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

PHKG1 (Q16816) - Overview - Molecular Target Synopsis

Protein


PHKG1, Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform
Enzyme Classification 2.7.11.19
UniProt Q16816

Also Known as PHKG1_HUMAN, PHKG1, PHKG

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. In vitro, phosphorylates PYGM, TNNI3, MAPT/TAU, GAP43 and NRGN/RC3. 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.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


GO terms: PHKG1 is active in the following subcellular-locations: cytosol, phosphorylase kinase complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PHKG1 has gain in 18 cell-lines, loss in 0 cell-lines and no signal in 987 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MDA_N, NCI_H460, TK_10

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, SK-N-FI, NCI-H322T

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, HSMM

(see details)

3D Structures


At greater than 90% identity similarity to PHKG1 there are:
3 structures (3 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PHKG1 has been screened with 553 compounds (990 bioactivities), 12 compounds have bioactivities that show binding affinity of <= 500nM (21 bioactivities). (see details)