Page last updated: 2024-08-07 17:04:47
Serine/threonine-protein kinase PAK 1
A serine/threonine-protein kinase PAK 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13153]
Synonyms
EC 2.7.11.1;
Alpha-PAK;
p21-activated kinase 1;
PAK-1;
p65-PAK
Research
Bioassay Publications (22)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (18.18) | 29.6817 |
| 2010's | 14 (63.64) | 24.3611 |
| 2020's | 4 (18.18) | 2.80 |
Compounds (86)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| ketorolac | Homo sapiens (human) | IC50 | 36.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0004 | 3 | 3 |
| resveratrol | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| IPA-3 | Homo sapiens (human) | IC50 | 1.7500 | 2 | 2 |
| curcumin | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| lch-7749944 | Homo sapiens (human) | IC50 | 24.2242 | 2 | 2 |
| 1-(3-chloro-2,6-dihydroxy-4-methoxyphenyl)-1-hexanone | Homo sapiens (human) | IC50 | 2.5000 | 1 | 1 |
| artepillin c | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| ym 155 | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pf 3758309 | Homo sapiens (human) | IC50 | 0.0281 | 6 | 6 |
| pf 3758309 | Homo sapiens (human) | Ki | 0.0300 | 3 | 3 |
| frax486 | Homo sapiens (human) | IC50 | 0.0092 | 2 | 2 |
| frax597 | Homo sapiens (human) | IC50 | 1.0185 | 7 | 10 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| staurosporine | Homo sapiens (human) | Kd | 0.0010 | 3 | 3 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.0300 | 2 | 2 |
| vatalanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| canertinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| cyc 202 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| enzastaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| tandutinib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| dasatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| zd 6474 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| bosutinib | Homo sapiens (human) | Kd | 2.3000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| jnj-7706621 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 4.4000 | 2 | 2 |
| ekb 569 | Homo sapiens (human) | Kd | 2.7500 | 2 | 2 |
| axitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 2.0667 | 3 | 3 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| hki 272 | Homo sapiens (human) | Kd | 0.2100 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 2.9000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 0.2600 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| kw 2449 | Homo sapiens (human) | Kd | 2.1000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| crizotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| motesanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| mln8054 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.6500 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 3.1000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 0.5500 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 1.4000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| nintedanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
Enables
This protein enables 7 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 serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| collagen binding | molecular function | Binding to collagen, a group of fibrous proteins of very high tensile strength that form the main component of connective tissue in animals. Collagen is highly enriched in glycine (some regions are 33% glycine) and proline, occurring predominantly as 3-hydroxyproline (about 20%). [GOC:ai, ISBN:0198506732] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| gamma-tubulin binding | molecular function | Binding to the microtubule constituent protein gamma-tubulin. [GOC:jl] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 17 target(s):
| Target | Category | Definition |
|---|---|---|
| ruffle | cellular component | Projection at the leading edge of a crawling cell; the protrusions are supported by a microfilament meshwork. [ISBN:0124325653] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| chromosome | cellular component | A structure composed of a very long molecule of DNA and associated proteins (e.g. histones) that carries hereditary information. [ISBN:0198547684] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
| 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] |
| actin filament | cellular component | A filamentous structure formed of a two-stranded helical polymer of the protein actin and associated proteins. Actin filaments are a major component of the contractile apparatus of skeletal muscle and the microfilaments of the cytoskeleton of eukaryotic cells. The filaments, comprising polymerized globular actin molecules, appear as flexible structures with a diameter of 5-9 nm. They are organized into a variety of linear bundles, two-dimensional networks, and three dimensional gels. In the cytoskeleton they are most highly concentrated in the cortex of the cell just beneath the plasma membrane. [GOC:mah, ISBN:0198506732, PMID:10666339] |
| 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] |
| focal adhesion | cellular component | A cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002] |
| intercalated disc | cellular component | A complex cell-cell junction at which myofibrils terminate in cardiomyocytes; mediates mechanical and electrochemical integration between individual cardiomyocytes. The intercalated disc contains regions of tight mechanical attachment (fasciae adherentes and desmosomes) and electrical coupling (gap junctions) between adjacent cells. [GOC:mtg_muscle, PMID:11732910] |
| Z disc | cellular component | Platelike region of a muscle sarcomere to which the plus ends of actin filaments are attached. [GOC:mtg_muscle, ISBN:0815316194] |
| lamellipodium | cellular component | A thin sheetlike process extended by the leading edge of a migrating cell or extending cell process; contains a dense meshwork of actin filaments. [ISBN:0815316194] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| nuclear membrane | cellular component | Either of the lipid bilayers that surround the nucleus and form the nuclear envelope; excludes the intermembrane space. [GOC:mah, GOC:pz] |
