Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTU6ZA26)

• DOT Name: Protein GREB1 (GREB1)
• Synonyms: Gene regulated in breast cancer 1 protein
• Gene Name: GREB1
• Related Disease:
  Prostate cancer
  Advanced cancer
  Bladder cancer
  Breast neoplasm
  Carcinoma
  Castration-resistant prostate carcinoma
  Endometrial cancer
  Endometrial carcinoma
  Epithelial ovarian cancer
  High blood pressure
  Hyperlipidemia
  Lung cancer
  Lung carcinoma
  Neoplasm
  Non-small-cell lung cancer
  Ovarian cancer
  Ovarian neoplasm
  Prostate carcinoma
  Prostate neoplasm
  Urinary bladder cancer
  Urinary bladder neoplasm
  Uterine fibroids
  Asthma
  Invasive breast carcinoma
• UniProt ID: GREB1_HUMAN
• Pfam ID: PF20692 ; PF20688 ; PF20267 ; PF15782 ; PF20691
• Sequence:
  MGNSYAGQLKTTRFEEVLHNSIEASLRSNNLVPRPIFSQLYLEAEQQLAALEGGSRVDNE
  EEEEEGEGGLETNGPPNPFQLHPLPEGCCTTDGFCQAGKDLRLVSISNEPMDVPAGFLLV
  GVKSPSLPDHLLVCAVDKRFLPDDNGHNALLGFSGNCVGCGKKGFCYFTEFSNHINLKLT
  TQPKKQKHLKYYLVRNAQGTLTKGPLICWKGSEFRSRQIPASTCSSSLFPALESTAAFPS
  EPVPGTNPSILMGAQQAGPASDHPSLNAAMGPAVFNGKDSPKCQQLAKNNLLALPRPSAL
  GILSNSGPPKKRHKGWSPESPSAPDGGCPQGGGNRAKYESAGMSCVPQVGLVGPASVTFP
  VVASGEPVSVPDNLLKICKAKPVIFKGHGNFPYLCGNLNDVVVSPLLYTCYQNSQSVSRA
  YEQYGASAIQPISEEMQLLLTVYYLVQLAADQVPLMEDLEQIFLRSWRESHLTEIRQYQQ
  APPQPFPPAPSAAAPVTSAQLPWLASLAASSCNDSVHVIECAYSLAEGLSEMFRLLVEGK
  LAKTNYVVIICACRSAAIDSCIAVTGKYQARILSESLLTPAEYQKEVNYELVTGKVDSLG
  AFFSTLCPEGDIDILLDKFHQENQGHISSSLAASSVTKAASLDVSGTPVCTSYNLEPHSI
  RPFQLAVAQKLLSHVCSIADSSTQNLDLGSFEKVDFLICIPPSEVTYQQTLLHVWHSGVL
  LELGLKKEHMTKQRVEQYVLKLDTEAQTKFKAFLQNSFQNPHTLFVLIHDHAHWDLVSST
  VHNLYSQSDPSVGLVDRLLNCREVKEAPNIVTLHVTSFPYALQTQHTLISPYNEIHWPAS
  CSNGVDLYHENKKYFGLSEFIESTLSGHSLPLLRYDSSFEAMVTALGKRFPRLHSAVIRT
  FVLVQHYAAALMAVSGLPQMKNYTSVETLEITQNLLNSPKQCPCGHGLMVLLRVPCSPLA
  VVAYERLAHVRARLALEEHFEIILGSPSSGVTVGKHFVKQLRMWQKIEDVEWRPQTYLEL
  EGLPCILIFSGMDPHGESLPRSLRYCDLRLINSSCLVRTALEQELGLAAYFVSNEVPLEK
  GARNEALESDAEKLSSTDNEDEELGTEGSTSEKRSPMKRERSRSHDSASSSLSSKASGSA
  LGGESSAQPTALPQGEHARSPQPRGPAEEGRAPGEKQRPRASQGPPSAISRHSPGPTPQP
  DCSLRTGQRSVQVSVTSSCSQLSSSSGSSSSSVAPAAGTWVLQASQCSLTKACRQPPIVF
  LPKLVYDMVVSTDSSGLPKAASLLPSPSVMWASSFRPLLSKTMTSTEQSLYYRQWTVPRP
  SHMDYGNRAEGRVDGFHPRRLLLSGPPQIGKTGAYLQFLSVLSRMLVRLTEVDVYDEEEI
  NINLREESDWHYLQLSDPWPDLELFKKLPFDYIIHDPKYEDASLICSHYQGIKSEDRGMS
  RKPEDLYVRRQTARMRLSKYAAYNTYHHCEQCHQYMGFHPRYQLYESTLHAFAFSYSMLG
  EEIQLHFIIPKSKEHHFVFSQPGGQLESMRLPLVTDKSHEYIKSPTFTPTTGRHEHGLFN
  LYHAMDGASHLHVLVVKEYEMAIYKKYWPNHIMLVLPSIFNSAGVGAAHFLIKELSYHNL
  ELERNRQEELGIKPQDIWPFIVISDDSCVMWNVVDVNSAGERSREFSWSERNVSLKHIMQ
  HIEAAPDIMHYALLGLRKWSSKTRASEVQEPFSRCHVHNFIILNVDLTQNVQYNQNRFLC
  DDVDFNLRVHSAGLLLCRFNRFSVMKKQIVVGGHRSFHITSKVSDNSAAVVPAQYICAPD
  SKHTFLAAPAQLLLEKFLQHHSHLFFPLSLKNHDHPVLSVDCYLNLGSQISVCYVSSRPH
  SLNISCSDLLFSGLLLYLCDSFVGASFLKKFHFLKGATLCVICQDRSSLRQTVVRLELED
  EWQFRLRDEFQTANAREDRPLFFLTGRHI
• Function: May play a role in estrogen-stimulated cell proliferation. Acts as a regulator of hormone-dependent cancer growth in breast and prostate cancers.
• Tissue Specificity: Expressed in proliferating prostatic tissue and prostate cancer.
• KEGG Pathway: Estrogen sig.ling pathway (hsa04915)
• Reactome Pathway: Estrogen-dependent gene expression (R-HSA-9018519)

