSDIYLEYVRSGGENTAYMSNGGLGSLKVVCGYLPTLNEEEEWTCADFK
  CKLSPTVVGLSSKTLRATASVRSTETVDSGYRSFKRSDPVNPYHIGSGYVFAPATSANDS
  EISSDALTDDSMSMTDSSVDGIPPYRVGSKKQLQREMHRSVKANGQVSLPHFPRTHRLPK
  EMTPVEPATFAAELISRLEKLKLELESRHSLEERLQQIREDEEREGSELTLNSREGAPTQ
  HPLSLLPSGSYEEDPQTILDDHLSRVLKTPGCQSPGVGRYSPRSRSPDHHHHHHSQYHSL
  LPPGGKLPPAAASPGACPLLGGKGFVTKQTTKHVHHHYIHHHAVPKTKEEIEAEATQRVH
  CFCPGGSEYYCYSKCKSHSKAPETMPSEQFGGSRGSTLPKRNGKGTEPGLALPAREGGAP
  GGAGALQLPREEGDRSQDVWQWMLESERQSKPKPHSAQSTKKAYPLESARSSPGERASRH
  HLWGGNSGHPRTTPRAHLFTQDPAMPPLTPPNTLAQLEEACRRLAEVSKPPKQRCCVASQ
  QRDRNHSATVQTGATPFSNPSLAPEDHKEPKKLAGVHALQASELVVTYFFCGEEIPYRRM
  LKAQSLTLGHFKEQLSKKGNYRYYFKKASDEFACGAVFEEIWEDETVLPMYEGRILGKVE
  RID
• Function: Inhibitor of the Wnt signaling pathway. Down-regulates beta-catenin. Probably facilitate the phosphorylation of beta-catenin and APC by GSK3B.
• Tissue Specificity: Expressed in brain and lymphoblast.
• KEGG Pathway:
  Wnt sig.ling pathway (hsa04310)
  Hippo sig.ling pathway (hsa04390)
  Sig.ling pathways regulating pluripotency of stem cells (hsa04550)
  Cushing syndrome (hsa04934)
  Alzheimer disease (hsa05010)
  Pathways of neurodegeneration - multiple diseases (hsa05022)
  Human papillomavirus infection (hsa05165)
  Pathways in cancer (hsa05200)
  Colorectal cancer (hsa05210)
  Endometrial cancer (hsa05213)
  Basal cell carcinoma (hsa05217)
  Breast cancer (hsa05224)
  Hepatocellular carcinoma (hsa05225)
  Gastric cancer (hsa05226)
• Reactome Pathway:
  Binding of TCF/LEF (R-HSA-4411364)
  Degradation of AXIN (R-HSA-4641257)
  Ub-specific processing proteases (R-HSA-5689880)
  TCF dependent signaling in response to WNT (R-HSA-201681)

