amyloid P component, serum | Serum pentaxins | IUPHAR/BPS Guide to PHARMACOLOGY

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amyloid P component, serum

target has curated data in GtoImmuPdb

Target id: 2839

Nomenclature: amyloid P component, serum

Family: Serum pentaxins

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 223 1q21-q23 APCS amyloid P component, serum 3-4
Mouse - 224 1 H3 Apcs serum amyloid P-component
Rat - 228 13q24 Apcs amyloid P component, serum
Gene and Protein Information Comments
The human protein has a signal peptide (1-19) with a mature peptide chain of 204 amino acids (20-223).
Previous and Unofficial Names
PTX2 | SAP | amyloid P component
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CPHPC Hs Binding 6.1 pIC50 7
pIC50 6.1 (IC50 9x10-7 M) [7]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
dezamizumab Hs Binding - - 1
[1]
Immunopharmacology Comments
Serum amyloid P or pentraxin 2 is a multi-function circulating plasma protein. It exhibits activity as a soluble pattern recognition receptor of the innate immune system, that can bind DNA and histones when these are released from damaged cells.

A recombinant form of human pentraxin 2 (PRM-151) has been reported as an anti-fibrotic immunomodulator [2]. PRM-151 was found to inhibit the differentiation of circulating monocytes into fibrocytes and profibrotic macrophages, with an associated anti-fibrotic effect in a preclinical model of opacity-producing corneal injury [6]. In humans PRM-151 has demonstrated clinical utility in patents with idiopathic pulmonary fibrosis (IPF; see Phase 2 trial NCT02550873) [5]. The anti-fibrotic efficacy of PRM-151 is also being evaluated in patients with myelofibrosis, and to reduce scarring post-trabeculectomy in gluacoma patients. Click here to link to ClinicalTrials.gov's full list of PRM-151 studies.
Immuno Process Associations
Immuno Process:  Barrier integrity
GO Annotations:  Associated to 1 GO processes
GO:0046597 negative regulation of viral entry into host cell IDA
Immuno Process:  Inflammation
GO Annotations:  Associated to 3 GO processes
GO:0002674 negative regulation of acute inflammatory response IC
GO:0006953 acute-phase response TAS
GO:0045087 innate immune response IDA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0002674 negative regulation of acute inflammatory response IC
GO:0006958 complement activation, classical pathway IBA
GO:0045656 negative regulation of monocyte differentiation IDA
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0045656 negative regulation of monocyte differentiation IDA
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0006958 complement activation, classical pathway IBA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0006958 complement activation, classical pathway IBA

References

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1. Bodin K, Ellmerich S, Kahan MC, Tennent GA, Loesch A, Gilbertson JA, Hutchinson WL, Mangione PP, Gallimore JR, Millar DJ et al.. (2010) Antibodies to human serum amyloid P component eliminate visceral amyloid deposits. Nature, 468 (7320): 93-7. [PMID:20962779]

2. Duffield JS, Lupher Jr ML. (2010) PRM-151 (recombinant human serum amyloid P/pentraxin 2) for the treatment of fibrosis. Drug News Perspect., 23 (5): 305-15. [PMID:20603654]

3. Mantzouranis EC, Dowton SB, Whitehead AS, Edge MD, Bruns GA, Colten HR. (1985) Human serum amyloid P component. cDNA isolation, complete sequence of pre-serum amyloid P component, and localization of the gene to chromosome 1. J. Biol. Chem., 260 (12): 7752-6. [PMID:2987268]

4. Ohnishi S, Maeda S, Shimada K, Arao T. (1986) Isolation and characterization of the complete complementary and genomic DNA sequences of human serum amyloid P component. J. Biochem., 100 (4): 849-58. [PMID:3029048]

5. Raghu G, van den Blink B, Hamblin MJ, Brown AW, Golden JA, Ho LA, Wijsenbeek MS, Vasakova M, Pesci A, Antin-Ozerkis DE et al.. (2019) Long-term treatment with recombinant human pentraxin 2 protein in patients with idiopathic pulmonary fibrosis: an open-label extension study. Lancet Respir Med, 7 (8): 657-664. [PMID:31122893]

6. Santhiago MR, Singh V, Barbosa FL, Agrawal V, Wilson SE. (2011) Monocyte development inhibitor PRM-151 decreases corneal myofibroblast generation in rabbits. Exp. Eye Res., 93 (5): 786-9. [PMID:21933674]

7. Wermuth CG. (2004) Selective optimization of side activities: another way for drug discovery. J. Med. Chem., 47 (6): 1303-14. [PMID:14998318]

How to cite this page

Serum pentaxins: amyloid P component, serum. Last modified on 22/10/2019. Accessed on 08/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2839.