Details of the Target

General Information of Target

Target ID LDTP06363
Target Name Ribosomal protein S6 kinase alpha-2 (RPS6KA2)
Gene Name RPS6KA2
Gene ID 6196
Synonyms
MAPKAPK1C; RSK3; Ribosomal protein S6 kinase alpha-2; S6K-alpha-2; EC 2.7.11.1; 90 kDa ribosomal protein S6 kinase 2; p90-RSK 2; p90RSK2; MAP kinase-activated protein kinase 1c; MAPK-activated protein kinase 1c; MAPKAP kinase 1c; MAPKAPK-1c; Ribosomal S6 kinase 3; RSK-3; pp90RSK3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDLSMKKFAVRRFFSVYLRRKSRSKSSSLSRLEEEGVVKEIDISHHVKEGFEKADPSQFE
LLKVLGQGSYGKVFLVRKVKGSDAGQLYAMKVLKKATLKVRDRVRSKMERDILAEVNHPF
IVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALALDHLHSLGI
IYRDLKPENILLDEEGHIKITDFGLSKEAIDHDKRAYSFCGTIEYMAPEVVNRRGHTQSA
DWWSFGVLMFEMLTGSLPFQGKDRKETMALILKAKLGMPQFLSGEAQSLLRALFKRNPCN
RLGAGIDGVEEIKRHPFFVTIDWNTLYRKEIKPPFKPAVGRPEDTFHFDPEFTARTPTDS
PGVPPSANAHHLFRGFSFVASSLIQEPSQQDLHKVPVHPIVQQLHGNNIHFTDGYEIKED
IGVGSYSVCKRCVHKATDTEYAVKIIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDGK
FVYLVMELMRGGELLDRILRQRYFSEREASDVLCTITKTMDYLHSQGVVHRDLKPSNILY
RDESGSPESIRVCDFGFAKQLRAGNGLLMTPCYTANFVAPEVLKRQGYDAACDIWSLGIL
LYTMLAGFTPFANGPDDTPEEILARIGSGKYALSGGNWDSISDAAKDVVSKMLHVDPHQR
LTAMQVLKHPWVVNREYLSPNQLSRQDVHLVKGAMAATYFALNRTPQAPRLEPVLSSNLA
QRRGMKRLTSTRL
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, S6 kinase subfamily
Subcellular location
Nucleus
Function
Serine/threonine-protein kinase that acts downstream of ERK (MAPK1/ERK2 and MAPK3/ERK1) signaling and mediates mitogenic and stress-induced activation of transcription factors, regulates translation, and mediates cellular proliferation, survival, and differentiation. May function as tumor suppressor in epithelial ovarian cancer cells.
TTD ID
T28043
Uniprot ID
Q15349
DrugMap ID
TT0ZW9O
Ensemble ID
ENST00000265678.9
HGNC ID
HGNC:10431
ChEMBL ID
CHEMBL3906

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO829 SNV: p.E311K .
HEC1B SNV: p.W243R .
KP4 SNV: p.L719P .
MCC26 SNV: p.G143R .
MFE319 Deletion: p.V100FfsTer5
SNV: p.Y225C		 .
RKO SNV: p.H654Y .
SNU1 SNV: p.R551Ter .
SW620 SNV: p.H197N .
SW948 SNV: p.K651N .
TOV21G SNV: p.D263Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C578(3.66)  LDD2469  [1]
Johansson_61
 Probe Info  		_(6.05)  LDD1489  [2]
AHL-Pu-1
 Probe Info  		C429(2.00)  LDD0169  [3]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe12
 Probe Info  		20.00  LDD0473  [4]
FFF probe3
 Probe Info  		20.00  LDD0465  [4]
FFF probe6
 Probe Info  		15.98  LDD0468  [4]
STS-1
 Probe Info  		N.A.  LDD0137  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA HEK-293T C429(2.00)  LDD0169  [3]
 LDCM0616  Fragment61 Jurkat _(6.05)  LDD1489  [2]
 LDCM0022  KB02 MGG123 C578(3.66)  LDD2469  [1]
 LDCM0023  KB03 MGG123 C578(3.84)  LDD2886  [1]
 LDCM0024  KB05 MGG123 C578(3.42)  LDD3303  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein kinase C epsilon type (PRKCE) AGC Ser/Thr protein kinase family Q02156
Mitogen-activated protein kinase 1 (MAPK1) CMGC Ser/Thr protein kinase family P28482
Serine/threonine-protein kinase B-raf (BRAF) TKL Ser/Thr protein kinase family P15056
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Krueppel-like factor 11 (KLF11) Sp1 C2H2-type zinc-finger protein family O14901
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein scribble homolog (SCRIB) LAP (LRR and PDZ) protein family Q14160
SH3 and multiple ankyrin repeat domains protein 1 (SHANK1) SHANK family Q9Y566

The Drug(s) Related To This Target

Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bi-d1870 Small molecular drug D02VBF
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid22564207c25b Small molecular drug D09AID

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
3 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
4 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
5 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.