Pathogenic ACVR1R206H activation by Activin A-induced receptor clustering and autophosphorylation

EMBO J. 2021 Jul 15;40(14):e106317. doi: 10.15252/embj.2020106317. Epub 2021 May 18.

Abstract

Fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG) are debilitating diseases that share causal mutations in ACVR1, a TGF-β family type I receptor. ACVR1R206H is a frequent mutation in both diseases. Pathogenic signaling via the SMAD1/5 pathway is mediated by Activin A, but how the mutation triggers aberrant signaling is not known. We show that ACVR1 is essential for Activin A-mediated SMAD1/5 phosphorylation and is activated by two distinct mechanisms. Wild-type ACVR1 is activated by the Activin type I receptors, ACVR1B/C. In contrast, ACVR1R206H activation does not require upstream kinases, but is predominantly activated via Activin A-dependent receptor clustering, which induces its auto-activation. We use optogenetics and live-imaging approaches to demonstrate Activin A-induced receptor clustering and show it requires the type II receptors ACVR2A/B. Our data provide molecular mechanistic insight into the pathogenesis of FOP and DIPG by linking the causal activating genetic mutation to disrupted signaling.

Keywords: ACVR1R206H; Activin A; DIPG; FOP; receptor clustering.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Activin Receptors, Type I / genetics*
  • Activin Receptors, Type I / metabolism*
  • Activins / genetics*
  • Activins / metabolism*
  • Animals
  • Cell Line
  • Cluster Analysis
  • HEK293 Cells
  • Humans
  • Mice
  • Mutation / genetics
  • Myositis Ossificans / genetics
  • NIH 3T3 Cells
  • Phosphorylation / genetics*
  • Signal Transduction / genetics

Substances

  • activin A
  • Activins
  • ACVR1 protein, human
  • Activin Receptors, Type I