2. Academic Validation
  3. Melanin Building Block as Scaffold for Dynamic Submicromolar Galectin Inhibitors

Melanin Building Block as Scaffold for Dynamic Submicromolar Galectin Inhibitors

  • ACS Omega. 2026 Mar 22;11(13):20115-20125. doi: 10.1021/acsomega.5c08192.
Emanuele Carrella 1,  Luciano Pirone 2,  Rita Russo 2,  Martina Filocaso 2 3 4,  Sonia Di Gaetano 2,  Alfonso Iadonisi 5,  Emilia Pedone 2,  Domenica Capasso 1 2 6,  Alessandro Pezzella 1 6 7 8
Affiliations

Affiliations

  • 1 Department of Physics Ettore Pancini, University of Naples Federico II, Via Cinthia 4, 80126 Naples, Italy.
  • 2 Institute of Biostructures and Bioimaging, National Research Council (CNR), Via P. Castellino 111, 80131 Naples, Italy.
  • 3 Department of Environmental, Biological and Pharmaceutical Sciences and Technologies, University of Campania "Luigi Vanvitelli", 81100 Caserta, Italy.
  • 4 Institute of Crystallography, CNR, 81100 Caserta, Italy.
  • 5 Department of Chemical Sciences, University of Naples Federico II, Via Cinthia 4, 80126 Naples, Italy.
  • 6 Bioelectronics Task Force, University of Naples Federico II, Naples 80126, Italy.
  • 7 National Interuniversity Consortium of Materials Science and Technology (INSTM), Piazza S. Marco 4, I-50121 Florence, Italy.
  • 8 Institute for Polymers Composites and Biomaterials (IPCB) CNR, via Campi Flegrei 34, I-80078 Pozzuoli (NA), Italy.
PMID: 41970859 DOI: 10.1021/acsomega.5c08192
Abstract

Galectins, β-galactoside-binding soluble proteins, are involved in a multitude of biological functions and several diseases, so numerous Galectin inhibitors, from small molecules to multivalent glycoconjugates, have been developed and investigated as tools for therapeutic applications. Notably, multivalent ligands on a biocompatible backbone offer a promising perspective for creating high-performance selective inhibitors with nanomolar affinity. Leveraging the oxidative polymerization of 5,6-dihydroxyindole (DHI), a key intermediate of eumelanin Pigments, here, we present the synthesis and complete nuclear magnetic resonance characterization of a submicromolar multivalent ligand of Galectin-3 based on a naturally biocompatible eumelanin backbone. The integration of several complementary techniques, namely, UV-vis spectrometry, dynamic light scattering, isothermal titration calorimetry, and biolayer interferometry, in the investigation of galectin-3-eumelanin-related ligand interactions, allowed us to calculate the KD and to propose a model for the protein-polymer interaction.

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