An Update on Non-CB1, Non-CB2 Cannabinoid Related G-Protein-Coupled Receptors

P Morales, PH Reggio - Cannabis and cannabinoid research, 2017 - liebertpub.com
The endocannabinoid system (ECS) has been shown to be of great importance in the
regulation of numerous physiological and pathological processes. To date, two Class A G …

Cannabinoid receptor CB1 and CB2 interacting proteins: Techniques, progress and perspectives

CRM Oyagawa, NL Grimsey - Methods in cell biology, 2021 - Elsevier
Abstract Cannabinoid receptors 1 and 2 (CB 1 and CB 2) are implicated in a range of
physiological processes and have gained attention as promising therapeutic targets for a …

2016 Philip S. Portoghese medicinal chemistry lectureship: designing bivalent or bitopic molecules for G-protein coupled receptors. The whole is greater than the sum …

AH Newman, FO Battiti, A Bonifazi - Journal of medicinal chemistry, 2019 - ACS Publications
The genesis of designing bivalent or bitopic molecules that engender unique
pharmacological properties began with Portoghese's work directed toward opioid receptors …

An in vitro and in vivo investigation of bivalent ligands that display preferential binding and functional activity for different melanocortin receptor homodimers

CJ Lensing, KT Freeman, SM Schnell… - Journal of medicinal …, 2016 - ACS Publications
Pharmacological probes for the melanocortin receptors have been utilized for studying
various disease states including cancer, sexual function disorders, Alzheimer's disease …

Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB2 Receptor**

P Morales, G Navarro, M Gómez‐Autet… - … A European Journal, 2020 - Wiley Online Library
Single chemical entities with potential to simultaneously interact with two binding sites are
emerging strategies in medicinal chemistry. We have designed, synthesized and functionally …

Modular one-pot strategy for the synthesis of heterobivalent tracers

T Bailly, S Bodin, V Goncalves, F Denat… - ACS Medicinal …, 2023 - ACS Publications
Bivalent ligands, ie, molecules having two ligands covalently connected by a linker, have
been gathering attention since the first description of their pharmacological potential in the …

The Olfactory Trail of Neurodegenerative Diseases

R Franco, C Garrigós, J Lillo - Cells, 2024 - mdpi.com
Alterations in olfactory functions are proposed as possible early biomarkers of
neurodegenerative diseases. Parkinson's and Alzheimer's diseases manifest olfactory …

One for the price of two… are bivalent ligands targeting cannabinoid receptor dimers capable of simultaneously binding to both receptors?

M Glass, K Govindpani, DP Furkert, DP Hurst… - Trends in …, 2016 - cell.com
Bivalent ligands bridging two G-protein-coupled receptors (GPCRs) provide valuable
pharmacological tools to target oligomers. The success of therapeutically targeting the …

New approaches in the design and development of cannabinoid receptor ligands: multifunctional and bivalent compounds

M Nimczick, M Decker - ChemMedChem, 2015 - Wiley Online Library
Since the identification of the endocannabinoid system, two G protein‐coupled receptors
(GPCRs) of this complex system were identified and characterized: cannabinoid receptors …

A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NH2 versus the Bivalent Agonist Ac-His-DPhe-Arg-Trp-PEDG20-His-DPhe-Arg-Trp …

CJ Lensing, DN Adank, SL Wilber… - ACS chemical …, 2017 - ACS Publications
Bivalent ligands targeting putative melanocortin receptor dimers have been developed and
characterized in vitro; however, studies of their functional in vivo effects have been limited …