Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTQBB8NT)

• DOT Name: Adhesion G-protein coupled receptor G1 (ADGRG1)
• Synonyms: G-protein coupled receptor 56; Protein TM7XN1
• Gene Name: ADGRG1
• Related Disease:
  Bilateral frontoparietal polymicrogyria
  Congenital muscular dystrophy
  Epilepsy
  Melanoma
  Non-insulin dependent diabetes
  Rheumatoid arthritis
  Acute monocytic leukemia
  Advanced cancer
  Astrocytoma
  Cobblestone lissencephaly
  Colorectal carcinoma
  Colorectal neoplasm
  Diabetic kidney disease
  Ehlers-Danlos syndrome, vascular type
  Epithelial ovarian cancer
  Esophageal squamous cell carcinoma
  Familial prostate carcinoma
  Joubert syndrome
  LennoxGastaut syndrome
  Lissencephaly spectrum disorders
  Lung adenocarcinoma
  Movement disorder
  Multiple sclerosis
  Neoplasm
  Pancreatic cancer
  Pancreatic tumour
  Peripheral arterial disease
  Polyarteritis nodosa
  Prostate cancer
  Prostate cancer, hereditary, 1
  Prostate carcinoma
  Squamous cell carcinoma
  Vasculitis due to ADA2 deficiency
  Adult glioblastoma
  Glioblastoma multiforme
  Glioma
  Metastatic malignant neoplasm
  Nervous system disease
  Acute myelogenous leukaemia
  Bilateral perisylvian polymicrogyria
  Metastatic melanoma
• UniProt ID: AGRG1_HUMAN
• PDB ID: 7SF8
• Pfam ID: PF00002 ; PF18619 ; PF01825 ; PF18587
• Sequence:
  MTPQSLLQTTLFLLSLLFLVQGAHGRGHREDFRFCSQRNQTHRSSLHYKPTPDLRISIEN
  SEEALTVHAPFPAAHPASRSFPDPRGLYHFCLYWNRHAGRLHLLYGKRDFLLSDKASSLL
  CFQHQEESLAQGPPLLATSVTSWWSPQNISLPSAASFTFSFHSPPHTAAHNASVDMCELK
  RDLQLLSQFLKHPQKASRRPSAAPASQQLQSLESKLTSVRFMGDMVSFEEDRINATVWKL
  QPTAGLQDLHIHSRQEEEQSEIMEYSVLLPRTLFQRTKGRSGEAEKRLLLVDFSSQALFQ
  DKNSSQVLGEKVLGIVVQNTKVANLTEPVVLTFQHQLQPKNVTLQCVFWVEDPTLSSPGH
  WSSAGCETVRRETQTSCFCNHLTYFAVLMVSSVEVDAVHKHYLSLLSYVGCVVSALACLV
  TIAAYLCSRVPLPCRRKPRDYTIKVHMNLLLAVFLLDTSFLLSEPVALTGSEAGCRASAI
  FLHFSLLTCLSWMGLEGYNLYRLVVEVFGTYVPGYLLKLSAMGWGFPIFLVTLVALVDVD
  NYGPIILAVHRTPEGVIYPSMCWIRDSLVSYITNLGLFSLVFLFNMAMLATMVVQILRLR
  PHTQKWSHVLTLLGLSLVLGLPWALIFFSFASGTFQLVVLYLFSIITSFQGFLIFIWYWS
  MRLQARGGPSPLKSNSDSARLPISSGSTSSSRI
• Function: Receptor involved in cell adhesion and probably in cell-cell interactions. Mediates cell matrix adhesion in developing neurons and hematopoietic stem cells. Receptor for collagen III/COL3A1 in the developing brain and involved in regulation of cortical development, specifically in maintenance of the pial basement membrane integrity and in cortical lamination. Binding to the COL3A1 ligand inhibits neuronal migration and activates the RhoA pathway by coupling to GNA13 and possibly GNA12. Plays a role in the maintenance of hematopoietic stem cells and/or leukemia stem cells in bone marrow niche. Plays a critical role in cancer progression by inhibiting VEGFA production threreby inhibiting angiogenesis through a signaling pathway mediated by PRKCA. Plays an essential role in testis development; [ADGRG1 N-terminal fragment]: Plays a critical role in cancer progression by activating VEGFA production and angiogenesis through a signaling pathway mediated by PRKCA.
• Tissue Specificity: Widely distributed with highest levels found in thyroid gland, brain and heart. Expressed in a great number of tumor cells. Expression is down-regulated in different tumors from highly metastatic cells.

