Binding site plasticity in viral PPxY Late domain recognition by the third WW domain of human NEDD4

M Iglesias-Bexiga, A Palencia, C Corbi-Verge… - Scientific Reports, 2019 - nature.com
M Iglesias-Bexiga, A Palencia, C Corbi-Verge, P Martin-Malpartida, FJ Blanco, MJ Macias
Scientific Reports, 2019nature.com
The recognition of PPxY viral Late domains by the third WW domain of the HECT-E3
ubiquitin ligase NEDD4 (hNEDD4-WW3) is essential for the completion of the budding
process of numerous enveloped viruses, including Ebola, Marburg, HTLV1 or Rabies.
hNEDD4-WW3 has been validated as a promising target for the development of novel host-
oriented broad spectrum antivirals. Nonetheless, finding inhibitors with good properties as
therapeutic agents remains a challenge since the key determinants of binding affinity and …
Abstract
The recognition of PPxY viral Late domains by the third WW domain of the HECT-E3 ubiquitin ligase NEDD4 (hNEDD4-WW3) is essential for the completion of the budding process of numerous enveloped viruses, including Ebola, Marburg, HTLV1 or Rabies. hNEDD4-WW3 has been validated as a promising target for the development of novel host-oriented broad spectrum antivirals. Nonetheless, finding inhibitors with good properties as therapeutic agents remains a challenge since the key determinants of binding affinity and specificity are still poorly understood. We present here a detailed structural and thermodynamic study of the interactions of hNEDD4-WW3 with viral Late domains combining isothermal titration calorimetry, NMR structural determination and molecular dynamics simulations. Structural and energetic differences in Late domain recognition reveal a highly plastic hNEDD4-WW3 binding site that can accommodate PPxY-containing ligands with varying orientations. These orientations are mostly determined by specific conformations adopted by residues I859 and T866. Our results suggest a conformational selection mechanism, extensive to other WW domains, and highlight the functional relevance of hNEDD4-WW3 domain conformational flexibility at the binding interface, which emerges as a key element to consider in the search for potent and selective inhibitors of therapeutic interest.
nature.com
以上显示的是最相近的搜索结果。 查看全部搜索结果