General Information of Drug Off-Target (DOT) (ID: OTX7MWW1)

DOT Name Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1)
Synonyms IP3 receptor isoform 1; IP3R 1; InsP3R1; Type 1 inositol 1,4,5-trisphosphate receptor; Type 1 InsP3 receptor
Gene Name ITPR1
Related Disease
Aniridia-cerebellar ataxia-intellectual disability syndrome ( )
Spinocerebellar ataxia type 29 ( )
Spinocerebellar ataxia type 15/16 ( )
UniProt ID
ITPR1_HUMAN
Pfam ID
PF08709 ; PF00520 ; PF02815 ; PF08454 ; PF01365
Sequence
MSDKMSSFLHIGDICSLYAEGSTNGFISTLGLVDDRCVVQPETGDLNNPPKKFRDCLFKL
CPMNRYSAQKQFWKAAKPGANSTTDAVLLNKLHHAADLEKKQNETENRKLLGTVIQYGNV
IQLLHLKSNKYLTVNKRLPALLEKNAMRVTLDEAGNEGSWFYIQPFYKLRSIGDSVVIGD
KVVLNPVNAGQPLHASSHQLVDNPGCNEVNSVNCNTSWKIVLFMKWSDNKDDILKGGDVV
RLFHAEQEKFLTCDEHRKKQHVFLRTTGRQSATSATSSKALWEVEVVQHDPCRGGAGYWN
SLFRFKHLATGHYLAAEVDPDFEEECLEFQPSVDPDQDASRSRLRNAQEKMVYSLVSVPE
GNDISSIFELDPTTLRGGDSLVPRNSYVRLRHLCTNTWVHSTNIPIDKEEEKPVMLKIGT
SPVKEDKEAFAIVPVSPAEVRDLDFANDASKVLGSIAGKLEKGTITQNERRSVTKLLEDL
VYFVTGGTNSGQDVLEVVFSKPNRERQKLMREQNILKQIFKLLQAPFTDCGDGPMLRLEE
LGDQRHAPFRHICRLCYRVLRHSQQDYRKNQEYIAKQFGFMQKQIGYDVLAEDTITALLH
NNRKLLEKHITAAEIDTFVSLVRKNREPRFLDYLSDLCVSMNKSIPVTQELICKAVLNPT
NADILIETKLVLSRFEFEGVSSTGENALEAGEDEEEVWLFWRDSNKEIRSKSVRELAQDA
KEGQKEDRDVLSYYRYQLNLFARMCLDRQYLAINEISGQLDVDLILRCMSDENLPYDLRA
SFCRLMLHMHVDRDPQEQVTPVKYARLWSEIPSEIAIDDYDSSGASKDEIKERFAQTMEF
VEEYLRDVVCQRFPFSDKEKNKLTFEVVNLARNLIYFGFYNFSDLLRLTKILLAILDCVH
VTTIFPISKMAKGEENKGNNDVEKLKSSNVMRSIHGVGELMTQVVLRGGGFLPMTPMAAA
PEGNVKQAEPEKEDIMVMDTKLKIIEILQFILNVRLDYRISCLLCIFKREFDESNSQTSE
TSSGNSSQEGPSNVPGALDFEHIEEQAEGIFGGSEENTPLDLDDHGGRTFLRVLLHLTMH
DYPPLVSGALQLLFRHFSQRQEVLQAFKQVQLLVTSQDVDNYKQIKQDLDQLRSIVEKSE
LWVYKGQGPDETMDGASGENEHKKTEEGNNKPQKHESTSSYNYRVVKEILIRLSKLCVQE
SASVRKSRKQQQRLLRNMGAHAVVLELLQIPYEKAEDTKMQEIMRLAHEFLQNFCAGNQQ
NQALLHKHINLFLNPGILEAVTMQHIFMNNFQLCSEINERVVQHFVHCIETHGRNVQYIK
FLQTIVKAEGKFIKKCQDMVMAELVNSGEDVLVFYNDRASFQTLIQMMRSERDRMDENSP
LMYHIHLVELLAVCTEGKNVYTEIKCNSLLPLDDIVRVVTHEDCIPEVKIAYINFLNHCY
VDTEVEMKEIYTSNHMWKLFENFLVDICRACNNTSDRKHADSILEKYVTEIVMSIVTTFF
SSPFSDQSTTLQTRQPVFVQLLQGVFRVYHCNWLMPSQKASVESCIRVLSDVAKSRAIAI
PVDLDSQVNNLFLKSHSIVQKTAMNWRLSARNAARRDSVLAASRDYRNIIERLQDIVSAL
EDRLRPLVQAELSVLVDVLHRPELLFPENTDARRKCESGGFICKLIKHTKQLLEENEEKL
CIKVLQTLREMMTKDRGYGEKLISIDELDNAELPPAPDSENATEELEPSPPLRQLEDHKR
GEALRQVLVNRYYGNVRPSGRRESLTSFGNGPLSAGGPGKPGGGGGGSGSSSMSRGEMSL
AEVQCHLDKEGASNLVIDLIMNASSDRVFHESILLAIALLEGGNTTIQHSFFCRLTEDKK
SEKFFKVFYDRMKVAQQEIKATVTVNTSDLGNKKKDDEVDRDAPSRKKAKEPTTQITEEV
RDQLLEASAATRKAFTTFRREADPDDHYQPGEGTQATADKAKDDLEMSAVITIMQPILRF
LQLLCENHNRDLQNFLRCQNNKTNYNLVCETLQFLDCICGSTTGGLGLLGLYINEKNVAL
INQTLESLTEYCQGPCHENQNCIATHESNGIDIITALILNDINPLGKKRMDLVLELKNNA
SKLLLAIMESRHDSENAERILYNMRPKELVEVIKKAYMQGEVEFEDGENGEDGAASPRNV
GHNIYILAHQLARHNKELQSMLKPGGQVDGDEALEFYAKHTAQIEIVRLDRTMEQIVFPV
PSICEFLTKESKLRIYYTTERDEQGSKINDFFLRSEDLFNEMNWQKKLRAQPVLYWCARN
MSFWSSISFNLAVLMNLLVAFFYPFKGVRGGTLEPHWSGLLWTAMLISLAIVIALPKPHG
IRALIASTILRLIFSVGLQPTLFLLGAFNVCNKIIFLMSFVGNCGTFTRGYRAMVLDVEF
LYHLLYLVICAMGLFVHEFFYSLLLFDLVYREETLLNVIKSVTRNGRSIILTAVLALILV
YLFSIVGYLFFKDDFILEVDRLPNETAVPETGESLASEFLFSDVCRVESGENCSSPAPRE
ELVPAEETEQDKEHTCETLLMCIVTVLSHGLRSGGGVGDVLRKPSKEEPLFAARVIYDLL
FFFMVIIIVLNLIFGVIIDTFADLRSEKQKKEEILKTTCFICGLERDKFDNKTVTFEEHI
KEEHNMWHYLCFIVLVKVKDSTEYTGPESYVAEMIKERNLDWFPRMRAMSLVSSDSEGEQ