Molecular Interaction Atlas (MIA) of This DOT

41 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Bilateral frontoparietal polymicrogyria	DIS9DK0G	Definitive	Autosomal recessive	[1]
Congenital muscular dystrophy	DISKY7OY	Definitive	Genetic Variation	[2]
Epilepsy	DISBB28L	Definitive	Genetic Variation	[3]
Melanoma	DIS1RRCY	Definitive	Biomarker	[4]
Non-insulin dependent diabetes	DISK1O5Z	Definitive	Biomarker	[5]
Rheumatoid arthritis	DISTSB4J	Definitive	Altered Expression	[6]
Acute monocytic leukemia	DIS28NEL	Strong	Altered Expression	[7]
Advanced cancer	DISAT1Z9	Strong	Altered Expression	[8]
Astrocytoma	DISL3V18	Strong	Altered Expression	[9]
Cobblestone lissencephaly	DIS56826	Strong	Genetic Variation	[10]
Colorectal carcinoma	DIS5PYL0	Strong	Biomarker	[11]
Colorectal neoplasm	DISR1UCN	Strong	Biomarker	[11]
Diabetic kidney disease	DISJMWEY	Strong	Biomarker	[12]
Ehlers-Danlos syndrome, vascular type	DISTZ07K	Strong	Biomarker	[13]
Epithelial ovarian cancer	DIS56MH2	Strong	Biomarker	[4]
Esophageal squamous cell carcinoma	DIS5N2GV	Strong	Altered Expression	[14]
Familial prostate carcinoma	DISL9KNO	Strong	Biomarker	[15]
Joubert syndrome	DIS7P5CO	Strong	Genetic Variation	[16]
LennoxGastaut syndrome	DISOTGO5	Strong	Genetic Variation	[17]
Lissencephaly spectrum disorders	DISBCZL7	Strong	Biomarker	[18]
Lung adenocarcinoma	DISD51WR	Strong	Biomarker	[19]
Movement disorder	DISOJJ2D	Strong	CausalMutation	[3]
Multiple sclerosis	DISB2WZI	Strong	Altered Expression	[20]
Neoplasm	DISZKGEW	Strong	Biomarker	[11]
Pancreatic cancer	DISJC981	Strong	Biomarker	[4]
Pancreatic tumour	DIS3U0LK	Strong	Altered Expression	[21]
Peripheral arterial disease	DIS78WFB	Strong	Altered Expression	[22]
Polyarteritis nodosa	DISRQ5X8	Strong	Biomarker	[23]
Prostate cancer	DISF190Y	Strong	Biomarker	[24]
Prostate cancer, hereditary, 1	DISE2P4L	Strong	Biomarker	[15]
Prostate carcinoma	DISMJPLE	Strong	Genetic Variation	[15]
Squamous cell carcinoma	DISQVIFL	Strong	Altered Expression	[14]
Vasculitis due to ADA2 deficiency	DIS1UHPY	Strong	Biomarker	[23]
Adult glioblastoma	DISVP4LU	moderate	Biomarker	[23]
Glioblastoma multiforme	DISK8246	moderate	Biomarker	[23]
Glioma	DIS5RPEH	moderate	Biomarker	[23]
Metastatic malignant neoplasm	DIS86UK6	moderate	Altered Expression	[25]
Nervous system disease	DISJ7GGT	Disputed	Biomarker	[26]
Acute myelogenous leukaemia	DISCSPTN	Limited	Biomarker	[7]
Bilateral perisylvian polymicrogyria	DISIF9XK	Limited	GermlineCausalMutation	[27]
Metastatic melanoma	DISSL43L	Limited	Biomarker	[25]

This DOT Affected the Drug Response of 2 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Fluorouracil	DMUM7HZ	Approved	Adhesion G-protein coupled receptor G1 (ADGRG1) affects the response to substance of Fluorouracil.	[59]
Mitomycin	DMH0ZJE	Approved	Adhesion G-protein coupled receptor G1 (ADGRG1) affects the response to substance of Mitomycin.	[59]

33 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 Adhesion G-protein coupled receptor G1 (ADGRG1).	[28]
Ciclosporin	DMAZJFX	Approved	Ciclosporin increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[29]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[30]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[31]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[32]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[33]
Cisplatin	DMRHGI9	Approved	Cisplatin decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[34]
Estradiol	DMUNTE3	Approved	Estradiol increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[35]
Arsenic	DMTL2Y1	Approved	Arsenic affects the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[36]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[37]
Temozolomide	DMKECZD	Approved	Temozolomide decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[38]
Calcitriol	DM8ZVJ7	Approved	Calcitriol increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[39]
Triclosan	DMZUR4N	Approved	Triclosan increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[40]
Decitabine	DMQL8XJ	Approved	Decitabine affects the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[41]
Zoledronate	DMIXC7G	Approved	Zoledronate decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[42]
Phenobarbital	DMXZOCG	Approved	Phenobarbital affects the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[43]
Panobinostat	DM58WKG	Approved	Panobinostat decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[44]
Troglitazone	DM3VFPD	Approved	Troglitazone increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[45]
Rosiglitazone	DMILWZR	Approved	Rosiglitazone increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[46]
Nicotine	DMWX5CO	Approved	Nicotine increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[47]
Mifepristone	DMGZQEF	Approved	Mifepristone decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[48]
Hydrocortisone	DMGEMB7	Approved	Hydrocortisone decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[49]
Cholecalciferol	DMGU74E	Approved	Cholecalciferol affects the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[50]
SNDX-275	DMH7W9X	Phase 3	SNDX-275 decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[44]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[35]
Belinostat	DM6OC53	Phase 2	Belinostat decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[44]
Afimoxifene	DMFORDT	Phase 2	Afimoxifene increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[51]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[52]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[53]
Leflunomide	DMR8ONJ	Phase 1 Trial	Leflunomide increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[54]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde increases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[56]
Sulforaphane	DMQY3L0	Investigative	Sulforaphane decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[57]
QUERCITRIN	DM1DH96	Investigative	QUERCITRIN decreases the expression of Adhesion G-protein coupled receptor G1 (ADGRG1).	[58]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the methylation of Adhesion G-protein coupled receptor G1 (ADGRG1).	[55]

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