› 3of8

X-ray diffraction
2.2Å resolution

Structural Basis for Reversible and Irreversible Inhibition of Human Cathepsin L by their Respective Dipeptidyl Glyoxal and Diazomethylketone Inhibitors

Released:
DOI: 10.2210/pdb3of8/pdb
PDB entry 3of8 coloured by chain, front view.
PDB entry 3of8 coloured by chain, side view.
PDB entry 3of8 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural basis for reversible and irreversible inhibition of human cathepsin L by their respective dipeptidyl glyoxal and diazomethylketone inhibitors.
Shenoy RT, Sivaraman J
J Struct Biol 173 14-9 (2011)
PMID: 20850545

Function and Biology Details

Reaction catalysed: 
Similar to that of papain. As compared to cathepsin B, cathepsin L exhibits higher activity toward protein substrates, but has little activity on Z-Arg-Arg-NHMec, and no peptidyl-dipeptidase activity.
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-139718 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Cathepsin L Chain: A
Molecule details ›
Chain: A
Length: 221 amino acids
Theoretical weight: 24.32 KDa
Source organism: Homo sapiens
Expression system: Komagataella pastoris
UniProt:
  • Canonical: P07711 (Residues: 113-333; Coverage: 70%)
Gene names: CTSL, CTSL1
Sequence domains: Papain family cysteine protease
Structure domains: Cysteine proteinases

Ligands and Environments

1 bound ligand:
Ligand I0Y 1 x I0Y
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSLS BEAMLINE X29A
Spacegroup: P65
Unit cell:
a: 85.318Å b: 85.318Å c: 50.018Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.197 0.194 0.253
Expression system: Komagataella pastoris

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Citations

1 review citation

SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells.
Cannalire et al. (2020)
7 other articles

12 mentions without citation

The role of cysteine peptidases in coronavirus cell entry and replication: The therapeutic potential of cathepsin inhibitors.
Pišlar et al. (2020)
11 more