Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT3KYWB)

• DTT Name: Ribosomal protein S6 kinase alpha-6 (RSK6)
• Synonyms: pp90RSK4; p90RSK6; p90-RSK 6; S6K-alpha-6; Ribosomal S6 kinase 4; RSK4; RSK-4; 90 kDa ribosomal protein S6 kinase 6
• Gene Name: RPS6KA6
• DTT Type: Patented-recorded target; [1]
• Related Disease: Mature B-cell leukaemia [ICD-11: 2A82]
• UniProt ID: KS6A6_HUMAN
• TTD ID: T95878
• EC Number: EC 2.7.11.1
• Sequence:
  MLPFAPQDEPWDREMEVFSGGGASSGEVNGLKMVDEPMEEGEADSCHDEGVVKEIPITHH
  VKEGYEKADPAQFELLKVLGQGSFGKVFLVRKKTGPDAGQLYAMKVLKKASLKVRDRVRT
  KMERDILVEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDVFTRLSKEVLFTEEDVKFYLA
  ELALALDHLHQLGIVYRDLKPENILLDEIGHIKLTDFGLSKESVDQEKKAYSFCGTVEYM
  APEVVNRRGHSQSADWWSYGVLMFEMLTGTLPFQGKDRNETMNMILKAKLGMPQFLSAEA
  QSLLRMLFKRNPANRLGSEGVEEIKRHLFFANIDWDKLYKREVQPPFKPASGKPDDTFCF
  DPEFTAKTPKDSPGLPASANAHQLFKGFSFVATSIAEEYKITPITSANVLPIVQINGNAA
  QFGEVYELKEDIGVGSYSVCKRCIHATTNMEFAVKIIDKSKRDPSEEIEILMRYGQHPNI
  ITLKDVFDDGRYVYLVTDLMKGGELLDRILKQKCFSEREASDILYVISKTVDYLHCQGVV
  HRDLKPSNILYMDESASADSIRICDFGFAKQLRGENGLLLTPCYTANFVAPEVLMQQGYD
  AACDIWSLGVLFYTMLAGYTPFANGPNDTPEEILLRIGNGKFSLSGGNWDNISDGAKDLL
  SHMLHMDPHQRYTAEQILKHSWITHRDQLPNDQPKRNDVSHVVKGAMVATYSALTHKTFQ
  PVLEPVAASSLAQRRSMKKRTSTGL
• Function: Constitutively active serine/threonine-protein kinase that exhibits growth-factor-independent kinase activity and that may participate in p53/TP53-dependent cell growth arrest signaling and play an inhibitory role during embryogenesis.
• KEGG Pathway:
  MAPK signaling pathway (hsa04010)
  Oocyte meiosis (hsa04114)
  mTOR signaling pathway (hsa04150)
  Thermogenesis (hsa04714)
  Long-term potentiation (hsa04720)
  Neurotrophin signaling pathway (hsa04722)
  Progesterone-mediated oocyte maturation (hsa04914)
  Insulin resistance (hsa04931)
  Yersinia infection (hsa05135)
  Chemical carcinogenesis - receptor activation (hsa05207)
• Reactome Pathway:
  CREB1 phosphorylation through NMDA receptor-mediated activation of RAS signaling (R-HSA-442742)
  RSK activation (R-HSA-444257)
  Recycling pathway of L1 (R-HSA-437239)

Molecular Interaction Atlas (MIA) of This DTT

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CID 138805970	DMINXMY	N. A.	N. A.	Patented	[2]
US10081632, Compound 25	DM3BDHN	N. A.	N. A.	Patented	[2]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BI-D1870	DMK3SAF	Chronic lymphocytic leukaemia	2A82.0	Preclinical	[1]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[3]

References

• [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.
• [2] Substituted tetrahydropyrido[3,2:4,5]pyrrolo[1,2-a]pyrazine-2-carboxamides as RSK inhibitors. US9771366.
• [3] Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.