| Target
Information |
| Name | Ribosomal protein S6 kinase |
| Type of target | Discontinued target |
| Synonyms | P70-S6K |
| S6K |
| Disease | Cancer, unspecific
[ICD9: 140-229 ICD10: C00-C96] | [1] |
Solid tumors
[ICD9: 140-199, 210-229 ICD10: C00-C75, C7A, C7B, D10-D36, D3A] | [2] |
| Drug(s) | XL418 |  | Suspended in Phase I | Solid Tumors | [3] |
| BioChemical Class | Transferases transferring phosphorus-containing groups |
| EC Number | EC 2.7.1.- |
| EC 2.7.1.37 |
| Pathway | Acute myeloid leukemia |
| ErbB signaling pathway |
| Insulin signaling pathway |
| TGF-beta signaling pathway |
| mTOR signaling pathway |
| UniProt ID | P23443 |
| PDB Structure | 3A60; 3A61; 3A62. |
| Function | Phosphorylates specifically ribosomal protein s6. |
| Sequence | MRRRRRRDGFYPAPDFRDREAEDMAGVFDIDLDQPEDAGSEDELEEGGQLNESMDHGGVG
PYELGMEHCEKFEISETSVNRGPEKIRPECFELLRVLGKGGYGKVFQVRKVTGANTGKIF
AMKVLKKAMIVRNAKDTAHTKAERNILEEVKHPFIVDLIYAFQTGGKLYLILEYLSGGEL
FMQLEREGIFMEDTACFYLAEISMALGHLHQKGIIYRDLKPENIMLNHQGHVKLTDFGLC
KESIHDGTVTHTFCGTIEYMAPEILMRSGHNRAVDWWSLGALMYDMLTGAPPFTGENRKK
TIDKILKCKLNLPPYLTQEARDLLKKLLKRNAASRLGAGPGDAGEVQAHPFFRHINWEEL
LARKVEPPFKPLLQSEEDVSQFDSKFTRQTPVDSPDDSTLSESANQVFLGFTYVAPSVLE
SVKEKFSFEPKIRSPRRFIGSPRTPVSPVKFSPGDFWGRGASASTANPQTPVEYPMETSG
IEQMDVTMSGEASAPLPIRQPNSGPYKKQAFPMISKRPEHLRMNL
|
| Target Validation | Click to Find Target Validation Information. |
| Inhibitor | 4,5,6,7-tetrabromobenzotriazole | | [4] |
| 4-[ (3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | | [5] |
| BISINDOLYLMALEIMIDE IX | | [6] |
| CI-1040, PD-18435, PD-184352 | | [6] |
| KN-62 | | [6] |
| KT-5720 | | [6] |
| LY-294002 | | [6] |
| PD-98059 | | [6] |
| PHA-767491 | | [7] |
| RO-316233 | | [6] |
| SB-202190 | | [6] |
| SB-203580 | | [6] |
| SB-415286 | | [8] |
| SB-747651A | | [9] |
| STAUROSPORINONE | | [6] |
| U-0126 | | [6] |
| XL418 | | [3] |
| Multitarget | XL418 | | [3] |
| Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
| Ref 1 | Identification of novel cellular targets in biliary tract cancers using global gene expression technology. Am J Pathol. 2003 Jul;163(1):217-29. To Reference |
| Ref 2 | CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference |
| Ref 3 | Drug information of XL418. National Cancer Institute. 2009 To Reference |
| Ref 4 | J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. To Reference |
| Ref 5 | J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. To Reference |
| Ref 6 | Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. To Reference |
| Ref 7 | J Med Chem. 2007 May 31;50(11):2647-54. Epub 2007 May 5.Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). To Reference |
| Ref 8 | Bioorg Med Chem Lett. 2001 Mar 12;11(5):635-9.3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). To Reference |
| Ref 9 | Bioorg Med Chem Lett. 2005 Jul 15;15(14):3407-11.(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors. To Reference |
