Biased allosteric modulators: new frontiers in GPCR drug discovery
G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
Allosteric modulation of class A GPCRs: targets, agents, and emerging concepts
EA Wold, J Chen, KA Cunningham… - Journal of medicinal …, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …
Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator
The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in
the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide …
the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide …
Overcoming the psychiatric side effects of the cannabinoid CB1 receptor antagonists: current approaches for therapeutics development
The Cannabinoid CB1 Receptor (CB1R) is involved in a variety of physiological pathways
and has long been considered a golden target for therapeutic manipulation. A large body of …
and has long been considered a golden target for therapeutic manipulation. A large body of …
Mu-Opioid receptor biased ligands: A safer and painless discovery of analgesics?
A Madariaga-Mazón, AF Marmolejo-Valencia, Y Li… - Drug discovery today, 2017 - Elsevier
Highlights•μ-OR biased agonists represent promising analgesics with improved therapeutic
profiles.•Protein-ligand interactions might account for biased ligands functional …
profiles.•Protein-ligand interactions might account for biased ligands functional …
Structural insights into CB1 receptor biased signaling
R Al-Zoubi, P Morales, PH Reggio - International journal of molecular …, 2019 - mdpi.com
The endocannabinoid system has emerged as a promising target for the treatment of
numerous diseases, including cancer, neurodegenerative disorders, and metabolic …
numerous diseases, including cancer, neurodegenerative disorders, and metabolic …
Diarylureas: Repositioning from antitumor to antimicrobials or multi-target agents against new pandemics
A Catalano, D Iacopetta, M Pellegrino, S Aquaro… - Antibiotics, 2021 - mdpi.com
Antimicrobials have allowed medical advancements over several decades. However, the
continuous emergence of antimicrobial resistance restricts efficacy in treating infectious …
continuous emergence of antimicrobial resistance restricts efficacy in treating infectious …
Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities
L Khurana, K Mackie, D Piomelli, DA Kendall - Neuropharmacology, 2017 - Elsevier
Cannabinoid pharmacology has been intensely studied because of cannabis' pervasive
medicinal and non-medicinal uses as well as for the therapeutic potential of cannabinoid …
medicinal and non-medicinal uses as well as for the therapeutic potential of cannabinoid …
[HTML][HTML] Recent advances in endocannabinoid system targeting for improved specificity: strategic approaches to targeted drug delivery
Opportunities for develo** innovative and intelligent drug delivery technologies by
targeting the endocannabinoid system are becoming more apparent. This review provides …
targeting the endocannabinoid system are becoming more apparent. This review provides …
Translational potential of allosteric modulators targeting the cannabinoid CB1 receptor
Abstract The cannabinoid type-1 (CB1) receptor, a G-protein-coupled receptor, is an
attractive target for drug discovery due to its involvement in many physiological processes …
attractive target for drug discovery due to its involvement in many physiological processes …