Proteins > Phosphatidylinositol 3-kinase catalytic subunit type 3
Page last updated: 2024-08-08 00:04:26
Phosphatidylinositol 3-kinase catalytic subunit type 3
A phosphatidylinositol 3-kinase catalytic subunit type 3 that is encoded in the genome of human. [PRO:DNx]
Synonyms
PI3-kinase type 3;
PI3K type 3;
PtdIns-3-kinase type 3;
EC 2.7.1.137;
Phosphatidylinositol 3-kinase p100 subunit;
Phosphoinositide-3-kinase class 3;
hVps34
Research
Bioassay Publications (19)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (5.26) | 29.6817 |
| 2010's | 17 (89.47) | 24.3611 |
| 2020's | 1 (5.26) | 2.80 |
Compounds (23)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ML162 | Homo sapiens (human) | IC50 | 0.0215 | 2 | 2 |
| PI3-Kinase alpha Inhibitor 2 | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
| idelalisib | Homo sapiens (human) | IC50 | 327.7990 | 3 | 3 |
| zstk474 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| dactolisib | Homo sapiens (human) | IC50 | 0.4500 | 1 | 1 |
| ku 60019 | Homo sapiens (human) | IC50 | 0.0170 | 1 | 1 |
| buparlisib | Homo sapiens (human) | IC50 | 2.4905 | 2 | 2 |
| gdc 0941 | Homo sapiens (human) | IC50 | 11.3627 | 3 | 10 |
| gdc 0980 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| ch 5132799 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| torin 1 | Homo sapiens (human) | IC50 | 0.5330 | 1 | 1 |
| gdc-0032 | Homo sapiens (human) | IC50 | 0.3740 | 2 | 1 |
| spautin-1 | Homo sapiens (human) | IC50 | 0.7400 | 1 | 1 |
| torin 2 | Homo sapiens (human) | IC50 | 0.0086 | 1 | 1 |
| cudc-907 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sar245408 | Homo sapiens (human) | IC50 | 7.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | IC50 | 9.1000 | 1 | 1 |
| amg 511 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sar405 | Homo sapiens (human) | IC50 | 0.0076 | 4 | 4 |
Drugs with Activation Measurements
Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 2011
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust iJournal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
[no title available],
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| kinase activity | molecular function | Catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [ISBN:0198506732] |
| 1-phosphatidylinositol-3-kinase activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol + ATP = a 1-phosphatidyl-1D-myo-inositol 3-phosphate + ADP + 2 H+. [EC:2.7.1.137, RHEA:12709] |
| phosphatidylinositol kinase activity | molecular function | Catalysis of the reaction: ATP + a phosphatidylinositol = ADP + a phosphatidylinositol phosphate. [GOC:ai] |
Located In
This protein is located in 8 target(s):
| Target | Category | Definition |
|---|
| late endosome | cellular component | A prelysosomal endocytic organelle differentiated from early endosomes by lower lumenal pH and different protein composition. Late endosomes are more spherical than early endosomes and are mostly juxtanuclear, being concentrated near the microtubule organizing center. [NIF_Subcellular:nlx_subcell_20090702, PMID:11964142, PMID:2557062] |
| autophagosome | cellular component | A double-membrane-bounded compartment that engulfs endogenous cellular material as well as invading microorganisms to target them to the lytic vacuole/lysosome for degradation as part of macroautophagy. [GOC:autophagy, ISBN:0198547684, PMID:11099404] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| axoneme | cellular component | The bundle of microtubules and associated proteins that forms the core of cilia (also called flagella) in eukaryotic cells and is responsible for their movements. [GOC:bf, GOC:cilia, ISBN:0198547684] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| midbody | cellular component | A thin cytoplasmic bridge formed between daughter cells at the end of cytokinesis. The midbody forms where the contractile ring constricts, and may persist for some time before finally breaking to complete cytokinesis. [ISBN:0815316194] |
| phagocytic vesicle membrane | cellular component | The lipid bilayer surrounding a phagocytic vesicle. [GOC:mah] |
| autolysosome | cellular component | A type of secondary lysosome in which a primary lysosome has fused with the outer membrane of an autophagosome or amphisome. It is involved in the second step of autophagy in which it degrades contents with acidic lysosomal hydrolases. [GOC:sart, NIF_Subcellular:sao8444068431, PMID:19008921, PMID:24657946] |
Active In
This protein is active in 5 target(s):
| Target | Category | Definition |
|---|
| peroxisome | cellular component | A small organelle enclosed by a single membrane, and found in most eukaryotic cells. Contains peroxidases and other enzymes involved in a variety of metabolic processes including free radical detoxification, lipid catabolism and biosynthesis, and hydrogen peroxide metabolism. [GOC:pm, PMID:9302272, UniProtKB-KW:KW-0576] |
