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glutaminyl-peptide cyclotransferase like

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 3289

Nomenclature: glutaminyl-peptide cyclotransferase like

Family: M28: Aminopeptidase Y

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 382 19q13.32 QPCTL glutaminyl-peptide cyclotransferase like
Mouse 1 383 7 9.46 cM Qpctl glutaminyl-peptide cyclotransferase-like
Rat 1 383 1q21 Qpctl glutaminyl-peptide cyclotransferase-like
Previous and Unofficial Names Click here for help
Golgi QC (gQC) | isoQC
Database Links Click here for help
Specialist databases
MEROPS M28.016
Other databases
Alphafold
BRENDA
Ensembl Gene
Human Protein Atlas
KEGG Enzyme
Pharos
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.3.2.5
Substrates and Reaction Kinetics Click here for help
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
CCL7 Substrate is endogenous in the given species Hs - -
CCL2 Substrate is endogenous in the given species Hs - -
CX3CL1 Substrate is endogenous in the given species Hs - -

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
QP5038 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3.3x10-9 M) [3]
QP5020 Small molecule or natural product Hs Inhibition 8.2 pIC50 3
pIC50 8.2 (IC50 6.4x10-9 M) [3]
BI-43 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 2
pIC50 7.4 (IC50 4x10-8 M) [2]
SEN177 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.5 pIC50 3
pIC50 6.5 (IC50 3.211x10-7 M) [3]
varoglutamstat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.0 pIC50 3
pIC50 6.0 (IC50 9.877x10-7 M) [3]
Immunopharmacology Comments
Golgi-resident glutaminyl cyclase (gQC, or isoQC) appears to influence the regulation of macrophages and monocytes and anti-tumour immunity in the tumour microenvironment [1]. Small molecule gQC inhibitors offer an approach to promote tumour-specific immunity.

References

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1. Bresser K, Logtenberg MEW, Toebes M, Proost N, Sprengers J, Siteur B, Boeije M, Kroese LJ, Schumacher TN. (2022) QPCTL regulates macrophage and monocyte abundance and inflammatory signatures in the tumor microenvironment. Oncoimmunology, 11 (1): 2049486. [PMID:35309731]

2. Mou J, Ning XL, Wang XY, Hou SY, Meng FB, Zhou C, Wu JW, Li C, Jia T, Wu X et al.. (2024) X-ray Structure-Guided Discovery of a Potent Benzimidazole Glutaminyl Cyclase Inhibitor That Shows Activity in a Parkinson's Disease Mouse Model. J Med Chem, 67 (11): 8730-8756. [PMID:38817193]

3. Yu L, Zhao P, Sun Y, Zheng Z, Du W, Zhang L, Li Y, Xie L, Xu S, Wang P. (2023) Development of a potent benzonitrile-based inhibitor of glutaminyl-peptide cyclotransferase-like protein (QPCTL) with antitumor efficacy. Signal Transduct Target Ther, 8 (1): 454. [PMID:38097557]

How to cite this page

M28: Aminopeptidase Y: glutaminyl-peptide cyclotransferase like. Last modified on 04/06/2024. Accessed on 15/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3289.