| ruffle membrane | cellular component | The portion of the plasma membrane surrounding a ruffle. [GOC:mah] |
Active In
This protein is active in 1 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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|---|---|
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
Involved In
This protein is involved in 30 target(s):
| Target | Category | Definition |
|---|---|---|
| positive regulation of protein phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd] |
| stimulatory C-type lectin receptor signaling pathway | biological process | The series of molecular signals initiated by the binding of C-type lectin to its receptor on the surface of a target cell, and resulting in cellular activation. [GO_REF:0000022, GOC:add, ISBN:0781735149] |
| chromatin remodeling | biological process | A dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| exocytosis | biological process | A process of secretion by a cell that results in the release of intracellular molecules (e.g. hormones, matrix proteins) contained within a membrane-bounded vesicle. Exocytosis can occur either by full fusion, when the vesicle collapses into the plasma membrane, or by a kiss-and-run mechanism that involves the formation of a transient contact, a pore, between a granule (for exemple of chromaffin cells) and the plasma membrane. The latter process most of the time leads to only partial secretion of the granule content. Exocytosis begins with steps that prepare vesicles for fusion with the membrane (tethering and docking) and ends when molecules are secreted from the cell. [GOC:mah, ISBN:0716731363, PMID:22323285] |
| apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
| DNA damage response | 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 stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| phosphorylation | biological process | The process of introducing a phosphate group into a molecule, usually with the formation of a phosphoric ester, a phosphoric anhydride or a phosphoric amide. [ISBN:0198506732] |
| actin cytoskeleton 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 cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:dph, GOC:jl, GOC:mah] |
| positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
| positive regulation of microtubule polymerization | biological process | Any process that activates or increases the frequency, rate or extent of microtubule polymerization. [GOC:mah] |
| positive regulation of peptidyl-serine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-serine. [GOC:mah] |
| positive regulation of intracellular estrogen receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of the activity of an intracellular estrogen receptor signaling pathway. [GOC:mah] |
| Fc-gamma receptor signaling pathway involved in phagocytosis | biological process | An Fc-gamma receptor signaling pathway that contributes to the endocytic engulfment of external particulate material by phagocytes. [GOC:phg, PMID:12488490, PMID:15466916] |
| wound healing | biological process | The series of events that restore integrity to a damaged tissue, following an injury. [GOC:bf, PMID:15269788] |
| positive regulation of JUN kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of JUN kinase activity. [GOC:jl] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| hepatocyte growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a hepatocyte growth factor receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| ephrin receptor signaling pathway | biological process | The series of molecular signals initiated by ephrin binding to its receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| branching morphogenesis of an epithelial tube | biological process | The process in which the anatomical structures of branches in an epithelial tube are generated and organized. A tube is a long hollow cylinder. [GOC:dgh, GOC:dph, GOC:jid] |
| neuron projection morphogenesis | biological process | The process in which the anatomical structures of a neuron projection are generated and organized. A neuron projection is any process extending from a neural cell, such as axons or dendrites. [GOC:mah] |
| positive regulation of stress fiber assembly | biological process | Any process that activates or increases the frequency, rate or extent of the assembly of a stress fiber, a bundle of microfilaments and other proteins found in fibroblasts. [GOC:ai] |
| negative regulation of cell proliferation involved in contact inhibition | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation in response to cell density. [GOC:dph] |
| positive regulation of microtubule nucleation | biological process | Any process that increases the rate, frequency or extent of microtubule nucleation. Microtubule nucleation is the 'de novo' formation of a microtubule, in which tubulin heterodimers form metastable oligomeric aggregates, some of which go on to support formation of a complete microtubule. Microtubule nucleation usually occurs from a specific site within a cell. [GOC:dph, GOC:tb] |
| protein localization to cytoplasmic stress granule | biological process | A process in which a protein is transported to, or maintained in, a location within a cytoplasmic stress granule. [GO_REF:0000087, GOC:TermGenie, PMID:24755092] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| regulation of actin cytoskeleton organization | biological process | Any process that modulates the frequency, rate or extent of the formation, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:mah] |
| regulation of axonogenesis | biological process | Any process that modulates the frequency, rate or extent of axonogenesis, the generation of an axon, the long process of a neuron. [GOC:ai] |
| regulation of MAPK cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the MAP kinase (MAPK) cascade. [GOC:go_curators] |