A monovalent mutant of cyanovirin-N provides insight into the role of multiple interactions with gp120 for antiviral activity

Biochemistry. 2007 Aug 14;46(32):9199-207. doi: 10.1021/bi700666m. Epub 2007 Jul 18.

Abstract

Cyanovirin-N (CV-N) is a 101 amino acid cyanobacterial lectin with potent antiviral activity against HIV, mediated by high-affinity binding to branched N-linked oligomannosides on the viral surface envelope protein gp120. The protein contains two carbohydrate-binding domains, A and B, each of which binds short oligomannosides independently in vitro. The interaction to gp120 could involve either a single domain or both domains simultaneously; it is not clear which mode would elicit the antiviral activity. The model is complicated by the formation of a domain-swapped dimer form, in which part of each domain is exchanged between two monomers, which contains four functional carbohydrate-binding domains. To clarify whether multivalent interactions with gp120 are necessary for the antiviral activity, we engineered a novel mutant, P51G-m4-CVN, in which the binding site on domain A has been knocked out; in addition, a [P51G] mutation prevents the formation of domain-swapped dimers under physiological conditions. Here, we present the crystal structures at 1.8 A of the free and of the dimannose-bound forms of P51G-m4-CVN, revealing a monomeric structure in which only domain B is bound to dimannose. P51G-m4-CVN binds gp120 with an affinity almost 2 orders of magnitude lower than wt CV-N and is completely inactive against HIV. The tight binding to gp120 is recovered in the domain-swapped version of P51G-m4-CVN, prepared under extreme conditions. Our findings show that the presence of at least two oligomannoside-binding sites, either by the presence of intact domains A and B or by formation of domain-swapped dimers, is essential for activity.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Amino Acid Substitution / genetics*
  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / metabolism*
  • Bacterial Proteins / chemistry*
  • Bacterial Proteins / genetics*
  • Bacterial Proteins / metabolism
  • Bacterial Proteins / physiology
  • Binding Sites / genetics
  • Carbohydrates / chemistry
  • Carrier Proteins / chemistry*
  • Carrier Proteins / genetics*
  • Carrier Proteins / metabolism
  • Carrier Proteins / physiology
  • Crystallography, X-Ray
  • HIV Envelope Protein gp120 / metabolism*
  • HIV Envelope Protein gp120 / physiology
  • Molecular Sequence Data
  • Protein Binding / genetics
  • Protein Structure, Tertiary / genetics
  • Tetrazolium Salts / metabolism
  • Thermodynamics

Substances

  • Anti-HIV Agents
  • Bacterial Proteins
  • Carbohydrates
  • Carrier Proteins
  • HIV Envelope Protein gp120
  • Tetrazolium Salts
  • 2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-5-((phenylamino)carbonyl)-2H-tetrazolium hydroxide
  • cyanovirin N

Associated data

  • PDB/2PYS
  • PDB/2Z21