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

ULK3 (Q6PHR2) - Overview - Molecular Target Synopsis

Protein


ULK3, Serine/threonine-protein kinase ULK3
Enzyme Classification 2.7.11.1
UniProt Q6PHR2

Also Known as ULK3_HUMAN, ULK3

Serine/threonine protein kinase that acts as a regulator of Sonic hedgehog (SHH) signaling and autophagy. Acts as a negative regulator of SHH signaling in the absence of SHH ligand: interacts with SUFU, thereby inactivating the protein kinase activity and preventing phosphorylation of GLI proteins (GLI1, GLI2 and/or GLI3). Positively regulates SHH signaling in the presence of SHH: dissociates from SUFU, autophosphorylates and mediates phosphorylation of GLI2, activating it and promoting its nuclear translocation. Phosphorylates in vitro GLI2, as well as GLI1 and GLI3, although less efficiently. Also acts as a regulator of autophagy: following cellular senescence, able to induce autophagy. Interacts (via protein kinase domain) with SUFU.

6FDY
UNC-51-LIKE KINASE 3 (ULK3) IN COMPLEX WITH BOSUTINIB
RCSB/PDB
Inspect Structure
See all 3D Structures for ULK3

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ULK3 is active in the following subcellular-locations: cytoplasm.
GO terms: ULK3 is active in the following subcellular-locations: ciliary tip, cytoplasm, cytosol, membrane, phagophore assembly site.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ULK3 has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, MDA_N, MDA_MB_435

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: OCUM-1, HEL, NCI-H1581

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, K562, HeLa-S3

(see details)

RNA Interference


ULK3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: A427, AC375. (see details)

3D Structures


For ULK3 there are:
3 structures (3 chains) solved
2 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

ULK3 is solved in complex with the approved drug(s):

DB8/BOSUTINIB (6FDY_U).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ULK3 has been screened with 274 compounds (448 bioactivities), 14 compounds have bioactivities that show binding affinity of <= 500nM (16 bioactivities). (see details)