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Structure-guided allosteric modulation of the delta opioid receptor
Abstract Opioid analgesics remain essential for pain management but are associated with significant adverse effects, including respiratory depression, tolerance, and dependence. The δ-opioid receptor (δOR) represents a promising therapeutic target for developing safer opioid analgesics with reduced adverse effects compared to conventional μ-opioid receptor-targeting drugs.
Identification of a Lipid-Exposed Extrahelical Binding Site for Positive Allosteric Modulators of the Dopamine D2 Receptor
Introduction Click to copy section linkSection link copied! Monoamine dopamine (DA) acts via G protein-coupled dopamine receptors to modulate physiological processes including motor function, reward mechanisms, and the learning process. (1) This family of five receptors (D1–5R) is divided into the Golf/s -coupled D1-like receptors (D1R and D5R) and the D2-like (D2R, D3R, and D4R) that couple to the Gαi/o/z family of G proteins to inhibit cAMP production.
Secondary Binding Site of CYP17A1 in Enhanced Sampling Simulations
Introduction Click to copy section linkSection link copied! Cancer remains a significant public health issue and ranks as the second most common cause of death. The increasing prevalence of prostate cancer (PCa) from 2014 to 2019 is particularly worrisome after a downward trend spanning two decades. (1) While considerable progress has been made in PCa treatment options, the need for more potent therapies remains pressing.
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