HtrA1 activation is driven by an allosteric mechanism of inter-monomer communication

Sci Rep. 2017 Nov 1;7(1):14804. doi: 10.1038/s41598-017-14208-z.

Abstract

The human protease family HtrA is responsible for preventing protein misfolding and mislocalization, and a key player in several cellular processes. Among these, HtrA1 is implicated in several cancers, cerebrovascular disease and age-related macular degeneration. Currently, HtrA1 activation is not fully characterized and relevant for drug-targeting this protease. Our work provides a mechanistic step-by-step description of HtrA1 activation and regulation. We report that the HtrA1 trimer is regulated by an allosteric mechanism by which monomers relay the activation signal to each other, in a PDZ-domain independent fashion. Notably, we show that inhibitor binding is precluded if HtrA1 monomers cannot communicate with each other. Our study establishes how HtrA1 trimerization plays a fundamental role in proteolytic activity. Moreover, it offers a structural explanation for HtrA1-defective pathologies as well as mechanistic insights into the degradation of complex extracellular fibrils such as tubulin, amyloid beta and tau that belong to the repertoire of HtrA1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allosteric Regulation
  • Amyloid beta-Peptides / chemistry
  • Amyloid beta-Peptides / genetics
  • Amyloid beta-Peptides / metabolism
  • High-Temperature Requirement A Serine Peptidase 1 / chemistry*
  • High-Temperature Requirement A Serine Peptidase 1 / genetics
  • High-Temperature Requirement A Serine Peptidase 1 / metabolism
  • Humans
  • Protein Domains
  • Protein Multimerization*
  • Proteolysis*
  • Structure-Activity Relationship
  • Tubulin / chemistry
  • Tubulin / genetics
  • Tubulin / metabolism
  • tau Proteins / chemistry
  • tau Proteins / genetics
  • tau Proteins / metabolism

Substances

  • Amyloid beta-Peptides
  • Tubulin
  • tau Proteins
  • High-Temperature Requirement A Serine Peptidase 1
  • HTRA1 protein, human