General Information of Drug Off-Target (DOT) (ID: OTJFOR67)

DOT Name Amphiregulin (AREG)
Synonyms AR; Colorectum cell-derived growth factor; CRDGF
Gene Name AREG
UniProt ID
AREG_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
2RNL
Sequence
MRAPLLPPAPVVLSLLILGSGHYAAGLDLNDTYSGKREPFSGDHSADGFEVTSRSEMSSG
SEISPVSEMPSSSEPSSGADYDYSEEYDNEPQIPGYIVDDSVRVEQVVKPPQNKTESENT
SDKPKRKKKGGKNGKNRRNRKKKNPCNAEFQNFCIHGECKYIEHLEAVTCKCQQEYFGER
CGEKSMKTHSMIDSSLSKIALAAIAAFMSAVILTAVAVITVQLRRQYVRKYEGEAEERKK
LRQENGNVHAIA
Function Ligand of the EGF receptor/EGFR. Autocrine growth factor as well as a mitogen for a broad range of target cells including astrocytes, Schwann cells and fibroblasts.
KEGG Pathway
MAPK sig.ling pathway (hsa04010 )
ErbB sig.ling pathway (hsa04012 )
PI3K-Akt sig.ling pathway (hsa04151 )
Hippo sig.ling pathway (hsa04390 )
Colorectal cancer (hsa05210 )
Reactome Pathway
Signaling by EGFR (R-HSA-177929 )
GRB2 events in EGFR signaling (R-HSA-179812 )
GAB1 signalosome (R-HSA-180292 )
SHC1 events in EGFR signaling (R-HSA-180336 )
EGFR downregulation (R-HSA-182971 )
COPII-mediated vesicle transport (R-HSA-204005 )
EGFR interacts with phospholipase C-gamma (R-HSA-212718 )
Constitutive Signaling by Aberrant PI3K in Cancer (R-HSA-2219530 )
Inhibition of Signaling by Overexpressed EGFR (R-HSA-5638303 )
RAF/MAP kinase cascade (R-HSA-5673001 )
Cargo concentration in the ER (R-HSA-5694530 )
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling (R-HSA-6811558 )
Cargo recognition for clathrin-mediated endocytosis (R-HSA-8856825 )
Clathrin-mediated endocytosis (R-HSA-8856828 )
Extra-nuclear estrogen signaling (R-HSA-9009391 )
Estrogen-dependent nuclear events downstream of ESR-membrane signaling (R-HSA-9634638 )
NFE2L2 regulating tumorigenic genes (R-HSA-9818030 )
PIP3 activates AKT signaling (R-HSA-1257604 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 2 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Gemcitabine DMSE3I7 Approved Amphiregulin (AREG) decreases the response to substance of Gemcitabine. [7]
Gefitinib DM15F0X Approved Amphiregulin (AREG) decreases the response to substance of Gefitinib. [48]
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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 Amphiregulin (AREG). [1]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Amphiregulin (AREG). [2]
Tretinoin DM49DUI Approved Tretinoin increases the expression of Amphiregulin (AREG). [3]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Amphiregulin (AREG). [4]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Amphiregulin (AREG). [5]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of Amphiregulin (AREG). [6]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Amphiregulin (AREG). [7]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Amphiregulin (AREG). [8]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Amphiregulin (AREG). [9]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Amphiregulin (AREG). [10]
Methotrexate DM2TEOL Approved Methotrexate decreases the expression of Amphiregulin (AREG). [11]
Decitabine DMQL8XJ Approved Decitabine increases the expression of Amphiregulin (AREG). [12]
Marinol DM70IK5 Approved Marinol decreases the expression of Amphiregulin (AREG). [13]
Phenobarbital DMXZOCG Approved Phenobarbital affects the expression of Amphiregulin (AREG). [14]
Progesterone DMUY35B Approved Progesterone increases the expression of Amphiregulin (AREG). [15]
Menadione DMSJDTY Approved Menadione increases the expression of Amphiregulin (AREG). [9]
Fluorouracil DMUM7HZ Approved Fluorouracil increases the expression of Amphiregulin (AREG). [16]
Fulvestrant DM0YZC6 Approved Fulvestrant decreases the expression of Amphiregulin (AREG). [17]
Cannabidiol DM0659E Approved Cannabidiol increases the expression of Amphiregulin (AREG). [18]
Diethylstilbestrol DMN3UXQ Approved Diethylstilbestrol increases the expression of Amphiregulin (AREG). [19]
Etoposide DMNH3PG Approved Etoposide increases the expression of Amphiregulin (AREG). [20]
Irinotecan DMP6SC2 Approved Irinotecan increases the expression of Amphiregulin (AREG). [21]
Testosterone enanthate DMB6871 Approved Testosterone enanthate affects the expression of Amphiregulin (AREG). [22]
Paclitaxel DMLB81S Approved Paclitaxel increases the expression of Amphiregulin (AREG). [7]
Estrone DM5T6US Approved Estrone increases the expression of Amphiregulin (AREG). [19]