Molecular Interaction Atlas (MIA) of This DOT

24 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Prostate cancer	DISF190Y	Definitive	Biomarker	[1]
Advanced cancer	DISAT1Z9	Strong	Altered Expression	[2]
Bladder cancer	DISUHNM0	Strong	Altered Expression	[3]
Breast neoplasm	DISNGJLM	Strong	Biomarker	[4]
Carcinoma	DISH9F1N	Strong	Altered Expression	[5]
Castration-resistant prostate carcinoma	DISVGAE6	Strong	Altered Expression	[6]
Endometrial cancer	DISW0LMR	Strong	Biomarker	[7]
Endometrial carcinoma	DISXR5CY	Strong	Altered Expression	[7]
Epithelial ovarian cancer	DIS56MH2	Strong	Biomarker	[5]
High blood pressure	DISY2OHH	Strong	Biomarker	[8]
Hyperlipidemia	DIS61J3S	Strong	Genetic Variation	[8]
Lung cancer	DISCM4YA	Strong	Biomarker	[9]
Lung carcinoma	DISTR26C	Strong	Biomarker	[9]
Neoplasm	DISZKGEW	Strong	Altered Expression	[10]
Non-small-cell lung cancer	DIS5Y6R9	Strong	Biomarker	[11]
Ovarian cancer	DISZJHAP	Strong	Biomarker	[5]
Ovarian neoplasm	DISEAFTY	Strong	Biomarker	[5]
Prostate carcinoma	DISMJPLE	Strong	Biomarker	[1]
Prostate neoplasm	DISHDKGQ	Strong	Biomarker	[6]
Urinary bladder cancer	DISDV4T7	Strong	Altered Expression	[3]
Urinary bladder neoplasm	DIS7HACE	Strong	Altered Expression	[3]
Uterine fibroids	DISBZRMJ	Strong	Genetic Variation	[12]
Asthma	DISW9QNS	Limited	Genetic Variation	[13]
Invasive breast carcinoma	DISANYTW	Limited	Altered Expression	[14]

