A5007339003- Supramolecular Self-Assembly in Materials
- Regulation of Appetite and Obesity
- Receptor Mechanisms and Signaling
- Adipose Tissue and Metabolism
- Biochemical and Structural Characterization
- Bacteriophages and microbial interactions
- Antimicrobial Peptides and Activities
- Biochemical Analysis and Sensing Techniques
- Neuropeptides and Animal Physiology
Vrije Universiteit Brussel
2022-2025
Melanocortin 4 receptor (MC4-R) antagonists are actively sought for treating cancer cachexia. We determined the structures of complexes with PG-934 and SBL-MC-31. These peptides differ from SHU9119 by substituting His6 Pro6 inserting Gly10 or Arg10. The revealed two subpockets at TM7-TM1-TM2 domains, separated N2857.36. Two peptide series based on complexed led to an antagonist activity selectivity SAR study. Most ligands retained potency, but several SBL-MC-31-derived significantly enhanced...
G protein–coupled receptor (GPCR) signaling is a dynamic process involving various conformational intermediates in addition to those captured static three-dimensional structures. Here, we used newly developed protein peptidomimetics characterize the interactions of ghrelin (GHSR) with proteins. Coupling peptidomimetic not only affected features cytoplasmic regions where binds but also allosterically extracellular ligand-binding pocket. These and allosteric changes increased affinity GHSR for...
Membrane interaction constitutes to be an essential parameter in the mode of action entities such as proteins, well cell-penetrating and antimicrobial peptides, resulting noninvasive or lytic activities depending on membrane compositions interactions. Recently, a nanobody able interact with top priority, multidrug-resistant bacterial pathogen Acinetobacter baumannii was discovered, although binding took place fixed cells only. To potentially overcome this limitation, linear peptides...