A minimized human insulin-receptor-binding motif revealed in a Conus geographus venom insulin

Nat Struct Mol Biol. 2016 Oct;23(10):916-920. doi: 10.1038/nsmb.3292. Epub 2016 Sep 12.

Abstract

Insulins in the venom of certain fish-hunting cone snails facilitate prey capture by rapidly inducing hypoglycemic shock. One such insulin, Conus geographus G1 (Con-Ins G1), is the smallest known insulin found in nature and lacks the C-terminal segment of the B chain that, in human insulin, mediates engagement of the insulin receptor and assembly of the hormone's hexameric storage form. Removal of this segment (residues B23-B30) in human insulin results in substantial loss of receptor affinity. Here, we found that Con-Ins G1 is monomeric, strongly binds the human insulin receptor and activates receptor signaling. Con-Ins G1 thus is a naturally occurring B-chain-minimized mimetic of human insulin. Our crystal structure of Con-Ins G1 reveals a tertiary structure highly similar to that of human insulin and indicates how Con-Ins G1's lack of an equivalent to the key receptor-engaging residue PheB24 is mitigated. These findings may facilitate efforts to design ultrarapid-acting therapeutic insulins.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antigens, CD / chemistry
  • Antigens, CD / metabolism*
  • Conus Snail / metabolism*
  • Humans
  • Insulin / chemistry
  • Insulin / metabolism*
  • Models, Molecular
  • Protein Binding
  • Protein Conformation
  • Protein Multimerization
  • Receptor, Insulin / chemistry
  • Receptor, Insulin / metabolism*
  • Selenocysteine / chemistry
  • Selenocysteine / metabolism
  • Venoms / chemistry
  • Venoms / metabolism*

Substances

  • Antigens, CD
  • Insulin
  • Venoms
  • Selenocysteine
  • INSR protein, human
  • Receptor, Insulin