NELRNLQEKLESTMKLVTNLSGQLSELKDQMTEQRKQKQRIGLLGHPPHMNVNPQQPA
Function
Intracellular channel that mediates calcium release from the endoplasmic reticulum following stimulation by inositol 1,4,5-trisphosphate. Involved in the regulation of epithelial secretion of electrolytes and fluid through the interaction with AHCYL1. Plays a role in ER stress-induced apoptosis. Cytoplasmic calcium released from the ER triggers apoptosis by the activation of CaM kinase II, eventually leading to the activation of downstream apoptosis pathways.
Tissue Specificity Widely expressed.
KEGG Pathway
Calcium sig.ling pathway (hsa04020 )
cGMP-PKG sig.ling pathway (hsa04022 )
Phosphatidylinositol sig.ling system (hsa04070 )
Oocyte meiosis (hsa04114 )
Autophagy - animal (hsa04140 )
Apoptosis (hsa04210 )
Cellular senescence (hsa04218 )
Vascular smooth muscle contraction (hsa04270 )
Apelin sig.ling pathway (hsa04371 )
Osteoclast differentiation (hsa04380 )
Gap junction (hsa04540 )
Platelet activation (hsa04611 )
NOD-like receptor sig.ling pathway (hsa04621 )
C-type lectin receptor sig.ling pathway (hsa04625 )
Circadian entrainment (hsa04713 )
Long-term potentiation (hsa04720 )
Retrograde endocan.binoid sig.ling (hsa04723 )
Glutamatergic sy.pse (hsa04724 )
Cholinergic sy.pse (hsa04725 )
Serotonergic sy.pse (hsa04726 )
Dopaminergic sy.pse (hsa04728 )
Long-term depression (hsa04730 )
Inflammatory mediator regulation of TRP channels (hsa04750 )
GnRH sig.ling pathway (hsa04912 )
Estrogen sig.ling pathway (hsa04915 )
Thyroid hormone synthesis (hsa04918 )
Oxytocin sig.ling pathway (hsa04921 )
Glucagon sig.ling pathway (hsa04922 )
Renin secretion (hsa04924 )
Aldosterone synthesis and secretion (hsa04925 )
Cortisol synthesis and secretion (hsa04927 )
Parathyroid hormone synthesis, secretion and action (hsa04928 )
GnRH secretion (hsa04929 )
Cushing syndrome (hsa04934 )
Growth hormone synthesis, secretion and action (hsa04935 )
Salivary secretion (hsa04970 )
Gastric acid secretion (hsa04971 )
Pancreatic secretion (hsa04972 )
Alzheimer disease (hsa05010 )
Parkinson disease (hsa05012 )
Huntington disease (hsa05016 )
Spinocerebellar ataxia (hsa05017 )
Prion disease (hsa05020 )
Pathways of neurodegeneration - multiple diseases (hsa05022 )
Shigellosis (hsa05131 )
Human cytomegalovirus infection (hsa05163 )
Kaposi sarcoma-associated herpesvirus infection (hsa05167 )
Human immunodeficiency virus 1 infection (hsa05170 )
Proteoglycans in cancer (hsa05205 )
Lipid and atherosclerosis (hsa05417 )
Reactome Pathway
Effects of PIP2 hydrolysis (R-HSA-114508 )
Elevation of cytosolic Ca2+ levels (R-HSA-139853 )
DAG and IP3 signaling (R-HSA-1489509 )
Role of phospholipids in phagocytosis (R-HSA-2029485 )
FCERI mediated Ca+2 mobilization (R-HSA-2871809 )
Glucagon-like Peptide-1 (GLP1) regulates insulin secretion (R-HSA-381676 )
Ca2+ pathway (R-HSA-4086398 )
cGMP effects (R-HSA-418457 )
Regulation of insulin secretion (R-HSA-422356 )
VEGFR2 mediated cell proliferation (R-HSA-5218921 )
Ion homeostasis (R-HSA-5578775 )
CLEC7A (Dectin-1) induces NFAT activation (R-HSA-5607763 )
FCGR3A-mediated IL10 synthesis (R-HSA-9664323 )
Antigen activates B Cell Receptor (BCR) leading to generation of second messengers (R-HSA-983695 )
PLC beta mediated events (R-HSA-112043 )

