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

PHKG2 (P15735) - Overview - Molecular Target Synopsis

Protein


PHKG2, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform
Enzyme Classification 2.7.11.19
UniProt P15735

Also Known as PHKG2_HUMAN, PHKG2

Catalytic subunit of the phosphorylase b kinase (PHK), which mediates the neural and hormonal regulation of glycogen breakdown (glycogenolysis) by phosphorylating and thereby activating glycogen phosphorylase. May regulate glycogeneolysis in the testis. In vitro, phosphorylates PYGM. Hexadecamer of 4 heterotetramers, each composed of alpha, beta, gamma, and delta subunits. Alpha (PHKA1 or PHKA2) and beta (PHKB) are regulatory subunits, gamma (PHKG1 or PHKG2) is the catalytic subunit, and delta is calmodulin.

2Y7J
STRUCTURE OF HUMAN PHOSPHORYLASE KINASE, GAMMA 2
RCSB/PDB
Inspect Structure
See all 3D Structures for PHKG2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


GO terms: PHKG2 is active in the following subcellular-locations: cytosol, phosphorylase kinase complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PHKG2 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: OVCAR_4, SN12C, T47D

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: OUMS-23, NCI-H1882, KYSE-520

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, A549

(see details)

RNA Interference


PHKG2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HCC202, BT474. (see details)

3D Structures


For PHKG2 there are:
1 structures (4 chains) solved
1 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

PHKG2 is solved in complex with the approved drug(s):

B49/SUNITINIB (2Y7J_A, 2Y7J_B, 2Y7J_C, 2Y7J_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PHKG2 has been screened with 736 compounds (1356 bioactivities), 12 compounds have bioactivities that show binding affinity of <= 500nM (22 bioactivities). (see details)