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

Ptgs2 (Q05769) - Overview - Molecular Target Synopsis

Protein


Ptgs2, Prostaglandin G/H synthase 2
Enzyme Classification 1.14.99.1
UniProt Q05769

Also Known as PGH2_MOUSE, Ptgs2, Cox-2, Cox2, Pghs-b, Tis10

Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, phenotypic changes, resistance to apoptosis and tumor angiogenesis. In cancer cells, PTGS2 is a key step in the production of prostaglandin E2 (PGE2), which plays important roles in modulating motility, proliferation and resistance to apoptosis. Homodimer.

6BL4
CRYSTAL COMPLEX OF CYCLOOXYGENASE-2 WITH INDOMETHACIN-ETHYLENEDIAMINE- DANSYL CONJUGATE
RCSB/PDB
Inspect Structure
See all 3D Structures for Ptgs2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
604Q05769-1

Sub-cellular localization


UniProt: Ptgs2 is active in the following subcellular-locations: endoplasmic reticulum membrane, microsome membrane.
GO terms: Ptgs2 is active in the following subcellular-locations: caveola, cytoplasm, endoplasmic reticulum, endoplasmic reticulum membrane, neuron projection, organelle membrane, protein-containing complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project Ptgs2 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

3D Structures


For Ptgs2 there are:
47 structures (138 chains) solved
47 are solved in complex with at least one small molecule ligand
13 are solved with an approved drug

Ptgs2 is solved in complex with the approved drug(s):

CEL/CELECOXIB (3LN1_A, 3LN1_B, 3LN1_C, 3LN1_D, 5JW1_A, 5JW1_B),
LUR/LUMIRACOXIB (4OTY_A, 4OTY_B, 4RRW_A, 4RRW_B, 4RRW_C, 4RRW_D, 4RRX_A, 4RRX_B, 4RRZ_A, 4RRZ_B, 4RRZ_C, 4RRZ_D),
MXM/MELOXICAM (4M11_A, 4M11_B, 4M11_C, 4M11_D),
IMN/INDOMETHACIN (4COX_A, 4COX_B, 4COX_C, 4COX_D),
DIF/DICLOFENAC (1PXX_A, 1PXX_B, 1PXX_C, 1PXX_D),
IBP/DEXIBUPROFEN (4PH9_A, 4PH9_B, 4RS0_A),
ICD/ISOXICAM (4M10_A, 4M10_B, 4M10_C, 4M10_D),
NPS/NAPROXEN (3NT1_A, 3NT1_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


Ptgs2 has been screened with 1237 compounds (2002 bioactivities), 316 compounds have bioactivities that show binding affinity of <= 500nM (413 bioactivities). (see details)