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

CAMKK2 (Q96RR4) - Overview - Molecular Target Synopsis

Protein


CAMKK2, Calcium/calmodulin-dependent protein kinase kinase 2
Enzyme Classification 2.7.11.17
UniProt Q96RR4

Also Known as KKCC2_HUMAN, CAMKK2, CAMKKB, KIAA0787

Calcium/calmodulin-dependent protein kinase belonging to a proposed calcium-triggered signaling cascade involved in a number of cellular processes. Isoform 1, isoform 2 and isoform 3 phosphorylate CAMK1 and CAMK4. Isoform 3 phosphorylates CAMK1D. Isoform 4, isoform 5 and isoform 6 lacking part of the calmodulin-binding domain are inactive. Efficiently phosphorylates 5'-AMP-activated protein kinase (AMPK) trimer, including that consisting of PRKAA1, PRKAB1 and PRKAG1. This phosphorylation is stimulated in response to Ca(2+) signals (By similarity). Seems to be involved in hippocampal activation of CREB1 (By similarity). May play a role in neurite growth. Isoform 3 may promote neurite elongation, while isoform 1 may promoter neurite branching. Interacts with calmodulin.

5YVA
A KINASE-INHIBITOR COMPLEX
RCSB/PDB
Inspect Structure
See all 3D Structures for CAMKK2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CAMKK2 is active in the following subcellular-locations: cell projection, cytoplasm, nucleus.
GO terms: CAMKK2 is active in the following subcellular-locations: cell projection, cytosol, intracellular, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CAMKK2 has gain in 2 cell-lines, loss in 0 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: ACHN, HL_60, PC_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, SCLC-21H, LP-1

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, A549

(see details)

RNA Interference


CAMKK2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: 93VU, SCC47. (see details)

3D Structures


For CAMKK2 there are:
18 structures (26 chains) solved
16 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CAMKK2 has been screened with 380 compounds (501 bioactivities), 14 compounds have bioactivities that show binding affinity of <= 500nM (22 bioactivities). (see details)