Macrocyclic supramolecular complexes demonstrate the dynamic potential to solve global
biomedical challenges, a promising cancer treatment modality. The macrocyclic system is an …

Introduction: Neurotensin is a gut-brain peptide hormone, a 13 amino acid neuropeptide
found in the central nervous system and in the GI tract. The neurotensinergic system is …

The stabilization of peptide secondary structure via stapling is a ubiquitous goal for creating
new probes, imaging agents, and drugs. Inspired by indole‐derived crosslinks found in …

The modulatory interactions between neurotensin (NT) and the dopaminergic
neurotransmitter system in the brain suggest that NT may be associated with the progression …

Neurotensin (NT) is a linear disordered peptide that activates two different class A GPCRs,
neurotensin receptor 1 (NTS 1) and NTS 2. Resolved structures of the complex of the C …

Peptides are regarded as promising next-generation therapeutics. However, an analysis of
over 1000 bioactive peptide candidates suggests that many have underdeveloped affinities …

Peptide stapling reactions represent powerful methods for structuring native α-helices to
improve their bioactivity in targeting protein–protein interactions (PPIs). In light of a growing …

Macrocycles have recognized therapeutic potential, but their limited cellular permeability
can hinder their development as oral drugs. To better understand the structure–permeability …

The opioid crisis has highlighted the urgent need to develop non‐opioid alternatives for
managing pain, with an effective, safe, and non‐addictive pharmacotherapeutic profile …

Fusion of nonopioid pharmacophores, such as neurotensin, with opioid ligands represents
an attractive approach for pain treatment. Herein, the μ-/δ-opioid agonist tetrapeptide H-Dmt …