Chapter 30. Recent Progress in the Rational Design of Peptide Hormones and Neurotransmitters

Emerging approaches in the molecular design of receptor-selective peptide ligands: conformational, topographical and dynamic considerations

“…group or by pseudoisosteric groups with different electronic properties to examine the importance of different side chain groups and their stereoelectronic properties for interaction with the receptor. 4. For cyclic peptides, systematic reduction or increase in ring size to determine the optimum ring size for biological activity.…”

“…Despite these difficulties, considerable progress has been made in the development of a rational approach to the design of peptide ligands with highly potent and specific biological and conformational properties [2][3][4][5][6][7][8][9][10][11][12][13]. In this review, we summarize some of the more useful approaches which have emerged from these studies, and assess the future developments in this area.…”

Simulations of the bis-penicillamine enkephalin in sodium chloride solution: A parameter study

“…DPDPE was designed using [D]penicillamine residues, isopropylcysteine derivatives with sulfur‐containing side chains, to form a constrained macrocyclic ring structure through the formation of a disulfide bond between the residues. DPDPE is a pharmacologically interesting molecule, developed as a synthetic neurotransmitter to map the structure of the δ‐opioid receptor 33–38. Studies demonstrated that DPDPE is the most specific and one of the most potent neurotransmitters for the δ‐opioid receptor ever found 39.…”

Simulation of the bis‐(penicillamine) enkephalin in ammonium chloride solution: A comparison with sodium chloride

“…The [ D ]penicillamine residues, isopropylcysteine derivatives, were used to form a constrained macrocyclic ring structure through the formation of a disulfide bond between the residues 25, 26. DPDPE is a well‐studied molecule, developed as a synthetic neurotransmitter to map the structure of the δ‐opioid receptor 27–32. Studies have demonstrated that DPDPE is one of the most specific and potent neurotransmitters for the δ‐opioid receptor 33.…”