Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T20973
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| Former ID |
TTDR00296
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| Target Name |
Cell division protein kinase 5
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| Gene Name |
CDK5
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| Synonyms |
Cyclin-dependent kinase 5; Cyclin-dependent kinase 5 (CDK5); PDPK; Proline-directed protein kinase 33 kDa subunit; Proline-directed protein kinase F(A) (PDPK F(A)); Serine/threonine protein kinase PSSALRE; Serine/threonine-protein kinase PSSALRE; TPKII catalytic subunit; Tau protein kinase II catalytic subunit; CDK5
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| Target Type |
Discontinued
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| Function |
Proline-directed serine/threonine-protein kinase essential for neuronal cell cycle arrest and differentiation and may be involved in apoptotic cell death in neuronal diseases by triggering abortive cell cycle re-entry. Interacts with D1 and D3- type G1 cyclins. Phosphorylates SRC, NOS3, VIM/vimentin, p35/CDK5R1, MEF2A, SIPA1L1, SH3GLB1, PXN, PAK1, MCAM/MUC18, SEPT5, SYN1, DNM1, AMPH, SYNJ1, CDK16, RAC1, RHOA, CDC42, TONEBP/NFAT5, MAPT/TAU, MAP1B, histone H1, p53/TP53, HDAC1, APEX1, PTK2/FAK1, huntingtin/HTT, ATM, MAP2, NEFH and NEFM. Regulates several neuronal development and physiological processes including neuronal survival, migration and differentiation, axonal and neurite growth, synaptogenesis, oligodendrocyte differentiation, synaptic plasticity and neurotransmission, by phosphorylating key proteins.
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| BioChemical Class |
Kinase
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| Target Validation |
T20973
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.22
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| Sequence |
MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKH
KNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSR NVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYS TSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYP MYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP |
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| Drugs and Mode of Action | |||||
| Drug(s) | Olomoucine | Drug Info | Terminated | Discovery agent | [1] |
| Inhibitor | 1-phenyl-3-(2-(pyridin-4-yl)thiazol-4-yl)urea | Drug Info | [2] | ||
| 3-(2-phenylthiazol-4-yl)quinolin-2(1H)-one | Drug Info | [3] | |||
| 6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE | Drug Info | [4] | |||
| 9-Nitropaullone | Drug Info | [5] | |||
| aloisine A | Drug Info | [6] | |||
| aminopurvalanol A | Drug Info | [7] | |||
| AZAKENPAULLONE | Drug Info | [8] | |||
| Hymenialdisine | Drug Info | [5] | |||
| Indirubin-3'-monoxime | Drug Info | [5] | |||
| Indirubin-5-sulfonate | Drug Info | [5] | |||
| KENPAULLONE | Drug Info | [8] | |||
| MANZAMINE A | Drug Info | [9] | |||
| NU6140 | Drug Info | [10] | |||
| Olomoucine | Drug Info | [5] | |||
| Oxindole 16 (compound 3) | Drug Info | [5] | |||
| Oxindole 95 | Drug Info | [5] | |||
| Purvalanol B | Drug Info | [5] | |||
| Quinoxaline1 | Drug Info | [7] | |||
| SU9516 | Drug Info | [5] | |||
| Thieno analogue of kenpaullone | Drug Info | [8] | |||
| Pathways | |||||
| KEGG Pathway | Axon guidance | ||||
| Alzheimer' | |||||
| s disease | |||||
| Cocaine addiction | |||||
| NetPath Pathway | EGFR1 Signaling Pathway | ||||
| TCR Signaling Pathway | |||||
| PANTHER Pathway | Axon guidance mediated by semaphorins | ||||
| Pathway Interaction Database | Reelin signaling pathway | ||||
| Glucocorticoid receptor regulatory network | |||||
| Lissencephaly gene (LIS1) in neuronal migration and development | |||||
| EPHA forward signaling | |||||
| Trk receptor signaling mediated by the MAPK pathway | |||||
| Reactome | DARPP-32 events | ||||
| CRMPs in Sema3A signaling | |||||
| Factors involved in megakaryocyte development and platelet production | |||||
| WikiPathways | DNA Damage Response | ||||
| BDNF signaling pathway | |||||
| Alzheimers Disease | |||||
| Opioid Signalling | |||||
| Semaphorin interactions | |||||
| Factors involved in megakaryocyte development and platelet production | |||||
| Nicotine Activity on Dopaminergic Neurons | |||||
| miRNA Regulation of DNA Damage Response | |||||
| References | |||||
| REF 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008577) | ||||
| REF 2 | Bioorg Med Chem. 2007 Oct 15;15(20):6574-95. Epub 2007 Jul 25.Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. | ||||
| REF 3 | Bioorg Med Chem Lett. 2007 Oct 1;17(19):5384-9. Epub 2007 Aug 6.Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors. | ||||
| REF 4 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
| REF 5 | Pharmacological inhibitors of cyclin-dependent kinases. Trends Pharmacol Sci. 2002 Sep;23(9):417-25. | ||||
| REF 6 | J Med Chem. 2003 Jan 16;46(2):222-36.Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. | ||||
| REF 7 | Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. | ||||
| REF 8 | Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. | ||||
| REF 9 | J Nat Prod. 2007 Sep;70(9):1397-405. Epub 2007 Aug 21.Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease. | ||||
| REF 10 | Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37. | ||||
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