Proteins > Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta
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Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta
A phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00750]
Synonyms
PI3K-C2-beta;
PtdIns-3-kinase C2 subunit beta;
EC 2.7.1.137;
EC 2.7.1.154;
C2-PI3K;
Phosphoinositide 3-kinase-C2-beta
Research
Bioassay Publications (15)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (33.33) | 29.6817 |
| 2010's | 10 (66.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (83)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 15, Issue:1, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
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
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
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
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
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 (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
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
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
[no title available],
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
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],
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
| 1-phosphatidylinositol-4-phosphate 3-kinase activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4-phosphate + ATP = 1-phosphatidyl-1D-myo-inositol 3,4-bisphosphate + ADP + 2 H+. [EC:2.7.1.154, RHEA:18373] |
| phosphatidylinositol binding | molecular function | Binding to an inositol-containing glycerophospholipid, i.e. phosphatidylinositol (PtdIns) and its phosphorylated derivatives. [GOC:bf, ISBN:0198506732, PMID:11395417] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| 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] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| endocytic vesicle | cellular component | A membrane-bounded intracellular vesicle formed by invagination of the plasma membrane around an extracellular substance. Endocytic vesicles fuse with early endosomes to deliver the cargo for further sorting. [GOC:go_curators, PMID:19696797] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| phosphatidylinositol 3-kinase complex | cellular component | A protein complex capable of phosphatidylinositol 3-kinase activity and containing subunits of any phosphatidylinositol 3-kinase (PI3K) enzyme. These complexes are divided in three classes (called I, II and III) that differ for their presence across taxonomic groups and for the type of their constituents. Catalytic subunits of phosphatidylinositol 3-kinase enzymes are present in all 3 classes; regulatory subunits of phosphatidylinositol 3-kinase enzymes are present in classes I and III; adaptor proteins have been observed in class II complexes and may be present in other classes too. [GOC:bf, PMID:24587488] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| biological_process | biological process | A biological process is the execution of a genetically-encoded biological module or program. It consists of all the steps required to achieve the specific biological objective of the module. A biological process is accomplished by a particular set of molecular functions carried out by specific gene products (or macromolecular complexes), often in a highly regulated manner and in a particular temporal sequence. [GOC:pdt] |
| cellular response to 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 nourishment. [GOC:jl] |
| autophagosome organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of an autophagosome. [GOC:bf, GOC:PARL, GOC:TermGenie, PMID:22186024] |
| cell migration | biological process | The controlled self-propelled movement of a cell from one site to a destination guided by molecular cues. [GOC:cjm, GOC:dph, GOC:ems, GOC:pf, Wikipedia:Cell_migration] |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | An intracellular signaling cassette that starts with phosphatidylinositol 3-kinase (PI3K) activation, production of phosphatidylinositol 3-phosphate (PI3P), activation of PDK1, which recruits and ending with the activation of protein kinase B (PKB, also known as Akt). PI3K is activated by cell surface receptors. Note that PTEN is an inhibitor of the pathway. [PMID:20517722, PMID:22952397] |
| 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] |
| 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] |