cathepsin L | C1: Papain | IUPHAR Guide to IMMUNOPHARMACOLOGY

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cathepsin L

  Target has curated data in GtoImmuPdb

Target id: 2351

Nomenclature: cathepsin L

Family: C1: Papain

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 333 9q21.33 CTSL cathepsin L
Mouse - 334 13 B3 Ctsl cathepsin L
Previous and Unofficial Names
cathepsin L1 | fs | furless | MEP | nackt | nkt | Cat L | p39 cysteine proteinase
Database Links
Specialist databases
MEROPS C01.032 (Hs)
Other databases
BRENDA 3.4.22.15
ChEMBL Target CHEMBL3837 (Hs), CHEMBL5291 (Mm)
Ensembl Gene ENSG00000135047 (Hs), ENSMUSG00000021477 (Mm)
Entrez Gene 1514 (Hs), 13039 (Mm)
Human Protein Atlas ENSG00000135047 (Hs)
KEGG Enzyme 3.4.22.15
KEGG Gene hsa:1514 (Hs), mmu:13039 (Mm)
OMIM 116880 (Hs)
RefSeq Nucleotide NM_001257971 (Hs), NM_001257972 (Hs), NM_001912 (Hs), NM_145918 (Hs), NM_009984 (Mm)
RefSeq Protein NP_666023 (Hs), NP_001244901 (Hs), NP_001244900 (Hs), NP_001903 (Hs), NP_034114 (Mm)
UniProtKB P07711 (Hs), P06797 (Mm)
Wikipedia CTSL (Hs)
Enzyme Reaction
EC Number: 3.4.22.15

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 Affinity Parameter Reference
CAA0225 Rn Inhibition 8.7 pIC50 3
⤷ pIC50 8.7 (IC50 1.9x10-9 M) [3]
LHVS Hs Inhibition 8.1 pIC50 2
⤷ pIC50 8.1 (IC50 7x10-9 M) [2]
KGP94 Hs Inhibition 6.9 pIC50 1
⤷ pIC50 6.9 (IC50 1.314x10-7 M) [1]
View species-specific inhibitor tables
Immunopharmacology Comments
Cathepsins B, H and L have become important therapeutic targets as their proteolytic activity has been implicated in several pathological inflammatory conditions, such as arthritis and periodontitis. Therefore, pharmacological inhibitors of these enzymes are in development as novel therapeutics.
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 2 GO processes
GO:0019882 antigen processing and presentation TAS
GO:0019886 antigen processing and presentation of exogenous peptide antigen via MHC class II TAS
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0002250 adaptive immune response IEP
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0002250 adaptive immune response IEP

References

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1. Kumar GD, Chavarria GE, Charlton-Sevcik AK, Yoo GK, Song J, Strecker TE, Siim BG, Chaplin DJ, Trawick ML, Pinney KG. (2010) Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L. Bioorg. Med. Chem. Lett., 20 (22): 6610-5. [PMID:20933415]

2. Méthot N, Rubin J, Guay D, Beaulieu C, Ethier D, Reddy TJ, Riendeau D, Percival MD. (2007) Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. J. Biol. Chem., 282 (29): 20836-46. [PMID:17535802]

3. Takahashi K, Ueno T, Tanida I, Minematsu-Ikeguchi N, Murata M, Kominami E. (2009) Characterization of CAA0225, a novel inhibitor specific for cathepsin L, as a probe for autophagic proteolysis. Biol. Pharm. Bull., 32 (3): 475-9. [PMID:19252298]

How to cite this page

C1: Papain: cathepsin L. Last modified on 21/04/2017. Accessed on 20/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2351.