Phosphatidylinositol 3-kinase regulatory subunit alpha

A phosphatidylinositol 3-kinase regulatory subunit alpha that is encoded in the genome of human. [PRO:DNx]

Synonyms

PI3-kinase regulatory subunit alpha;
PI3K regulatory subunit alpha;
PtdIns-3-kinase regulatory subunit alpha;
Phosphatidylinositol 3-kinase 85 kDa regulatory subunit alpha;
PI3-kinase subunit p85-alpha;
PtdIns-3-kinase regulatory subu

Research

Bioassay Publications (59)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	7 (11.86)	29.6817
2010's	42 (71.19)	24.3611
2020's	10 (16.95)	2.80

Compounds (34)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one	Homo sapiens (human)	IC50	3.1638	2	5
vorinostat	Homo sapiens (human)	IC50	10.0000	1	1
whi p180	Homo sapiens (human)	IC50	0.0020	1	1
wortmannin	Homo sapiens (human)	IC50	16,333.5438	6	9
quercetin	Homo sapiens (human)	IC50	3.8000	1	1
panobinostat	Homo sapiens (human)	IC50	10.0000	1	1
nu 7026	Homo sapiens (human)	IC50	13.0000	1	1
pi103	Homo sapiens (human)	IC50	0.0114	9	9
PI3-Kinase alpha Inhibitor 2	Homo sapiens (human)	IC50	0.0080	1	1
tgx 221	Homo sapiens (human)	IC50	2.7210	3	3
ic 87114	Homo sapiens (human)	IC50	0.1300	1	1
ic 87114	Homo sapiens (human)	Ki	0.0163	1	2
tg100-115	Homo sapiens (human)	IC50	0.7045	2	8
idelalisib	Homo sapiens (human)	IC50	1.5770	19	19
zstk474	Homo sapiens (human)	IC50	0.0049	4	4
dactolisib	Homo sapiens (human)	IC50	0.1532	16	16
buparlisib	Homo sapiens (human)	IC50	0.0878	5	5
gdc 0941	Homo sapiens (human)	IC50	0.6252	11	18
gsk 2126458	Homo sapiens (human)	IC50	0.0000	1	1
gsk 2126458	Homo sapiens (human)	Ki	0.0002	3	3
azd2014	Homo sapiens (human)	IC50	3.8000	1	1
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol	Homo sapiens (human)	IC50	5.5770	1	1
4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester	Homo sapiens (human)	IC50	0.5152	1	2
vs-5584	Homo sapiens (human)	IC50	0.0078	1	1
etp-46321	Homo sapiens (human)	IC50	0.0023	2	2
etp-46321	Homo sapiens (human)	Ki	0.0622	9	9
torin 1	Homo sapiens (human)	IC50	0.4070	2	2
ipi-145	Homo sapiens (human)	IC50	1.4450	8	5
pf-4989216	Homo sapiens (human)	IC50	0.0481	3	3
torin 2	Homo sapiens (human)	IC50	0.0111	2	2
azd8186	Homo sapiens (human)	IC50	0.1630	3	3
hs-173	Homo sapiens (human)	IC50	0.0310	3	3
cudc-907	Homo sapiens (human)	IC50	0.0712	9	9
byl719	Homo sapiens (human)	IC50	0.7672	5	5
amg 511	Homo sapiens (human)	Ki	0.0040	4	4
vx-970	Homo sapiens (human)	Ki	0.1400	1	1
bay 80-6946	Homo sapiens (human)	IC50	0.0016	3	3

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
zstk474	Homo sapiens (human)	EC50	0.0500	2	2
dactolisib	Homo sapiens (human)	EC50	0.0400	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one	Homo sapiens (human)	INH	0.0160	1	1

Enables

This protein enables 19 target(s):