52 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 Protein GREB1 (GREB1).	[15]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Protein GREB1 (GREB1).	[16]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Protein GREB1 (GREB1).	[17]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Protein GREB1 (GREB1).	[18]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Protein GREB1 (GREB1).	[19]
Cisplatin	DMRHGI9	Approved	Cisplatin increases the expression of Protein GREB1 (GREB1).	[20]
Estradiol	DMUNTE3	Approved	Estradiol increases the expression of Protein GREB1 (GREB1).	[21]
Ivermectin	DMDBX5F	Approved	Ivermectin increases the expression of Protein GREB1 (GREB1).	[22]
Arsenic	DMTL2Y1	Approved	Arsenic decreases the expression of Protein GREB1 (GREB1).	[23]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide increases the expression of Protein GREB1 (GREB1).	[24]
Calcitriol	DM8ZVJ7	Approved	Calcitriol increases the expression of Protein GREB1 (GREB1).	[25]
Testosterone	DM7HUNW	Approved	Testosterone decreases the expression of Protein GREB1 (GREB1).	[26]
Progesterone	DMUY35B	Approved	Progesterone increases the expression of Protein GREB1 (GREB1).	[27]
Fulvestrant	DM0YZC6	Approved	Fulvestrant decreases the expression of Protein GREB1 (GREB1).	[28]
Diethylstilbestrol	DMN3UXQ	Approved	Diethylstilbestrol increases the expression of Protein GREB1 (GREB1).	[29]
Ethinyl estradiol	DMODJ40	Approved	Ethinyl estradiol increases the expression of Protein GREB1 (GREB1).	[30]
Mifepristone	DMGZQEF	Approved	Mifepristone increases the expression of Protein GREB1 (GREB1).	[22]
Enzalutamide	DMGL19D	Approved	Enzalutamide decreases the expression of Protein GREB1 (GREB1).	[31]
Testosterone Undecanoate	DMZO10Y	Approved	Testosterone Undecanoate decreases the expression of Protein GREB1 (GREB1).	[32]
Mestranol	DMG3F94	Approved	Mestranol increases the expression of Protein GREB1 (GREB1).	[22]
Spironolactone	DM2AQ5N	Approved	Spironolactone increases the expression of Protein GREB1 (GREB1).	[22]
Norethindrone	DMTY169	Approved	Norethindrone increases the expression of Protein GREB1 (GREB1).	[22]
Methyltestosterone	DMWLFGO	Approved	Methyltestosterone increases the expression of Protein GREB1 (GREB1).	[33]
Nandrolone	DMFWKG1	Approved	Nandrolone increases the expression of Protein GREB1 (GREB1).	[33]
Cyproterone	DMQXLD2	Approved	Cyproterone increases the expression of Protein GREB1 (GREB1).	[22]
Dihydrotestosterone	DM3S8XC	Phase 4	Dihydrotestosterone increases the expression of Protein GREB1 (GREB1).	[6]
Pregnenolone	DM6VFO1	Phase 4	Pregnenolone increases the expression of Protein GREB1 (GREB1).	[22]
Lynestrenol	DM82JP0	Phase 4	Lynestrenol increases the expression of Protein GREB1 (GREB1).	[22]
Resveratrol	DM3RWXL	Phase 3	Resveratrol increases the expression of Protein GREB1 (GREB1).	[35]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Protein GREB1 (GREB1).	[36]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of Protein GREB1 (GREB1).	[37]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Protein GREB1 (GREB1).	[38]
GSK525762	DMPAWBN	Phase 1	GSK525762 decreases the expression of Protein GREB1 (GREB1).	[38]
HEXESTROL	DM9AGWQ	Withdrawn from market	HEXESTROL increases the expression of Protein GREB1 (GREB1).	[33]
MX-4509	DMC4RK7	Discontinued in Phase 1	MX-4509 increases the expression of Protein GREB1 (GREB1).	[33]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A increases the expression of Protein GREB1 (GREB1).	[40]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of Protein GREB1 (GREB1).	[41]
Coumestrol	DM40TBU	Investigative	Coumestrol increases the expression of Protein GREB1 (GREB1).	[42]
methyl p-hydroxybenzoate	DMO58UW	Investigative	methyl p-hydroxybenzoate increases the expression of Protein GREB1 (GREB1).	[43]
Glyphosate	DM0AFY7	Investigative	Glyphosate increases the expression of Protein GREB1 (GREB1).	[44]
[3H]methyltrienolone	DMTSGOW	Investigative	[3H]methyltrienolone increases the expression of Protein GREB1 (GREB1).	[6]
Chrysin	DM7V2LG	Investigative	Chrysin increases the expression of Protein GREB1 (GREB1).	[22]
Kaempferol	DMHEMUB	Investigative	Kaempferol increases the expression of Protein GREB1 (GREB1).	[35]
OXYBENZONE	DMMZYX6	Investigative	OXYBENZONE increases the expression of Protein GREB1 (GREB1).	[22]
Daidzein	DMRFTJX	Investigative	Daidzein increases the expression of Protein GREB1 (GREB1).	[40]
Linalool	DMGZQ5P	Investigative	Linalool increases the expression of Protein GREB1 (GREB1).	[45]
Apigenin	DMI3491	Investigative	Apigenin increases the expression of Protein GREB1 (GREB1).	[22]
Tetramethylbutylphenol	DMW9CH2	Investigative	Tetramethylbutylphenol increases the expression of Protein GREB1 (GREB1).	[33]
eucalyptol	DME5CK3	Investigative	eucalyptol increases the expression of Protein GREB1 (GREB1).	[45]
HPTE	DMRPZD4	Investigative	HPTE increases the expression of Protein GREB1 (GREB1).	[40]
(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE	DMTPQ84	Investigative	(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE increases the expression of Protein GREB1 (GREB1).	[33]
ETHISTERONE	DMDXRP1	Investigative	ETHISTERONE increases the expression of Protein GREB1 (GREB1).	[22]

1 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 decreases the phosphorylation of Protein GREB1 (GREB1).	[39]

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