Details of Drug Off-Target (DOT)

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

DOT Name	Glypican-1 (GPC1)
Gene Name	GPC1
Related Disease	Ovarian neoplasm ( ) Pancreatic tumour ( ) ADan amyloidosis ( ) Adenocarcinoma ( ) Alzheimer disease ( ) Benign prostatic hyperplasia ( ) Brachydactyly ( ) Breast cancer ( ) Breast carcinoma ( ) Breast neoplasm ( ) Bronchopulmonary dysplasia ( ) Cervical cancer ( ) Colon cancer ( ) Colon carcinoma ( ) Colorectal carcinoma ( ) Craniosynostosis ( ) Duchenne muscular dystrophy ( ) Epithelioid mesothelioma ( ) Esophageal squamous cell carcinoma ( ) Fibrodysplasia ossificans progressiva ( ) Glioma ( ) Hepatocellular carcinoma ( ) Mesothelioma ( ) Neoplasm ( ) Niemann-Pick disease, type C1 ( ) Pachyonychia congenita 3 ( ) Pancreatic adenocarcinoma ( ) Pancreatic ductal carcinoma ( ) Prostate cancer ( ) Prostate carcinoma ( ) Pseudohypoparathyroidism type 1A ( ) Schizophrenia ( ) Simpson-Golabi-Behmel syndrome ( ) Simpson-Golabi-Behmel syndrome type 1 ( ) Squamous cell carcinoma ( ) Glioblastoma multiforme ( ) Pancreas disorder ( ) Advanced cancer ( ) Cholangiocarcinoma ( ) Chronic pancreatitis ( ) Gallbladder carcinoma ( ) Hereditary hemochromatosis ( ) Lung adenocarcinoma ( ) Pancreatic cancer ( ) Rheumatoid arthritis ( )
UniProt ID	GPC1_HUMAN
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
PDB ID	4ACR; 4AD7; 4BWE; 4YWT
Pfam ID	PF01153
Sequence	MELRARGWWLLCAAAALVACARGDPASKSRSCGEVRQIYGAKGFSLSDVPQAEISGEHLR ICPQGYTCCTSEMEENLANRSHAELETALRDSSRVLQAMLATQLRSFDDHFQHLLNDSER TLQATFPGAFGELYTQNARAFRDLYSELRLYYRGANLHLEETLAEFWARLLERLFKQLHP QLLLPDDYLDCLGKQAEALRPFGEAPRELRLRATRAFVAARSFVQGLGVASDVVRKVAQV PLGPECSRAVMKLVYCAHCLGVPGARPCPDYCRNVLKGCLANQADLDAEWRNLLDSMVLI TDKFWGTSGVESVIGSVHTWLAEAINALQDNRDTLTAKVIQGCGNPKVNPQGPGPEEKRR RGKLAPRERPPSGTLEKLVSEAKAQLRDVQDFWISLPGTLCSEKMALSTASDDRCWNGMA RGRYLPEVMGDGLANQINNPEVEVDITKPDMTIRQQIMQLKIMTNRLRSAYNGNDVDFQD ASDDGSGSGSGDGCLDDLCSRKVSRKSSSSRTPLTHALPGLSEQEGQKTSAASCPQPPTF LLPLLLFLALTVARPRWR
Function	Cell surface proteoglycan that bears heparan sulfate. Binds, via the heparan sulfate side chains, alpha-4 (V) collagen and participates in Schwann cell myelination. May act as a catalyst in increasing the rate of conversion of prion protein PRPN(C) to PRNP(Sc) via associating (via the heparan sulfate side chains) with both forms of PRPN, targeting them to lipid rafts and facilitating their interaction. Required for proper skeletal muscle differentiation by sequestering FGF2 in lipid rafts preventing its binding to receptors (FGFRs) and inhibiting the FGF-mediated signaling.
KEGG Pathway	Proteoglycans in cancer (hsa05205 ) Fluid shear stress and atherosclerosis (hsa05418 )
Reactome Pathway	HS-GAG biosynthesis (R-HSA-2022928 ) HS-GAG degradation (R-HSA-2024096 ) Cell surface interactions at the vascular wall (R-HSA-202733 ) Defective B4GALT7 causes EDS, progeroid type (R-HSA-3560783 ) Defective B3GAT3 causes JDSSDHD (R-HSA-3560801 ) Defective EXT2 causes exostoses 2 (R-HSA-3656237 ) Defective EXT1 causes exostoses 1, TRPS2 and CHDS (R-HSA-3656253 ) Signaling by ROBO receptors (R-HSA-376176 ) Defective B3GALT6 causes EDSP2 and SEMDJL1 (R-HSA-4420332 ) Attachment and Entry (R-HSA-9694614 ) Retinoid metabolism and transport (R-HSA-975634 ) A tetrasaccharide linker sequence is required for GAG synthesis (R-HSA-1971475 )

