Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT9H4P3)

DTT Name PI3K p110 beta messenger RNA (PIK3CB mRNA)
Synonyms
p110beta (mRNA); PtdIns3kinase subunit p110beta (mRNA); PtdIns3kinase subunit beta (mRNA); PtdIns-3-kinase subunit p110-beta (mRNA); PtdIns-3-kinase subunit beta (mRNA); Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunitbeta isoform (mRNA); Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalyticsubunit beta (mRNA); Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (mRNA); Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta (mRNA); PIK3C1 (mRNA); PI3kinase subunit beta (mRNA); PI3Kbeta (mRNA); PI3K-beta (mRNA); PI3-kinase subunit beta (mRNA)
Gene Name PIK3CB
DTT Type
Literature-reported target
 [1]
BioChemical Class
mRNA target
UniProt ID
PK3CB_HUMAN
TTD ID
T95594
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
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EC Number
EC 2.7.1.153
Sequence
MCFSFIMPPAMADILDIWAVDSQIASDGSIPVDFLLPTGIYIQLEVPREATISYIKQMLW
KQVHNYPMFNLLMDIDSYMFACVNQTAVYEELEDETRRLCDVRPFLPVLKLVTRSCDPGE
KLDSKIGVLIGKGLHEFDSLKDPEVNEFRRKMRKFSEEKILSLVGLSWMDWLKQTYPPEH
EPSIPENLEDKLYGGKLIVAVHFENCQDVFSFQVSPNMNPIKVNELAIQKRLTIHGKEDE
VSPYDYVLQVSGRVEYVFGDHPLIQFQYIRNCVMNRALPHFILVECCKIKKMYEQEMIAI
EAAINRNSSNLPLPLPPKKTRIISHVWENNNPFQIVLVKGNKLNTEETVKVHVRAGLFHG
TELLCKTIVSSEVSGKNDHIWNEPLEFDINICDLPRMARLCFAVYAVLDKVKTKKSTKTI
NPSKYQTIRKAGKVHYPVAWVNTMVFDFKGQLRTGDIILHSWSSFPDELEEMLNPMGTVQ
TNPYTENATALHVKFPENKKQPYYYPPFDKIIEKAAEIASSDSANVSSRGGKKFLPVLKE
ILDRDPLSQLCENEMDLIWTLRQDCREIFPQSLPKLLLSIKWNKLEDVAQLQALLQIWPK
LPPREALELLDFNYPDQYVREYAVGCLRQMSDEELSQYLLQLVQVLKYEPFLDCALSRFL
LERALGNRRIGQFLFWHLRSEVHIPAVSVQFGVILEAYCRGSVGHMKVLSKQVEALNKLK
TLNSLIKLNAVKLNRAKGKEAMHTCLKQSAYREALSDLQSPLNPCVILSELYVEKCKYMD
SKMKPLWLVYNNKVFGEDSVGVIFKNGDDLRQDMLTLQMLRLMDLLWKEAGLDLRMLPYG
CLATGDRSGLIEVVSTSETIADIQLNSSNVAAAAAFNKDALLNWLKEYNSGDDLDRAIEE
FTLSCAGYCVASYVLGIGDRHSDNIMVKKTGQLFHIDFGHILGNFKSKFGIKRERVPFIL
TYDFIHVIQQGKTGNTEKFGRFRQCCEDAYLILRRHGNLFITLFALMLTAGLPELTSVKD
IQYLKDSLALGKSEEEALKQFKQKFDEALRESWTTKVNWMAHTVRKDYRS
Function
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Involved in the activation of AKT1 upon stimulation by G-protein coupled receptors (GPCRs) ligands such as CXCL12, sphingosine 1-phosphate, and lysophosphatidic acid. May also act downstream receptor tyrosine kinases. Required in different signaling pathways for stable platelet adhesion and aggregation. Plays a role in platelet activation signaling triggered by GPCRs, alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) and ITAM (immunoreceptor tyrosine-based activation motif)-bearing receptors such as GP6. Regulates the strength of adhesion of ITGA2B/ ITGB3 activated receptors necessary for the cellular transmission of contractile forces. Required for platelet aggregation induced by F2 (thrombin) and thromboxane A2 (TXA2). Has a role in cell survival. May have a role in cell migration. Involved in the early stage of autophagosome formation. Modulates the intracellular level of PtdIns3P (Phosphatidylinositol 3-phosphate) and activates PIK3C3 kinase activity. May act as a scaffold, independently of its lipid kinase activity to positively regulate autophagy. May have a role in insulin signaling as scaffolding protein in which the lipid kinase activity is not required. May have a kinase-independent function in regulating cell proliferation and in clathrin-mediated endocytosis. Mediator of oncogenic signal in cell lines lacking PTEN. The lipid kinase activity is necessary for its role in oncogenic transformation. Required for the growth of ERBB2 and RAS driven tumors.
