Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T03279
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| Former ID |
TTDI03520
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| Target Name |
ribosomal protein S6 kinase, 90kDa, polypeptide 3
|
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| Gene Name |
RPS6KA3
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| Synonyms |
RPS6KA3
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| Target Type |
Research
|
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| Disease | Chronic lymphocytic leukaemia [ICD10: C91] | ||||
| UniProt ID | |||||
| Sequence |
MPLAQLADPWQKMAVESPSDSAENGQQIMDEPMGEEEINPQTEEVSIKEIAITHHVKEGH
EKADPSQFELLKVLGQGSFGKVFLVKKISGSDARQLYAMKVLKKATLKVRDRVRTKMERD ILVEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALA LDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKESIDHEKKAYSFCGTVEYMAPEVV NRRGHTQSADWWSFGVLMFEMLTGTLPFQGKDRKETMTMILKAKLGMPQFLSPEAQSLLR MLFKRNPANRLGAGPDGVEEIKRHSFFSTIDWNKLYRREIHPPFKPATGRPEDTFYFDPE FTAKTPKDSPGIPPSANAHQLFRGFSFVAITSDDESQAMQTVGVHSIVQQLHRNSIQFTD GYEVKEDIGVGSYSVCKRCIHKATNMEFAVKIIDKSKRDPTEEIEILLRYGQHPNIITLK DVYDDGKYVYVVTELMKGGELLDKILRQKFFSEREASAVLFTITKTVEYLHAQGVVHRDL KPSNILYVDESGNPESIRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDAACD IWSLGVLLYTMLTGYTPFANGPDDTPEEILARIGSGKFSLSGGYWNSVSDTAKDLVSKML HVDPHQRLTAALVLRHPWIVHWDQLPQYQLNRQDAPHLVKGAMAATYSALNRNQSPVLEP VGRSTLAQRRGIKKITSTAL |
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| Drugs and Mode of Action | |||||
| Drug(s) | BI-D1870 | Drug Info | Preclinical | Chronic lymphocytic leukaemia | [1] |
| Inhibitor | BI-D1870 | Drug Info | [1] | ||
| BIX 02565 | Drug Info | [2] | |||
| compound 25b | Drug Info | [3] | |||
| compound 8h | Drug Info | [4] | |||
| References | |||||
| REF 1 | BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38. | ||||
| REF 2 | Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42. | ||||
| REF 3 | Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93. | ||||
| REF 4 | The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. | ||||
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