8TDU

STX-478, a Mutant-Selective, Allosteric Inhibitor bound to PI3Kalpha

Functional Information from GO Data

Chain	GOid	namespace	contents
A	0001525	biological_process	angiogenesis
A	0001889	biological_process	liver development
A	0001932	biological_process	regulation of protein phosphorylation
A	0001944	biological_process	vasculature development
A	0004674	molecular_function	protein serine/threonine kinase activity
A	0005515	molecular_function	protein binding
A	0005524	molecular_function	ATP binding
A	0005737	cellular_component	cytoplasm
A	0005829	cellular_component	cytosol
A	0005886	cellular_component	plasma membrane
A	0005942	cellular_component	phosphatidylinositol 3-kinase complex
A	0005943	cellular_component	phosphatidylinositol 3-kinase complex, class IA
A	0005944	cellular_component	phosphatidylinositol 3-kinase complex, class IB
A	0006006	biological_process	glucose metabolic process
A	0006629	biological_process	lipid metabolic process
A	0006909	biological_process	phagocytosis
A	0007173	biological_process	epidermal growth factor receptor signaling pathway
A	0008286	biological_process	insulin receptor signaling pathway
A	0010468	biological_process	regulation of gene expression
A	0010592	biological_process	positive regulation of lamellipodium assembly
A	0010629	biological_process	negative regulation of gene expression
A	0014704	cellular_component	intercalated disc
A	0014823	biological_process	response to activity
A	0014870	biological_process	response to muscle inactivity
A	0016242	biological_process	negative regulation of macroautophagy
A	0016301	molecular_function	kinase activity
A	0016303	molecular_function	1-phosphatidylinositol-3-kinase activity
A	0016310	biological_process	phosphorylation
A	0030027	cellular_component	lamellipodium
A	0030036	biological_process	actin cytoskeleton organization
A	0030168	biological_process	platelet activation
A	0030295	molecular_function	protein kinase activator activity
A	0030835	biological_process	negative regulation of actin filament depolymerization
A	0031295	biological_process	T cell costimulation
A	0032008	biological_process	positive regulation of TOR signaling
A	0032869	biological_process	cellular response to insulin stimulus
A	0035005	molecular_function	1-phosphatidylinositol-4-phosphate 3-kinase activity
A	0035994	biological_process	response to muscle stretch
A	0036092	biological_process	phosphatidylinositol-3-phosphate biosynthetic process
A	0038084	biological_process	vascular endothelial growth factor signaling pathway
A	0040014	biological_process	regulation of multicellular organism growth
A	0043201	biological_process	response to L-leucine
A	0043276	biological_process	anoikis
A	0043457	biological_process	regulation of cellular respiration
A	0043491	biological_process	phosphatidylinositol 3-kinase/protein kinase B signal transduction
A	0043524	biological_process	negative regulation of neuron apoptotic process
A	0043542	biological_process	endothelial cell migration
A	0043560	molecular_function	insulin receptor substrate binding
A	0046854	biological_process	phosphatidylinositol phosphate biosynthetic process
A	0046934	molecular_function	1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity
A	0048009	biological_process	insulin-like growth factor receptor signaling pathway
A	0048015	biological_process	phosphatidylinositol-mediated signaling
A	0048471	cellular_component	perinuclear region of cytoplasm
A	0048661	biological_process	positive regulation of smooth muscle cell proliferation
A	0050852	biological_process	T cell receptor signaling pathway
A	0051897	biological_process	positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
A	0055119	biological_process	relaxation of cardiac muscle
A	0060048	biological_process	cardiac muscle contraction
A	0060612	biological_process	adipose tissue development
A	0071333	biological_process	cellular response to glucose stimulus
A	0071464	biological_process	cellular response to hydrostatic pressure
A	0071548	biological_process	response to dexamethasone
A	0086003	biological_process	cardiac muscle cell contraction
A	0097009	biological_process	energy homeostasis
A	0106310	molecular_function	protein serine kinase activity
A	0110053	biological_process	regulation of actin filament organization
A	0141068	biological_process	autosome genomic imprinting
A	1903544	biological_process	response to butyrate
A	1905477	biological_process	positive regulation of protein localization to membrane
A	2000270	biological_process	negative regulation of fibroblast apoptotic process
A	2000811	biological_process	negative regulation of anoikis
C	0001525	biological_process	angiogenesis
C	0001889	biological_process	liver development
C	0001932	biological_process	regulation of protein phosphorylation
C	0001944	biological_process	vasculature development
C	0004674	molecular_function	protein serine/threonine kinase activity
C	0005515	molecular_function	protein binding
