The epidermal growth factor receptor as a substrate for a kinase-splitting membranal proteinase

J Biol Chem. 1988 Mar 5;263(7):3496-500.

Abstract

A brush-border membranal proteinase, which specifically clips the catalytic subunit of cAMP-dependent protein kinase, is shown to cleave the receptor for the epidermal growth factor (EGF) (Mr = 170,000) into two fragments of Mr = 140,000 and 30,000. The 140-kDa fragment retains its EGF-binding site and its EGF-dependent protein tyrosine kinase activity on exogenous substrates, but it loses its capacity to undergo self-phosphorylation. It is shown to be distinct from the 150-kDa fragment of the EGF receptor obtained by the Ca2+-activated neutral proteinase. The membranal proteinase strictly recognizes the native structure of the receptor and fails to cleave either the denatured receptor or its 150-kDa degradation product. Thus the membranal proteinase acts as a conformation-recognizing probe for both the protein-tyrosine kinase domain of the EGF receptor and the catalytic subunit of cAMP-dependent protein-Ser/Thr kinase, suggesting that the known sequence homology between these two kinases is also reflected in their conformation. The well defined 140-kDa fragment described here is useful for structure-function studies of the EGF receptor.

Publication types

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

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Animals
  • Binding Sites
  • Cyclic AMP / pharmacology
  • Edetic Acid / pharmacology
  • Endopeptidases / metabolism*
  • ErbB Receptors / metabolism*
  • Humans
  • Kidney / enzymology*
  • Kinetics
  • Microvilli / enzymology
  • Molecular Weight
  • Oligopeptides / pharmacology
  • Peptide Fragments / metabolism
  • Protease Inhibitors / pharmacology
  • Protein Conformation
  • Protein Denaturation
  • Protein Kinases / metabolism
  • Rats
  • Substrate Specificity

Substances

  • Oligopeptides
  • Peptide Fragments
  • Protease Inhibitors
  • Adenosine Triphosphate
  • chymostatin
  • Edetic Acid
  • Cyclic AMP
  • Protein Kinases
  • ErbB Receptors
  • Endopeptidases