Details of the Target
General Information of Target
| Target ID | LDTP01351 | |||||
|---|---|---|---|---|---|---|
| Target Name | Serine/threonine-protein kinase PAK 3 (PAK3) | |||||
| Gene Name | PAK3 | |||||
| Gene ID | 5063 | |||||
| Synonyms |
OPHN3; Serine/threonine-protein kinase PAK 3; EC 2.7.11.1; Beta-PAK; Oligophrenin-3; p21-activated kinase 3; PAK-3 |
|||||
| 3D Structure | ||||||
| Sequence |
MSDGLDNEEKPPAPPLRMNSNNRDSSALNHSSKPLPMAPEEKNKKARLRSIFPGGGDKTN
KKKEKERPEISLPSDFEHTIHVGFDAVTGEFTPDLYGSQMCPGKLPEGIPEQWARLLQTS NITKLEQKKNPQAVLDVLKFYDSKETVNNQKYMSFTSGDKSAHGYIAAHPSSTKTASEPP LAPPVSEEEDEEEEEEEDENEPPPVIAPRPEHTKSIYTRSVVESIASPAVPNKEVTPPSA ENANSSTLYRNTDRQRKKSKMTDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTA LDIATGQEVAIKQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYL AGGSLTDVVTETCMDEGQIAAVCRECLQALDFLHSNQVIHRDIKSDNILLGMDGSVKLTD FGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMVEGEPPYLNE NPLRALYLIATNGTPELQNPERLSAVFRDFLNRCLEMDVDRRGSAKELLQHPFLKLAKPL SSLTPLIIAAKEAIKNSSR |
|||||
| Target Bioclass |
Enzyme
|
|||||
| Family |
Protein kinase superfamily, STE Ser/Thr protein kinase family, STE20 subfamily
|
|||||
| Subcellular location |
Cytoplasm
|
|||||
| Function |
Serine/threonine protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell migration, or cell cycle regulation. Plays a role in dendrite spine morphogenesis as well as synapse formation and plasticity. Acts as a downstream effector of the small GTPases CDC42 and RAC1. Activation by the binding of active CDC42 and RAC1 results in a conformational change and a subsequent autophosphorylation on several serine and/or threonine residues. Phosphorylates MAPK4 and MAPK6 and activates the downstream target MAPKAPK5, a regulator of F-actin polymerization and cell migration. Additionally, phosphorylates TNNI3/troponin I to modulate calcium sensitivity and relaxation kinetics of thin myofilaments. May also be involved in early neuronal development. In hippocampal neurons, necessary for the formation of dendritic spines and excitatory synapses; this function is dependent on kinase activity and may be exerted by the regulation of actomyosin contractility through the phosphorylation of myosin II regulatory light chain (MLC).
|
|||||
| Uniprot ID | ||||||
| Ensemble ID | ||||||
| HGNC ID | ||||||
| ChEMBL ID | ||||||
Probe(s) Labeling This Target
ABPP Probe
| Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
|---|---|---|---|---|---|
|
BTD Probe Info |
![]() |
C424(0.66) | LDD2100 | [1] | |
|
IPM Probe Info |
![]() |
N.A. | LDD0025 | [2] | |
|
JW-RF-010 Probe Info |
![]() |
N.A. | LDD0026 | [2] | |
|
Compound 10 Probe Info |
![]() |
N.A. | LDD2216 | [3] | |
|
NAIA_5 Probe Info |
![]() |
N.A. | LDD2223 | [4] | |
Competitor(s) Related to This Target
| Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
|---|---|---|---|---|---|
| LDCM0539 | 3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile | MDA-MB-231 | C424(0.43) | LDD2132 | [1] |
| LDCM0538 | 4-(Cyanoacetyl)morpholine | MDA-MB-231 | C424(0.88) | LDD2131 | [1] |
| LDCM0507 | Nucleophilic fragment 16b | MDA-MB-231 | C424(0.66) | LDD2100 | [1] |
| LDCM0527 | Nucleophilic fragment 26b | MDA-MB-231 | C424(1.02) | LDD2120 | [1] |
The Interaction Atlas With This Target
References





