Structure Determination of Mycobacterium tuberculosis Serine Protease Hip1 (Rv2224c)

Biochemistry. 2017 May 2;56(17):2304-2314. doi: 10.1021/acs.biochem.6b01066. Epub 2017 Apr 7.

Abstract

The Mycobacterium tuberculosis (Mtb) serine protease Hip1 (hydrolase important for pathogenesis; Rv2224c) promotes tuberculosis (TB) pathogenesis by impairing host immune responses through proteolysis of a protein substrate, Mtb GroEL2. The cell surface localization of Hip1 and its immunomodulatory functions make Hip1 a good drug target for new adjunctive immune therapies for TB. Here, we report the crystal structure of Hip1 to a resolution of 2.6 Å and the kinetic studies of the enzyme against model substrates and the protein GroEL2. The structure shows a two-domain protein, one of which contains the catalytic residues that are the signature of a serine protease. Surprisingly, a threonine is located within the active site close enough to hydrogen bond with the catalytic residues Asp463 and His490. Mutation of this residue, Thr466, to alanine established its importance for function. Our studies provide insights into the structure of a member of a novel family of proteases. Knowledge of the Hip1 structure will aid in designing inhibitors that could block Hip1 activity.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acid Substitution
  • Bacterial Proteins / chemistry
  • Bacterial Proteins / genetics
  • Bacterial Proteins / metabolism*
  • Biocatalysis
  • Catalytic Domain
  • Circular Dichroism
  • Crystallography, X-Ray
  • Enzyme Stability
  • Methionine / chemistry
  • Models, Molecular*
  • Mutagenesis, Site-Directed
  • Mutation
  • Mycobacterium tuberculosis / enzymology*
  • Peptide Fragments / chemistry
  • Peptide Fragments / genetics
  • Peptide Fragments / metabolism
  • Protein Conformation
  • Proteolysis
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Selenomethionine / chemistry
  • Serine Proteases / chemistry
  • Serine Proteases / genetics
  • Serine Proteases / metabolism*
  • Structural Homology, Protein
  • Substrate Specificity

Substances

  • Bacterial Proteins
  • Peptide Fragments
  • Recombinant Fusion Proteins
  • Recombinant Proteins
  • Selenomethionine
  • Methionine
  • Hip1 protein, Mycobacterium tuberculosis
  • Serine Proteases