KEGG Pathway
Inositol phosphate metabolism (hsa00562 )
ErbB signaling pathway (hsa04012 )
Ras signaling pathway (hsa04014 )
Rap1 signaling pathway (hsa04015 )
cGMP-PKG signaling pathway (hsa04022 )
cAMP signaling pathway (hsa04024 )
Chemokine signaling pathway (hsa04062 )
HIF-1 signaling pathway (hsa04066 )
FoxO signaling pathway (hsa04068 )
Phosphatidylinositol signaling system (hsa04070 )
Sphingolipid signaling pathway (hsa04071 )
mTOR signaling pathway (hsa04150 )
PI3K-Akt signaling pathway (hsa04151 )
AMPK signaling pathway (hsa04152 )
Apoptosis (hsa04210 )
Adrenergic signaling in cardiomyocytes (hsa04261 )
VEGF signaling pathway (hsa04370 )
Osteoclast differentiation (hsa04380 )
Focal adhesion (hsa04510 )
Signaling pathways regulating pluripotency of stem cells (hsa04550 )
Platelet activation (hsa04611 )
Toll-like receptor signaling pathway (hsa04620 )
Jak-STAT signaling pathway (hsa04630 )
Natural killer cell mediated cytotoxicity (hsa04650 )
T cell receptor signaling pathway (hsa04660 )
B cell receptor signaling pathway (hsa04662 )
Fc epsilon RI signaling pathway (hsa04664 )
Fc gamma R-mediated phagocytosis (hsa04666 )
TNF signaling pathway (hsa04668 )
Leukocyte transendothelial migration (hsa04670 )
Neurotrophin signaling pathway (hsa04722 )
Cholinergic synapse (hsa04725 )
Inflammatory mediator regulation of TRP channels (hsa04750 )
Regulation of actin cytoskeleton (hsa04810 )
Insulin signaling pathway (hsa04910 )
Progesterone-mediated oocyte maturation (hsa04914 )
Estrogen signaling pathway (hsa04915 )
Prolactin signaling pathway (hsa04917 )
Thyroid hormone signaling pathway (hsa04919 )
Oxytocin signaling pathway (hsa04921 )
Regulation of lipolysis in adipocytes (hsa04923 )
Type II diabetes mellitus (hsa04930 )
Non-alcoholic fatty liver disease (NAFLD) (hsa04932 )
Aldosterone-regulated sodium reabsorption (hsa04960 )
Carbohydrate digestion and absorption (hsa04973 )
Bacterial invasion of epithelial cells (hsa05100 )
Chagas disease (American trypanosomiasis) (hsa05142 )
Toxoplasmosis (hsa05145 )
Amoebiasis (hsa05146 )
Hepatitis C (hsa05160 )
Hepatitis B (hsa05161 )
Measles (hsa05162 )
Influenza A (hsa05164 )
HTLV-I infection (hsa05166 )
Epstein-Barr virus infection (hsa05169 )
Pathways in cancer (hsa05200 )
Viral carcinogenesis (hsa05203 )
Proteoglycans in cancer (hsa05205 )
Colorectal cancer (hsa05210 )
Renal cell carcinoma (hsa05211 )
Pancreatic cancer (hsa05212 )
Endometrial cancer (hsa05213 )
Glioma (hsa05214 )
Prostate cancer (hsa05215 )
Melanoma (hsa05218 )
Chronic myeloid leukemia (hsa05220 )
Acute myeloid leukemia (hsa05221 )
Small cell lung cancer (hsa05222 )
Non-small cell lung cancer (hsa05223 )