Target	Category	Definition
phosphotyrosine residue binding	molecular function	Binding to a phosphorylated tyrosine residue within a protein. [PMID:14636584]
transmembrane receptor protein tyrosine kinase adaptor activity	molecular function	The binding activity of a molecule that brings together a transmembrane receptor protein tyrosine kinase and one or more other molecules, permitting them to function in a coordinated way. [GOC:mtg_MIT_16mar07, PMID:10502414, PMID:20565848]
insulin receptor binding	molecular function	Binding to an insulin receptor. [GOC:ai]
insulin-like growth factor receptor binding	molecular function	Binding to an insulin-like growth factor receptor. [GOC:jl]
neurotrophin TRKA receptor binding	molecular function	Binding to a neurotrophin TRKA receptor. [GOC:ai]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
kinase activator activity	molecular function	Binds to and increases the activity of a kinase, an enzyme which catalyzes of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:ai]
protein phosphatase binding	molecular function	Binding to a protein phosphatase. [GOC:jl]
phosphatidylinositol 3-kinase regulator activity	molecular function	Modulates the activity of a phosphatidylinositol 3-kinase (PI3K). Regulatory subunits can link a PI3K catalytic subunit to upstream signaling events and help position the catalytic subunits close to their lipid substrates. [GOC:bf, PMID:9255069]
phosphatidylinositol 3-kinase regulatory subunit binding	molecular function	Binding to a regulatory subunit of phosphatidylinositol 3-kinase. The regulatory subunit associates with the catalytic subunit to regulate both its activity and subcellular location. [GOC:bf, PMID:20505341]
ErbB-3 class receptor binding	molecular function	Binding to the protein-tyrosine kinase receptor ErbB-3/HER3. [GOC:jl]
phosphatidylinositol 3-kinase binding	molecular function	Binding to a phosphatidylinositol 3-kinase, any enzyme that catalyzes the addition of a phosphate group to an inositol lipid at the 3' position of the inositol ring. [PMID:10209156, PMID:9255069]
insulin binding	molecular function	Binding to insulin, a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [ISBN:0198506732]
insulin receptor substrate binding	molecular function	Binding to an insulin receptor substrate (IRS) protein, an adaptor protein that bind to the transphosphorylated insulin and insulin-like growth factor receptors, are themselves phosphorylated and in turn recruit SH2 domain-containing signaling molecules to form a productive signaling complex. [PMID:12829233]
protein heterodimerization activity	molecular function	Binding to a nonidentical protein to form a heterodimer. [GOC:ai]
phosphatidylinositol kinase activity	molecular function	Catalysis of the reaction: ATP + a phosphatidylinositol = ADP + a phosphatidylinositol phosphate. [GOC:ai]
enzyme-substrate adaptor activity	molecular function	An adaptor that brings together an enzyme and its substrate. Adaptors recruit the substrate to its enzyme, thus contributing to substrate selection and specificity. [PMID:16250895, PMID:34358446]
phosphatidylinositol 3-kinase activator activity	molecular function	Binds to and increases the activity of a phosphatidylinositol 3-kinase (PI3K). [PMID:31686003]
1-phosphatidylinositol-3-kinase regulator activity	molecular function	Modulates the activity of the enzyme 1-phosphatidylinositol-3-kinase activity. [GOC:ai]

Located In

This protein is located in 9 target(s):

Target	Category	Definition
nucleus	cellular component	A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
cytoplasm	cellular component	The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
cis-Golgi network	cellular component	The network of interconnected tubular and cisternal structures located at the convex side of the Golgi apparatus, which abuts the endoplasmic reticulum. [ISBN:0198506732, ISBN:0815316194]
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]
cell-cell junction	cellular component	A cell junction that forms a connection between two or more cells of an organism; excludes direct cytoplasmic intercellular bridges, such as ring canals in insects. [GOC:aruk, GOC:bc, GOC:dgh, GOC:hb, GOC:mah, PMID:21422226, PMID:28096264]
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]
perinuclear region of cytoplasm	cellular component	Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid]
perinuclear endoplasmic reticulum membrane	cellular component	The membrane of the perinuclear endoplasmic reticulum, which is the portion of endoplasmic reticulum, the intracellular network of tubules and cisternae, that occurs near the nucleus. [PMID:25454947]

