Association of opioid agonist treatment with all-cause mortality and specific causes of death among people with opioid dependence: a systematic review and meta …

T Santo, B Clark, M Hickman, J Grebely… - JAMA …, 2021 - jamanetwork.com
Importance Mortality among people with opioid dependence is higher than that of the
general population. Opioid agonist treatment (OAT) is an effective treatment for opioid …

Protein design: From the aspect of water solubility and stability

R Qing, S Hao, E Smorodina, D Jin, A Zalevsky… - Chemical …, 2022 - ACS Publications
Water solubility and structural stability are key merits for proteins defined by the primary
sequence and 3D-conformation. Their manipulation represents important aspects of the …

Amide bond bioisosteres: Strategies, synthesis, and successes

S Kumari, AV Carmona, AK Tiwari… - Journal of medicinal …, 2020 - ACS Publications
The amide functional group plays a key role in the composition of biomolecules, including
many clinically approved drugs. Bioisosterism is widely employed in the rational …

Structure-based design of bitopic ligands for the µ-opioid receptor

A Faouzi, H Wang, SA Zaidi, JF DiBerto, T Che, Q Qu… - Nature, 2023 - nature.com
Mu-opioid receptor (µOR) agonists such as fentanyl have long been used for pain
management, but are considered a major public health concern owing to their adverse side …

Structure-based discovery of opioid analgesics with reduced side effects

A Manglik, H Lin, DK Aryal, JD McCorvy, D Dengler… - Nature, 2016 - nature.com
Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side
effects of morphine and related opioids—which include fatal respiratory depression—are …

Structural insights into µ-opioid receptor activation

W Huang, A Manglik, AJ Venkatakrishnan… - Nature, 2015 - nature.com
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …

Breaking barriers to novel analgesic drug development

AS Yekkirala, DP Roberson, BP Bean… - Nature reviews Drug …, 2017 - nature.com
Acute and chronic pain complaints, although common, are generally poorly served by
existing therapies. This unmet clinical need reflects a failure to develop novel classes of …

Transition‐Metal‐Catalyzed Selective Functionalization of C(sp3)−H Bonds in Natural Products

RR Karimov, JF Hartwig - Angewandte Chemie International …, 2018 - Wiley Online Library
Direct functionalization of natural products is important for studying the structure–activity and
structure–property relationships of these molecules. Recent advances in the transition‐metal …

Opioid-induced hyperalgesia: cellular and molecular mechanisms

LA Roeckel, GM Le Coz, C Gavériaux-Ruff, F Simonin - Neuroscience, 2016 - Elsevier
Opioids produce strong analgesia but their use is limited by a paradoxical hypersensitivity
named opioid-induced hyperalgesia (OIH) that may be associated to analgesic tolerance. In …

Mitragynine/corynantheidine pseudoindoxyls as opioid analgesics with mu agonism and delta antagonism, which do not recruit β-arrestin-2

A Váradi, GF Marrone, TC Palmer… - Journal of medicinal …, 2016 - ACS Publications
Natural products found in Mitragyna speciosa, commonly known as kratom, represent
diverse scaffolds (indole, indolenine, and spiro pseudoindoxyl) with opioid activity, providing …