Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

RIOK1 (Q9BRS2) - Overview - Molecular Target Synopsis

Protein


RIOK1, Serine/threonine-protein kinase RIO1
Enzyme Classification 2.7.11.1
UniProt Q9BRS2

Also Known as RIOK1_HUMAN, RIOK1, RIO1

Involved in the final steps of cytoplasmic maturation of the 40S ribosomal subunit. Involved in processing of 18S-E pre-rRNA to the mature 18S rRNA. Required for the recycling of NOB1 and PNO1 from the late 40S precursor (PubMed:22072790). The association with the very late 40S subunit intermediate may involve a translation-like checkpoint point cycle preceeding the binding to the 60S ribosomal subunit (By similarity). Despite the protein kinase domain is proposed to act predominantly as an ATPase (By similarity). The catalytic activity regulates its dynamic association with the 40S subunit (By similarity). In addition to its role in ribosomal biogenesis acts as an adapter protein by recruiting NCL/nucleolin the to PRMT5 complex for its symmetrical methylation (PubMed:21081503). Associates with the precursor of the 40S ribosome subunit. Interacts (via its N-terminus) with PRMT5 (via its N-terminus) (PubMed:22072790, PubMed:21081503). Interacts with WDR77 (PubMed:22072790). Found in a PRMT5 complex composed of PRMT5, WDR77 and RIOK1 (PubMed:21081503). Interacts (via its C-terminus) with NCL; this interaction targets NCL for PRTM5 methylation (PubMed:21081503).

6G5I
29 RESIDUE FRAGMENT OF
SERINE/THREONINE-PROTEIN KINASE RIO1
IN THE STRUCTURE OF
CRYO-EM STRUCTURE OF A LATE HUMAN PRE-40S RIBOSOMAL SUBUNIT - STATE R
RCSB/PDB
Inspect Structure
See all 3D Structures for RIOK1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
568ENSG00000124784ENST00000379834ENSP00000369162Q9BRS2-1
95ENSG00000124784ENST00000475351ENSP00000418263

Sub-cellular localization


UniProt: RIOK1 is active in the following subcellular-locations: cytoplasm, cytosol.
GO terms: RIOK1 is active in the following subcellular-locations: cytosol, methyltransferase complex, nucleoplasm, preribosome.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project RIOK1 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, RPMI_8226, IGROV1

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC2270, HGC-27, NCI-H1155

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, K562

(see details)

RNA Interference


RIOK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: H1793, TE11. (see details)

3D Structures


For RIOK1 there are:
2 structures (2 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


RIOK1 has been screened with 107 compounds (149 bioactivities), 10 compounds have bioactivities that show binding affinity of <= 500nM (16 bioactivities). (see details)