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chitinase acidic

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2982

Nomenclature: chitinase acidic

Abbreviated Name: AMCase

Family: Chitinases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 476 1p13.2 CHIA chitinase acidic
Mouse - 473 3 F2.2 Chia1 chitinase, acidic 1
Rat - 473 2q34 Chia chitinase, acidic
Gene and Protein Information Comments
Several transcript variants from the human gene have been reported, but these produce only three protein isoforms (isoform c is the longest at 467 amino acids, isoform a has a shorter N-terminus and is 368 amino acids, and isoform c initiates from an alternative downstream AUG and is 315 amino acids).
Previous and Unofficial Names Click here for help
chitinase, acidic 1 | chitinase, acidic | chitinase | CHIT2
Database Links Click here for help
Alphafold
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GLPG4716 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Inhibition 8.1 pIC50 2
pIC50 8.1 (IC50 7.8x10-9 M) [2]
GLPG4716 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 2
pIC50 8.1 (IC50 9x10-9 M) [2]
compound 7f [PMID: 29283260] Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.4x10-8 M) [3]
compound 7f [PMID: 29283260] Small molecule or natural product Immunopharmacology Ligand Mm Inhibition 7.7 pIC50 3
pIC50 7.7 (IC50 1.9x10-8 M) [3]
View species-specific inhibitor tables
Immunopharmacology Comments
AMCase has been shown to be produced during type 2 inflammatory responses [6], such as those mediating allergic asthma [1,4]. As part of this type 2 response, AMCase activity causes IL-13 pathway activation. Laboratory studies have shown that AMCase neutralization, genetic ablation or pharmacological inhibition results in reduced IL-13-mediated allergic airway inflammation. Selective AMCase inhibitors are subsequently being investigated for anti-inflammatory potential in asthma [3].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0002532 production of molecular mediator involved in inflammatory response IDA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0032722 positive regulation of chemokine production IDA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0032722 positive regulation of chemokine production IDA
Clinically-Relevant Mutations and Pathophysiology Comments
Mutations in this gene are associated with asthma susceptibility.
Biologically Significant Variants Click here for help
Type:  Naturally occurring SNP
Species:  Human
Description:  The rs10494132 polymorphism of CHIA might be a risk factor for asthma.
SNP accession: 
References:  5
General Comments
Chitinase degrades the chitin in the cell walls of fungi, arthropods and nematodes.

References

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1. Elias JA, Homer RJ, Hamid Q, Lee CG. (2005) Chitinases and chitinase-like proteins in T(H)2 inflammation and asthma. J Allergy Clin Immunol, 116 (3): 497-500. [PMID:16159614]

2. Koralewski R, Dymek B, Mazur M, Sklepkiewicz P, Olejniczak S, Czestkowski W, Matyszewski K, Andryianau G, Niedziejko P, Kowalski M et al.. (2020) Discovery of OATD-01, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis. J Med Chem, 63 (24): 15527-15540. [PMID:33078933]

3. Mazur M, Olczak J, Olejniczak S, Koralewski R, Czestkowski W, Jedrzejczak A, Golab J, Dzwonek K, Dymek B, Sklepkiewicz PL et al.. (2018) Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma. J Med Chem, 61 (3): 695-710. [PMID:29283260]

4. Shen CR, Juang HH, Chen HS, Yang CJ, Wu CJ, Lee MH, Hwang YS, Kuo ML, Chen YS, Chen JK et al.. (2015) The Correlation between Chitin and Acidic Mammalian Chitinase in Animal Models of Allergic Asthma. Int J Mol Sci, 16 (11): 27371-7. [PMID:26580611]

5. Zhu Y, Yan X, Zhai C, Yang L, Li M. (2017) Association between risk of asthma and gene polymorphisms in CHI3L1 and CHIA: a systematic meta-analysis. BMC Pulm Med, 17 (1): 193. [PMID:29233108]

6. Zhu Z, Zheng T, Homer RJ, Kim YK, Chen NY, Cohn L, Hamid Q, Elias JA. (2004) Acidic mammalian chitinase in asthmatic Th2 inflammation and IL-13 pathway activation. Science, 304 (5677): 1678-82. [PMID:15192232]

How to cite this page

Chitinases: chitinase acidic. Last modified on 16/07/2021. Accessed on 22/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2982.