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| phagophore assembly site | cellular component | Punctate structures proximal to the endoplasmic reticulum which are the sites where the Atg machinery assembles upon autophagy induction. [GOC:elh, PMID:11689437, PMID:12048214, PMID:12554655] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| phosphatidylinositol 3-kinase complex, class III | cellular component | A phosphatidylinositol 3-kinase complex that contains a catalytic class III phosphoinositide 3-kinase (PI3K) subunit bound to a regulatory (adaptor) subunit. Additional adaptor proteins may be present. Class III PI3Ks have a substrate specificity restricted to phosphatidylinositol (PI). [GOC:bf, PMID:9255069] |
| phosphatidylinositol 3-kinase complex, class III, type II | cellular component | A class III phosphatidylinositol 3-kinase complex that is involved in vacuolar protein sorting (VPS) via endosomes. In budding yeast, this complex consists of Vps30p, Vps34p, Vps38 and Vps15p. [GOC:ha, GOC:rb, PMID:11157979, PMID:16421251] |
| phosphatidylinositol 3-kinase complex, class III, type I | cellular component | A class III phosphatidylinositol 3-kinase complex that is involved in autophagy. In budding yeast, this complex consists of Vps30p, Vps34p, Apg14p and Vps15p. [GOC:ha, GOC:rb, PMID:11157979, PMID:16421251] |
Involved In
This protein is involved in 17 target(s):
| Target | Category | Definition |
|---|
| autophagosome assembly | biological process | The formation of a double membrane-bounded structure, the autophagosome, that occurs when a specialized membrane sac, called the isolation membrane, starts to enclose a portion of the cytoplasm. [GOC:autophagy, PMID:9412464] |
| protein targeting to lysosome | biological process | The process of directing proteins towards the lysosome using signals contained within the protein. [GOC:curators] |
| regulation of autophagy | biological process | Any process that modulates the frequency, rate or extent of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| macroautophagy | biological process | The autophagic process that proceeds via the formation of an autophagosome. [PMID:24366339] |
| regulation of macroautophagy | biological process | Any process that modulates the frequency, rate or extent of macroautophagy. [GOC:krc] |
| regulation of cytokinesis | biological process | Any process that modulates the frequency, rate or extent of the division of the cytoplasm of a cell and its separation into two daughter cells. [GOC:mah] |
| protein localization to phagophore assembly site | biological process | Any process in which a protein is transported to, or maintained at, the phagophore assembly site (PAS). [GOC:rb] |
| phosphatidylinositol-3-phosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of phosphatidylinositol-3-phosphate, a phosphatidylinositol monophosphate carrying the phosphate group at the 3-position. [GOC:al, GOC:vw] |
| cellular response to glucose starvation | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of deprivation of glucose. [GOC:jl] |
| positive regulation by host of viral genome replication | biological process | A process in which a host organism activates or increases the frequency, rate or extent of viral genome replication. [GOC:jl] |
| early endosome to late endosome transport | biological process | The directed movement of substances, in membrane-bounded vesicles, from the early sorting endosomes to the late sorting endosomes; transport occurs along microtubules and can be experimentally blocked with microtubule-depolymerizing drugs. [ISBN:0815316194, PMID:29980602] |
| phosphatidylinositol phosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of phosphatidylinositol phosphate. [ISBN:0198506732] |
| cell division | biological process | The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr] |
| autophagosome maturation | biological process | Removal of PI3P and Atg8/LC3 after the closure of the phagophore and before the fusion with the endosome/lysosome (e.g. mammals and insects) or vacuole (yeast), and that very likely destabilizes other Atg proteins and thus enables their efficient dissociation and recycling. [GOC:autophagy, GOC:lf, PMID:28077293] |
| autophagy of peroxisome | biological process | The process in which peroxisomes are delivered to a type of vacuole and degraded in response to changing nutrient conditions. [GOC:autophagy, PMID:10547367, PMID:20083110] |
| endocytosis | biological process | A vesicle-mediated transport process in which cells take up external materials or membrane constituents by the invagination of a part of the plasma membrane to form a new membrane-bounded vesicle. [GOC:mah, ISBN:0198506732, ISBN:0716731363, Wikipedia:Endocytosis] |
| phosphatidylinositol-mediated signaling | biological process | The series of molecular signals in which a cell uses a phosphatidylinositol-mediated signaling to convert a signal into a response. Phosphatidylinositols include phosphatidylinositol (PtdIns) and its phosphorylated derivatives. [GOC:bf, GOC:ceb, ISBN:0198506732] |