Central carbon metabolism in cancer (hsa05230 )
Choline metabolism in cancer (hsa05231 )
Reactome Pathway
GPVI-mediated activation cascade (R-HSA-114604 )
PIP3 activates AKT signaling (R-HSA-1257604 )
PI3K/AKT activation (R-HSA-198203 )
Role of phospholipids in phagocytosis (R-HSA-2029485 )
Tie2 Signaling (R-HSA-210993 )
Constitutive Signaling by Aberrant PI3K in Cancer (R-HSA-2219530 )
DAP12 signaling (R-HSA-2424491 )
Role of LAT2/NTAL/LAB on calcium mobilization (R-HSA-2730905 )
Nephrin interactions (R-HSA-373753 )
G beta (R-HSA-392451 )
VEGFA-VEGFR2 Pathway (R-HSA-4420097 )
Interleukin-3, 5 and GM-CSF signaling (R-HSA-512988 )
Interleukin receptor SHC signaling (R-HSA-912526 )
Regulation of signaling by CBL (R-HSA-912631 )
PI3K Cascade (R-HSA-109704 )
BioCyc Pathway
MetaCyc:HS00644-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
22 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
3-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)phenol DM54MDH Discovery agent N.A. Investigative [2]
Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate DM3FH02 Discovery agent N.A. Investigative [3]
ISIS 31963 DMOHZKW Discovery agent N.A. Investigative [1]
ISIS 31982 DMP9IR2 Discovery agent N.A. Investigative [1]
ISIS 31996 DM21ZCQ Discovery agent N.A. Investigative [1]
ISIS 32000 DM0O9WM Discovery agent N.A. Investigative [1]
ISIS 32002 DMEAXV3 Discovery agent N.A. Investigative [1]
ISIS 32003 DM7EVQX Discovery agent N.A. Investigative [1]
ISIS 32004 DME7VX6 Discovery agent N.A. Investigative [1]
ISIS 32005 DMT8GWX Discovery agent N.A. Investigative [1]
ISIS 32006 DMFKLUS Discovery agent N.A. Investigative [1]
ISIS 32008 DME1KXM Discovery agent N.A. Investigative [1]
ISIS 32010 DM8PBCA Discovery agent N.A. Investigative [1]
ISIS 32014 DMF5SK8 Discovery agent N.A. Investigative [1]
ISIS 32015 DMMV4WX Discovery agent N.A. Investigative [1]
ISIS 32020 DMXL9IY Discovery agent N.A. Investigative [1]
ISIS 32021 DMISB5V Discovery agent N.A. Investigative [1]
ISIS 32024 DMPKGIU Discovery agent N.A. Investigative [1]
ISIS 32028 DMATWDO Discovery agent N.A. Investigative [1]
ISIS 32035 DM47B2O Discovery agent N.A. Investigative [1]
ISIS 32039 DMY1R0Q Discovery agent N.A. Investigative [1]
LY-292223 DML36ZE Discovery agent N.A. Investigative [3]
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⏷ Show the Full List of 22 Investigative Drug(s)

References

1 US patent application no. 6,133,032, Antisense modulation of PI3 kinase p110 beta expression.
2 Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007 Sep 1;15(17):5837-44.
3 LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. Bioorg Med Chem Lett. 2001 Apr 9;11(7):909-13.