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Papers of the Week


Papers: 30 Apr 2022 - 6 May 2022


Pharmacology/Drug Development


2022 Apr 29


Br J Pharmacol

Design and development of novel, short, stable dynorphin-based opioid agonists for safer analgesic therapy.

Authors

Lohman R-J, Tupally K R, Kandale A, Cabot PJ, Parekh HS
Br J Pharmacol. 2022 Apr 29.
PMID: 35485985.

Abstract

The kappa opioid receptor has exceptional potential as an analgesic target, seemingly devoid of the many peripheral side-effects of Mu opioid receptors. Kappa-selective, small molecule pharmaceutical agents have been developed, but centrally-mediated side effects have limited their clinical translation. Here, we modify an active endogenous dynorphin peptide to improve drug-likeness and develop safer KOPr agonists for clinical use.