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Opioids and Their Receptors: Present and Emerging Concepts in Opioid Drug Discovery
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Opioids and Their Receptors: Present and Emerging Concepts in Opioid Drug Discovery
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Journal Article
Opioids and Their Receptors: Present and Emerging Concepts in Opioid Drug Discovery
2020
Overview
[...]it highlights current concepts in opioid drug discovery together with strategies to mitigate the deleterious effects of opioids. The imperative need for safer therapies for pain and other human disease states involving the opioid system continues to drive the search for novel lead molecules and the development of new mechanism-based treatment strategies. Since the structural elucidation of morphine, its skeleton and its conversion to new analogues has been constantly in the attention of medicinal chemists, aiming to discover therapeutically useful drugs and research tools. [7] explored SAR trends, at the meta-position of Phe4, of the endogenous DOR peptide Leu5-enkephalin, demonstrating that substitution at this position variously regulated DOR and MOR affinity and G protein activity, enabled the fine-tuning of β-arrestin2 recruitment to both receptors, and increased the plasma stability of the derived peptides. Increasing evidence on the heteromerization of native opioid receptors in discrete brain neuronal circuits with selective targeting of heteromers as a tool to modulate receptor activity, and multifunctional ligands, which simultaneously activate two or more targets to produce a more desirable drug profile, are emerging concepts for the development of novel therapeutic drugs and strategies, presented in the earlier cited report [2] and in two additional research articles [13,14].
Publisher
MDPI AG,MDPI