Dinoprostone DMTYOPD Approved Dinoprostone increases the expression of Amphiregulin (AREG). [24]
Mestranol DMG3F94 Approved Mestranol increases the expression of Amphiregulin (AREG). [19]
Exemestane DM9HPW3 Approved Exemestane increases the expression of Amphiregulin (AREG). [26]
Seocalcitol DMKL9QO Phase 3 Seocalcitol increases the expression of Amphiregulin (AREG). [27]
Chlorpromazine DMBGZI3 Phase 3 Trial Chlorpromazine decreases the expression of Amphiregulin (AREG). [28]
Genistein DM0JETC Phase 2/3 Genistein increases the expression of Amphiregulin (AREG). [29]
Afimoxifene DMFORDT Phase 2 Afimoxifene decreases the expression of Amphiregulin (AREG). [30]
ANW-32821 DMMJOZD Phase 2 ANW-32821 increases the expression of Amphiregulin (AREG). [31]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the expression of Amphiregulin (AREG). [32]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Amphiregulin (AREG). [33]
HEXESTROL DM9AGWQ Withdrawn from market HEXESTROL increases the expression of Amphiregulin (AREG). [19]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of Amphiregulin (AREG). [29]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Amphiregulin (AREG). [1]
Formaldehyde DM7Q6M0 Investigative Formaldehyde decreases the expression of Amphiregulin (AREG). [35]
Milchsaure DM462BT Investigative Milchsaure affects the expression of Amphiregulin (AREG). [36]
Forskolin DM6ITNG Investigative Forskolin increases the expression of Amphiregulin (AREG). [24]
CH-223191 DMMJZYC Investigative CH-223191 decreases the expression of Amphiregulin (AREG). [38]
Bilirubin DMI0V4O Investigative Bilirubin increases the expression of Amphiregulin (AREG). [39]
Nitrobenzanthrone DMN6L70 Investigative Nitrobenzanthrone increases the expression of Amphiregulin (AREG). [40]
Cycloheximide DMGDA3C Investigative Cycloheximide increases the expression of Amphiregulin (AREG). [41]
OXYBENZONE DMMZYX6 Investigative OXYBENZONE increases the expression of Amphiregulin (AREG). [43]
Isoarnebin 4 DM0B7NO Investigative Isoarnebin 4 decreases the expression of Amphiregulin (AREG). [44]
Ginsenoside RG3 DMFN58T Investigative Ginsenoside RG3 decreases the expression of Amphiregulin (AREG). [45]
All-trans-retinal DM6CEVB Investigative All-trans-retinal increases the expression of Amphiregulin (AREG). [3]
ROLIPRAM DMJ03UM Investigative ROLIPRAM increases the expression of Amphiregulin (AREG). [24]
isobutylmethylxanthine DM46F5X Investigative isobutylmethylxanthine increases the expression of Amphiregulin (AREG). [24]
Hydroxybenzo(a)pyrene DM9H5EN Investigative Hydroxybenzo(a)pyrene increases the expression of Amphiregulin (AREG). [46]
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⏷ Show the Full List of 52 Drug(s)
8 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Sodium lauryl sulfate DMLJ634 Approved Sodium lauryl sulfate increases the secretion of Amphiregulin (AREG). [23]
Deoxycholic acid DM3GYAL Approved Deoxycholic acid increases the secretion of Amphiregulin (AREG). [25]
Batimastat DM92VRP Preclinical Batimastat decreases the secretion of Amphiregulin (AREG). [34]
Phencyclidine DMQBEYX Investigative Phencyclidine increases the secretion of Amphiregulin (AREG). [37]
U0126 DM31OGF Investigative U0126 decreases the secretion of Amphiregulin (AREG). [42]
PD-158780 DMQXYE9 Investigative PD-158780 decreases the secretion of Amphiregulin (AREG). [42]
SU 6656 DMF1P6W Investigative SU 6656 decreases the secretion of Amphiregulin (AREG). [42]
Pervanadate DM873BS Investigative Pervanadate increases the cleavage of Amphiregulin (AREG). [47]
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⏷ Show the Full List of 8 Drug(s)

References

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18 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
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21 Gefitinib ("Iressa", ZD1839) inhibits SN38-triggered EGF signals and IL-8 production in gastric cancer cells. Cancer Chemother Pharmacol. 2005 Apr;55(4):393-403. doi: 10.1007/s00280-004-0904-0. Epub 2004 Oct 5.
22 Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
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28 Effects of chlorpromazine with and without UV irradiation on gene expression of HepG2 cells. Mutat Res. 2005 Aug 4;575(1-2):47-60. doi: 10.1016/j.mrfmmm.2005.03.002. Epub 2005 Apr 26.
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