Part Of

This protein is part of 2 target(s):

Target	Category	Definition
phosphatidylinositol 3-kinase complex, class IA	cellular component	A class I phosphatidylinositol 3-kinase complex that possesses 1-phosphatidylinositol-4-phosphate 3-kinase activity; comprises a catalytic class IA phosphoinositide 3-kinase (PI3K) subunit and an associated SH2 domain-containing regulatory subunit that is a member of a family of related proteins often called p85 proteins. Through the interaction with the SH2-containing adaptor subunits, Class IA PI3K catalytic subunits are linked to tyrosine kinase signaling pathways. [PMID:9255069, PMID:9759495]
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 40 target(s):

Target	Category	Definition
intracellular glucose homeostasis	biological process	A homeostatic process involved in the maintenance of a steady state level of glucose within a cell. [GOC:dph, GOC:go_curators, GOC:tb]
negative regulation of cell-matrix adhesion	biological process	Any process that stops, prevents, or reduces the rate or extent of cell adhesion to the extracellular matrix. [GOC:hjd]
positive regulation of leukocyte migration	biological process	Any process that activates or increases the frequency, rate, or extent of leukocyte migration. [GOC:add]
transcription by RNA polymerase II	biological process	The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382]
protein import into nucleus	biological process	The directed movement of a protein from the cytoplasm to the nucleus. [GOC:jl]
immune response	biological process	Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add]
extrinsic apoptotic signaling pathway via death domain receptors	biological process	The series of molecular signals in which a signal is conveyed from the cell surface to trigger the apoptotic death of a cell. The pathway starts with a ligand binding to a death domain receptor on the cell surface, and ends when the execution phase of apoptosis is triggered. [GOC:mah, GOC:mtg_apoptosis]
intrinsic apoptotic signaling pathway in response to DNA damage	biological process	The series of molecular signals in which an intracellular signal is conveyed to trigger the apoptotic death of a cell. The pathway is induced by the detection of DNA damage, and ends when the execution phase of apoptosis is triggered. [GOC:go_curators, GOC:mtg_apoptosis]
positive regulation of lamellipodium assembly	biological process	Any process that increases the rate, frequency or extent of the formation of a lamellipodium, a thin sheetlike extension of the surface of a migrating cell. [GOC:dph, GOC:tb]
cytokine-mediated signaling pathway	biological process	The series of molecular signals initiated by the binding of a cytokine to a receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, PMID:19295629]
B cell differentiation	biological process	The process in which a precursor cell type acquires the specialized features of a B cell. A B cell is a lymphocyte of B lineage with the phenotype CD19-positive and capable of B cell mediated immunity. [GO_REF:0000022, GOC:mah]
T cell differentiation	biological process	The process in which a precursor cell type acquires characteristics of a more mature T-cell. A T cell is a type of lymphocyte whose definin characteristic is the expression of a T cell receptor complex. [GO_REF:0000022, GOC:jid, GOC:mah]
osteoclast differentiation	biological process	The process in which a relatively unspecialized monocyte acquires the specialized features of an osteoclast. An osteoclast is a specialized phagocytic cell associated with the absorption and removal of the mineralized matrix of bone tissue. [CL:0000092, GOC:add, ISBN:0781735149, PMID:12161749]
positive regulation of tumor necrosis factor production	biological process	Any process that activates or increases the frequency, rate or extent of tumor necrosis factor production. [GO_REF:0000058, GOC:TermGenie, PMID:10891884, PMID:15560120]
cellular response to insulin stimulus	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 an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732]
positive regulation of RNA splicing	biological process	Any process that activates or increases the frequency, rate or extent of RNA splicing. [GOC:mah]
regulation of toll-like receptor 4 signaling pathway	biological process	Any process that modulates the frequency, rate, or extent of toll-like receptor 4 signaling pathway. [GOC:add, PMID:16551253, PMID:17328678]
