Structure of the SOCS4-ElonginB/C complex reveals a distinct SOCS box interface and the molecular basis for SOCS-dependent EGFR degradation

Structure. 2007 Nov;15(11):1493-504. doi: 10.1016/j.str.2007.09.016.

Abstract

Tyrosine kinase signaling is tightly controlled by negative feedback inhibitors including suppressors of cytokine signaling (SOCS). SOCS assemble as SH2 domain substrate recognition modules in ElonginB/C-cullin ubiquitin ligases. In accordance, SOCS4 reduces STAT3 signaling from EGFR through increased receptor degradation. Variable C-termini in SOCS4-SOCS7 exclude these family members from a SOCS2-type domain arrangement in which a strictly conserved C terminus determines domain packing. The structure of the SOCS4-ElonginC-ElonginB complex reveals a distinct SOCS structural class. The N-terminal ESS helix functionally replaces the CIS/SOCS1-SOCS3 family C terminus in a distinct SH2-SOCS box interface that facilitates further interdomain packing between the extended N- and C-terminal regions characteristic for this subfamily. Using peptide arrays and calorimetry the STAT3 site in EGFR (pY(1092)) was identified as a high affinity SOCS4 substrate (K(D) = 0.5 microM) revealing a mechanism for EGFR degradation. SOCS4 also bound JAK2 and KIT with low micromolar affinity, whereas SOCS2 was specific for GH-receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Crystallography, X-Ray
  • Elongin
  • ErbB Receptors / metabolism*
  • Humans
  • Isoleucine / metabolism
  • Models, Molecular
  • Molecular Sequence Data
  • Phosphotyrosine / metabolism
  • STAT3 Transcription Factor / antagonists & inhibitors
  • STAT3 Transcription Factor / metabolism
  • Sequence Alignment
  • Suppressor of Cytokine Signaling Proteins / chemistry*
  • Suppressor of Cytokine Signaling Proteins / metabolism
  • Transcription Factors / chemistry*
  • Transcription Factors / metabolism

Substances

  • Elongin
  • SOCS4 protein, human
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • Suppressor of Cytokine Signaling Proteins
  • Transcription Factors
  • Isoleucine
  • Phosphotyrosine
  • EGFR protein, human
  • ErbB Receptors

Associated data

  • PDB/2IZV