Molecular Interaction Atlas (MIA) of This DOT

3 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Aniridia-cerebellar ataxia-intellectual disability syndrome DIS4QZ3S Definitive Autosomal dominant [1]
Spinocerebellar ataxia type 29 DISAST24 Definitive Autosomal dominant [1]
Spinocerebellar ataxia type 15/16 DISTNCLR Strong Autosomal dominant [2]
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Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Etoposide DMNH3PG Approved Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1) affects the response to substance of Etoposide. [35]
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5 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 Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [3]
Arsenic DMTL2Y1 Approved Arsenic affects the methylation of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [8]
Procaine DM4LSNE Approved Procaine increases the phosphorylation of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [22]
TAK-243 DM4GKV2 Phase 1 TAK-243 affects the sumoylation of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [29]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the methylation of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [32]
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32 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Tretinoin DM49DUI Approved Tretinoin decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [4]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [5]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [6]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [7]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [9]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [10]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [11]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [12]
Vorinostat DMWMPD4 Approved Vorinostat increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [13]
Testosterone DM7HUNW Approved Testosterone decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [12]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [14]
Phenobarbital DMXZOCG Approved Phenobarbital affects the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [15]
Dexamethasone DMMWZET Approved Dexamethasone increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [16]
Demecolcine DMCZQGK Approved Demecolcine increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [17]
Ethanol DMDRQZU Approved Ethanol increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [18]
Sodium lauryl sulfate DMLJ634 Approved Sodium lauryl sulfate increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [19]
Dasatinib DMJV2EK Approved Dasatinib increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [20]
Bexarotene DMOBIKY Approved Bexarotene increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [21]
Urethane DM7NSI0 Phase 4 Urethane increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [23]
SNDX-275 DMH7W9X Phase 3 SNDX-275 increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [24]
Resveratrol DM3RWXL Phase 3 Resveratrol increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [16]
Genistein DM0JETC Phase 2/3 Genistein increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [25]
phorbol 12-myristate 13-acetate DMJWD62 Phase 2 phorbol 12-myristate 13-acetate decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [26]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [27]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [28]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [30]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [25]
EMODIN DMAEDQG Terminated EMODIN decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [31]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [33]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [17]
Coumestrol DM40TBU Investigative Coumestrol decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [7]
Glyphosate DM0AFY7 Investigative Glyphosate decreases the expression of Inositol 1,4,5-trisphosphate receptor type 1 (ITPR1). [34]
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⏷ Show the Full List of 32 Drug(s)

References

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23 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
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