Molecular Interaction Atlas (MIA) of This DOT

49 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Adult glioblastoma	DISVP4LU	Definitive	Altered Expression	[1]
Glioblastoma multiforme	DISK8246	Definitive	Altered Expression	[1]
Glioma	DIS5RPEH	Definitive	Biomarker	[2]
Oligodontia-cancer predisposition syndrome	DIS0ZOJU	Definitive	Autosomal dominant	[3]
Adenoma	DIS78ZEV	Strong	Posttranslational Modification	[4]
Advanced cancer	DISAT1Z9	Strong	Genetic Variation	[5]
Bone osteosarcoma	DIST1004	Strong	Biomarker	[6]
Breast carcinoma	DIS2UE88	Strong	Biomarker	[7]
Breast neoplasm	DISNGJLM	Strong	Biomarker	[8]
Carcinoma	DISH9F1N	Strong	Posttranslational Modification	[4]
Carcinoma of esophagus	DISS6G4D	Strong	Biomarker	[9]
Carcinoma of liver and intrahepatic biliary tract	DIS8WA0W	Strong	Biomarker	[10]
Clear cell renal carcinoma	DISBXRFJ	Strong	Altered Expression	[11]
Colon carcinoma	DISJYKUO	Strong	Biomarker	[12]
Colonic neoplasm	DISSZ04P	Strong	Genetic Variation	[13]
Colorectal neoplasm	DISR1UCN	Strong	Posttranslational Modification	[14]
Ectodermal dysplasia	DISLRS4M	Strong	Genetic Variation	[15]
Esophageal cancer	DISGB2VN	Strong	Biomarker	[9]
Gastric neoplasm	DISOKN4Y	Strong	Genetic Variation	[16]
Hepatocellular carcinoma	DIS0J828	Strong	Altered Expression	[17]
Intestinal neoplasm	DISK0GUH	Strong	Altered Expression	[18]
Liver cancer	DISDE4BI	Strong	Biomarker	[10]
Melanoma	DIS1RRCY	Strong	Genetic Variation	[19]
Neoplasm	DISZKGEW	Strong	Altered Expression	[20]
Neoplasm of esophagus	DISOLKAQ	Strong	Biomarker	[9]
Osteosarcoma	DISLQ7E2	Strong	Biomarker	[6]
Prostate cancer	DISF190Y	Strong	Altered Expression	[21]
Prostate carcinoma	DISMJPLE	Strong	Altered Expression	[21]
Renal cell carcinoma	DISQZ2X8	Strong	Altered Expression	[11]
Cleft palate	DIS6G5TF	moderate	Altered Expression	[22]
Isolated cleft palate	DISV80CD	moderate	Altered Expression	[22]
Lung cancer	DISCM4YA	moderate	Altered Expression	[21]
Lung carcinoma	DISTR26C	moderate	Altered Expression	[21]
Metastatic malignant neoplasm	DIS86UK6	moderate	Altered Expression	[23]
Triple negative breast cancer	DISAMG6N	moderate	Biomarker	[24]
Tooth agenesis	DIS1PWC7	Supportive	Autosomal dominant	[25]
Colon cancer	DISVC52G	Limited	Biomarker	[12]
Craniosynostosis	DIS6J405	Limited	Autosomal dominant	[26]
Dilated cardiomyopathy	DISX608J	Limited	Biomarker	[27]
Dilated cardiomyopathy 1A	DIS0RK9Z	Limited	Biomarker	[27]
Endometrial carcinoma	DISXR5CY	Limited	Biomarker	[28]
Epithelial ovarian cancer	DIS56MH2	Limited	Genetic Variation	[29]
Gastric cancer	DISXGOUK	Limited	Genetic Variation	[30]
Myocardial ischemia	DISFTVXF	Limited	Biomarker	[27]
Neuroblastoma	DISVZBI4	Limited	Altered Expression	[31]
Ovarian cancer	DISZJHAP	Limited	Genetic Variation	[29]
Ovarian neoplasm	DISEAFTY	Limited	Genetic Variation	[29]
Parkinson disease	DISQVHKL	Limited	Biomarker	[32]
Tooth agenesis, selective, 1	DIS84ERL	Limited	Biomarker	[33]

23 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the expression of Axin-2 (AXIN2).	[34]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate increases the expression of Axin-2 (AXIN2).	[35]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Axin-2 (AXIN2).	[36]
Quercetin	DM3NC4M	Approved	Quercetin decreases the expression of Axin-2 (AXIN2).	[37]
Temozolomide	DMKECZD	Approved	Temozolomide increases the expression of Axin-2 (AXIN2).	[38]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Axin-2 (AXIN2).	[39]
Vorinostat	DMWMPD4	Approved	Vorinostat increases the expression of Axin-2 (AXIN2).	[40]
Carbamazepine	DMZOLBI	Approved	Carbamazepine affects the expression of Axin-2 (AXIN2).	[41]
Panobinostat	DM58WKG	Approved	Panobinostat increases the expression of Axin-2 (AXIN2).	[40]
Niclosamide	DMJAGXQ	Approved	Niclosamide decreases the expression of Axin-2 (AXIN2).	[42]
Diethylstilbestrol	DMN3UXQ	Approved	Diethylstilbestrol decreases the expression of Axin-2 (AXIN2).	[43]
Gemcitabine	DMSE3I7	Approved	Gemcitabine affects the expression of Axin-2 (AXIN2).	[44]
Mifepristone	DMGZQEF	Approved	Mifepristone increases the expression of Axin-2 (AXIN2).	[45]
Resveratrol	DM3RWXL	Phase 3	Resveratrol decreases the expression of Axin-2 (AXIN2).	[46]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of Axin-2 (AXIN2).	[47]
LY294002	DMY1AFS	Phase 1	LY294002 decreases the expression of Axin-2 (AXIN2).	[38]
Calphostin C	DM9X2D0	Terminated	Calphostin C affects the expression of Axin-2 (AXIN2).	[49]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A increases the expression of Axin-2 (AXIN2).	[51]
Lithium chloride	DMHYLQ2	Investigative	Lithium chloride increases the expression of Axin-2 (AXIN2).	[52]
Okadaic acid	DM47CO1	Investigative	Okadaic acid increases the expression of Axin-2 (AXIN2).	[53]
CH-223191	DMMJZYC	Investigative	CH-223191 decreases the expression of Axin-2 (AXIN2).	[54]
Bilirubin	DMI0V4O	Investigative	Bilirubin decreases the expression of Axin-2 (AXIN2).	[55]
Paraoxon	DMN4ZKC	Investigative	Paraoxon decreases the expression of Axin-2 (AXIN2).	[56]

2 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 affects the phosphorylation of Axin-2 (AXIN2).	[48]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the methylation of Axin-2 (AXIN2).	[50]

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