Decrypting Integrins by Mixed-Solvent Molecular Dynamics Simulations

J Chem Inf Model. 2023 Jun 26;63(12):3878-3891. doi: 10.1021/acs.jcim.3c00480. Epub 2023 Jun 13.

Abstract

Integrins are a family of α/β heterodimeric cell surface adhesion receptors which are capable of transmitting signals bidirectionally across membranes. They are known for their therapeutic potential in a wide range of diseases. However, the development of integrin-targeting medications has been impacted by unexpected downstream effects including unwanted agonist-like effects. Allosteric modulation of integrins is a promising approach to potentially overcome these limitations. Applying mixed-solvent molecular dynamics (MD) simulations to integrins, the current study uncovers hitherto unknown allosteric sites within the integrin α I domains of LFA-1 (αLβ2; CD11a/CD18), VLA-1 (α1β1; CD49a/CD29), and Mac-1 (αMβ2, CD11b/CD18). We show that these pockets are putatively accessible to small-molecule modulators. The findings reported here may provide opportunities for the design of novel allosteric integrin inhibitors lacking the unwanted agonism observed with earlier as well as current integrin-targeting drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • CD18 Antigens* / metabolism
  • Lymphocyte Function-Associated Antigen-1 / metabolism
  • Macrophage-1 Antigen / metabolism
  • Molecular Dynamics Simulation*
  • Receptors, Cell Surface

Substances

  • CD18 Antigens
  • Lymphocyte Function-Associated Antigen-1
  • Macrophage-1 Antigen
  • Receptors, Cell Surface