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

PFKP (Q01813) - Overview - Molecular Target Synopsis

Protein


PFKP, ATP-dependent 6-phosphofructokinase, platelet type
Enzyme Classification 2.7.1.11
UniProt Q01813

Also Known as PFKAP_HUMAN, PFKP, PFKF

Catalyzes the phosphorylation of D-fructose 6-phosphate to fructose 1,6-bisphosphate by ATP, the first committing step of glycolysis. Homo- and heterotetramers (By similarity). Phosphofructokinase (PFK) enzyme functions as a tetramer composed of different combinations of 3 types of subunits, called PFKM (where M stands for Muscle), PFKL (Liver) and PFKP (Platelet). The composition of the PFK tetramer differs according to the tissue type it is present in. In muscles, it is composed of 4 PFKM subunits (also called M4). In the liver, the predominant form is a tetramer of PFKL subunits (L4). In erythrocytes, both PFKM and PFKL subunits randomly tetramerize to form M4, L4 and other combinations (ML3, M2L2, M3L). In platelets, brain and fibroblasts, PFK contains a higher proportion of PFKP subunits. The kinetic and regulatory properties of the tetrameric enzyme are dependent on the subunit composition, hence can vary across tissues (Probable).

4RH3
AMPPCP-BOUND STRUCTURE OF HUMAN PLATELET PHOSPHOFRUCTOKINASE IN AN R- STATE, CRYSTAL FORM II
RCSB/PDB
Inspect Structure
See all 3D Structures for PFKP

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PFKP is active in the following subcellular-locations: cytoplasm.
GO terms: PFKP is active in the following subcellular-locations: 6-phosphofructokinase complex, cytoplasm, cytosol, extracellular exosome, membrane, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PFKP has gain in 3 cell-lines, loss in 7 cell-lines and no signal in 995 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: TK_10, A498, NCI_ADR_RES

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: 786-O, Caki-1, Caki-2

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, A549, HMEC

(see details)

RNA Interference


PFKP was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HCC70, OVISE. (see details)

3D Structures


For PFKP there are:
6 structures (28 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PFKP has been screened with 223 compounds (223 bioactivities). (see details)