C	0005524	molecular_function	ATP binding
C	0005737	cellular_component	cytoplasm
C	0005829	cellular_component	cytosol
C	0005886	cellular_component	plasma membrane
C	0005942	cellular_component	phosphatidylinositol 3-kinase complex
C	0005943	cellular_component	phosphatidylinositol 3-kinase complex, class IA
C	0005944	cellular_component	phosphatidylinositol 3-kinase complex, class IB
C	0006006	biological_process	glucose metabolic process
C	0006629	biological_process	lipid metabolic process
C	0006909	biological_process	phagocytosis
C	0007173	biological_process	epidermal growth factor receptor signaling pathway
C	0008286	biological_process	insulin receptor signaling pathway
C	0010468	biological_process	regulation of gene expression
C	0010592	biological_process	positive regulation of lamellipodium assembly
C	0010629	biological_process	negative regulation of gene expression
C	0014704	cellular_component	intercalated disc
C	0014823	biological_process	response to activity
C	0014870	biological_process	response to muscle inactivity
C	0016242	biological_process	negative regulation of macroautophagy
C	0016301	molecular_function	kinase activity
C	0016303	molecular_function	1-phosphatidylinositol-3-kinase activity
C	0016310	biological_process	phosphorylation
C	0030027	cellular_component	lamellipodium
C	0030036	biological_process	actin cytoskeleton organization
C	0030168	biological_process	platelet activation
C	0030295	molecular_function	protein kinase activator activity
C	0030835	biological_process	negative regulation of actin filament depolymerization
C	0031295	biological_process	T cell costimulation
C	0032008	biological_process	positive regulation of TOR signaling
C	0032869	biological_process	cellular response to insulin stimulus
C	0035005	molecular_function	1-phosphatidylinositol-4-phosphate 3-kinase activity
C	0035994	biological_process	response to muscle stretch
C	0036092	biological_process	phosphatidylinositol-3-phosphate biosynthetic process
C	0038084	biological_process	vascular endothelial growth factor signaling pathway
C	0040014	biological_process	regulation of multicellular organism growth
C	0043201	biological_process	response to L-leucine
C	0043276	biological_process	anoikis
C	0043457	biological_process	regulation of cellular respiration
C	0043491	biological_process	phosphatidylinositol 3-kinase/protein kinase B signal transduction
C	0043524	biological_process	negative regulation of neuron apoptotic process
C	0043542	biological_process	endothelial cell migration
C	0043560	molecular_function	insulin receptor substrate binding
C	0046854	biological_process	phosphatidylinositol phosphate biosynthetic process
C	0046934	molecular_function	1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity
C	0048009	biological_process	insulin-like growth factor receptor signaling pathway
C	0048015	biological_process	phosphatidylinositol-mediated signaling
C	0048471	cellular_component	perinuclear region of cytoplasm
C	0048661	biological_process	positive regulation of smooth muscle cell proliferation
C	0050852	biological_process	T cell receptor signaling pathway
C	0051897	biological_process	positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
C	0055119	biological_process	relaxation of cardiac muscle
C	0060048	biological_process	cardiac muscle contraction
C	0060612	biological_process	adipose tissue development
C	0071333	biological_process	cellular response to glucose stimulus
C	0071464	biological_process	cellular response to hydrostatic pressure
C	0071548	biological_process	response to dexamethasone
C	0086003	biological_process	cardiac muscle cell contraction
C	0097009	biological_process	energy homeostasis
C	0106310	molecular_function	protein serine kinase activity
C	0110053	biological_process	regulation of actin filament organization
C	0141068	biological_process	autosome genomic imprinting
C	1903544	biological_process	response to butyrate
C	1905477	biological_process	positive regulation of protein localization to membrane
C	2000270	biological_process	negative regulation of fibroblast apoptotic process
C	2000811	biological_process	negative regulation of anoikis

Functional Information from PROSITE/UniProt

site_id	PS00915
Number of Residues	15
Details	PI3_4_KINASE_1 Phosphatidylinositol 3- and 4-kinases signature 1. FKng.DDLRQDmltlQ

Chain	Residue	Details
A	PHE801-GLN815

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site_id	PS00916
Number of Residues	21
Details	PI3_4_KINASE_2 Phosphatidylinositol 3- and 4-kinases signature 2. ScAgycVatFILgIgDRHnsN

Chain	Residue	Details
A	SER900-ASN920

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Functional Information from SwissProt/UniProt

site_id	SWS_FT_FI1
Number of Residues	4
Details	MOD_RES: Phosphoserine => ECO:0007744|PubMed:23186163

Chain	Residue	Details
D	THR454
D	GLN579
B	THR454
B	GLN579

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