substrate adhesion-dependent cell spreading	biological process	The morphogenetic process that results in flattening of a cell as a consequence of its adhesion to a substrate. [GOC:mah, GOC:pf, PMID:17050732]
cellular response to UV	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 an ultraviolet radiation (UV light) stimulus. Ultraviolet radiation is electromagnetic radiation with a wavelength in the range of 10 to 380 nanometers. [GOC:mah]
response to endoplasmic reticulum stress	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 a stress acting at the endoplasmic reticulum. ER stress usually results from the accumulation of unfolded or misfolded proteins in the ER lumen. [GOC:cjm, GOC:mah]
interleukin-18-mediated signaling pathway	biological process	The series of molecular signals initiated by interleukin-18 binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:BHF, GOC:signaling]
natural killer cell mediated cytotoxicity	biological process	The directed killing of a target cell by a natural killer cell through the release of granules containing cytotoxic mediators or through the engagement of death receptors. [GOC:add, GOC:pr]
positive regulation of protein import into nucleus	biological process	Any process that activates or increases the frequency, rate or extent of movement of proteins from the cytoplasm into the nucleus. [GOC:jl]
negative regulation of apoptotic process	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
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]
negative regulation of osteoclast differentiation	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of osteoclast differentiation. [GOC:go_curators]
positive regulation of transcription by RNA polymerase II	biological process	Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
positive regulation of glucose import	biological process	Any process that activates or increases the frequency, rate or extent of the import of the hexose monosaccharide glucose into a cell or organelle. [GOC:ai, GOC:dph, GOC:tb]
phosphatidylinositol phosphate biosynthetic process	biological process	The chemical reactions and pathways resulting in the formation of phosphatidylinositol phosphate. [ISBN:0198506732]
insulin-like growth factor receptor signaling pathway	biological process	The series of molecular signals initiated by a ligand binding to an insulin-like growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb]
positive regulation of smooth muscle cell proliferation	biological process	Any process that activates or increases the rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc]
protein stabilization	biological process	Any process involved in maintaining the structure and integrity of a protein and preventing it from degradation or aggregation. [GOC:ai]
positive regulation of filopodium assembly	biological process	Any process that activates or increases the frequency, rate or extent of the assembly of a filopodium, a thin, stiff protrusion extended by the leading edge of a motile cell such as a crawling fibroblast or amoeba, or an axonal growth cone. [GOC:ai, GOC:dph, GOC:tb]
negative regulation of stress fiber assembly	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of the assembly a stress fiber, a bundle of microfilaments and other proteins found in fibroblasts. [GOC:ai]
growth hormone receptor signaling pathway	biological process	The series of molecular signals generated as a consequence of growth hormone receptor binding to its physiological ligand. [GOC:BHF, GOC:dph, PMID:11445442]
myeloid leukocyte migration	biological process	The movement of a myeloid leukocyte within or between different tissues and organs of the body. [GOC:cvs, PMID:22342843, PMID:24157461]
positive regulation of focal adhesion disassembly	biological process	Any process that activates or increases the frequency, rate or extent of disaggregation of a focal adhesion into its constituent components. [PMID:25490267]
positive regulation of endoplasmic reticulum unfolded protein response	biological process	Any process that activates or increases the frequency, rate or extent of endoplasmic reticulum unfolded protein response. [GOC:TermGenie]
positive regulation of protein localization to plasma membrane	biological process	Any process that activates or increases the frequency, rate or extent of protein localization to plasma membrane. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:11602640]
insulin receptor signaling pathway	biological process	The series of molecular signals generated as a consequence of the insulin receptor binding to insulin. [GOC:ceb]