Molecular Interaction Atlas (MIA) of This DOT

45 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance
Ovarian neoplasm	DISEAFTY	Definitive	Biomarker	[1]
Pancreatic tumour	DIS3U0LK	Definitive	Biomarker	[2]
ADan amyloidosis	DISXF54F	Strong	Biomarker	[3]
Adenocarcinoma	DIS3IHTY	Strong	Biomarker	[4]
Alzheimer disease	DISF8S70	Strong	Altered Expression	[5]
Benign prostatic hyperplasia	DISI3CW2	Strong	Biomarker	[6]
Brachydactyly	DIS2533F	Strong	Biomarker	[7]
Breast cancer	DIS7DPX1	Strong	Altered Expression	[8]
Breast carcinoma	DIS2UE88	Strong	Altered Expression	[8]
Breast neoplasm	DISNGJLM	Strong	Biomarker	[9]
Bronchopulmonary dysplasia	DISO0BY5	Strong	Biomarker	[10]
Cervical cancer	DISFSHPF	Strong	Biomarker	[11]
Colon cancer	DISVC52G	Strong	Biomarker	[12]
Colon carcinoma	DISJYKUO	Strong	Biomarker	[12]
Colorectal carcinoma	DIS5PYL0	Strong	Altered Expression	[13]
Craniosynostosis	DIS6J405	Strong	Biomarker	[14]
Duchenne muscular dystrophy	DISRQ3NV	Strong	Biomarker	[15]
Epithelioid mesothelioma	DIS17SNY	Strong	Altered Expression	[16]
Esophageal squamous cell carcinoma	DIS5N2GV	Strong	Biomarker	[17]
Fibrodysplasia ossificans progressiva	DISAT6WU	Strong	Altered Expression	[18]
Glioma	DIS5RPEH	Strong	Altered Expression	[19]
Hepatocellular carcinoma	DIS0J828	Strong	Altered Expression	[13]
Mesothelioma	DISKWK9M	Strong	Biomarker	[4]
Neoplasm	DISZKGEW	Strong	Biomarker	[20]
Niemann-Pick disease, type C1	DIS9HUE3	Strong	Biomarker	[21]
Pachyonychia congenita 3	DISZLC6C	Strong	Biomarker	[22]
Pancreatic adenocarcinoma	DISKHX7S	Strong	Biomarker	[23]
Pancreatic ductal carcinoma	DIS26F9Q	Strong	Biomarker	[24]
Prostate cancer	DISF190Y	Strong	Altered Expression	[22]
Prostate carcinoma	DISMJPLE	Strong	Altered Expression	[22]
Pseudohypoparathyroidism type 1A	DISSOR3M	Strong	Biomarker	[25]
Schizophrenia	DISSRV2N	Strong	Biomarker	[26]
Simpson-Golabi-Behmel syndrome	DIS9H9TY	Strong	Genetic Variation	[27]
Simpson-Golabi-Behmel syndrome type 1	DISYV73N	Strong	Genetic Variation	[27]
Squamous cell carcinoma	DISQVIFL	Strong	Altered Expression	[11]
Glioblastoma multiforme	DISK8246	moderate	Altered Expression	[28]
Pancreas disorder	DISDH7NI	Disputed	Altered Expression	[29]
Advanced cancer	DISAT1Z9	Limited	Biomarker	[30]
Cholangiocarcinoma	DIS71F6X	Limited	Altered Expression	[13]
Chronic pancreatitis	DISBUOMJ	Limited	Altered Expression	[31]
Gallbladder carcinoma	DISD6ACL	Limited	Altered Expression	[13]
Hereditary hemochromatosis	DISVG5MT	Limited	Biomarker	[32]
Lung adenocarcinoma	DISD51WR	Limited	Altered Expression	[16]
Pancreatic cancer	DISJC981	Limited	Biomarker	[10]
Rheumatoid arthritis	DISTSB4J	Limited	Altered Expression	[33]
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⏷ Show the Full List of 45 Disease(s)

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This DOT

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the methylation of Glypican-1 (GPC1).	[34]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of Glypican-1 (GPC1).	[45]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A increases the methylation of Glypican-1 (GPC1).	[47]
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15 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Ciclosporin	DMAZJFX	Approved	Ciclosporin increases the expression of Glypican-1 (GPC1).	[35]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Glypican-1 (GPC1).	[36]
Estradiol	DMUNTE3	Approved	Estradiol affects the expression of Glypican-1 (GPC1).	[37]
Ivermectin	DMDBX5F	Approved	Ivermectin decreases the expression of Glypican-1 (GPC1).	[38]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of Glypican-1 (GPC1).	[39]
Temozolomide	DMKECZD	Approved	Temozolomide decreases the expression of Glypican-1 (GPC1).	[40]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide increases the expression of Glypican-1 (GPC1).	[41]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Glypican-1 (GPC1).	[42]
Testosterone enanthate	DMB6871	Approved	Testosterone enanthate affects the expression of Glypican-1 (GPC1).	[43]
Bicalutamide	DMZMSPF	Approved	Bicalutamide decreases the expression of Glypican-1 (GPC1).	[44]
Vitamin C	DMXJ7O8	Approved	Vitamin C increases the expression of Glypican-1 (GPC1).	[41]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Glypican-1 (GPC1).	[46]
Sulforaphane	DMQY3L0	Investigative	Sulforaphane increases the expression of Glypican-1 (GPC1).	[48]
Deguelin	DMXT7WG	Investigative	Deguelin decreases the expression of Glypican-1 (GPC1).	[49]
3R14S-OCHRATOXIN A	DM2KEW6	Investigative	3R14S-OCHRATOXIN A increases the expression of Glypican-1 (GPC1).	[50]
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⏷ Show the Full List of 15 Drug(s)

References

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