User profiles for Spyros P Nikas
Spyros P. NikasResearch Associate Professor, Northeastern University Verified email at northeastern.edu Cited by 3440 |
Crystal structures of agonist-bound human cannabinoid receptor CB1
T Hua, K Vemuri, SP Nikas, RB Laprairie, Y Wu, L Qu… - Nature, 2017 - nature.com
The cannabinoid receptor 1 (CB 1 ) is the principal target of the psychoactive constituent of
marijuana, the partial agonist Δ 9 -tetrahydrocannabinol (Δ 9 -THC) 1 . Here we report two …
marijuana, the partial agonist Δ 9 -tetrahydrocannabinol (Δ 9 -THC) 1 . Here we report two …
Synthon-based ligand discovery in virtual libraries of over 11 billion compounds
Abstract Structure-based virtual ligand screening is emerging as a key paradigm for early drug
discovery owing to the availability of high-resolution target structures 1 , 2 , 3 – 4 and ultra-…
discovery owing to the availability of high-resolution target structures 1 , 2 , 3 – 4 and ultra-…
[PDF][PDF] Activation and signaling mechanism revealed by cannabinoid receptor-Gi complex structures
…, Y Wang, M Wu, L Shen, CA Brust, SP Nikas… - Cell, 2020 - cell.com
Human endocannabinoid systems modulate multiple physiological processes mainly through
the activation of cannabinoid receptors CB1 and CB2. Their high sequence similarity, low …
the activation of cannabinoid receptors CB1 and CB2. Their high sequence similarity, low …
[HTML][HTML] Structural basis for activation of CB1 by an endocannabinoid analog
Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …
CB1 cannabinoid receptor ligands
The CB1 receptor is expressed in the central nervous system and numerous other tissues
including heart, lung and uterus and has been recognized as an important therapeutic target …
including heart, lung and uterus and has been recognized as an important therapeutic target …
Δ9-Tetrahydrocannabinol acts as a partial agonist/antagonist in mice
Δ 9-Tetrahydrocannabinol (THC) has been characterized as a partial agonist at cannabinoid
CB1 receptors in vitro; however, it often produces the same maximum effects in vivo as …
CB1 receptors in vitro; however, it often produces the same maximum effects in vivo as …
[PDF][PDF] Inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in hypertension without adverse metabolic effects
The enzyme fatty acid amide hydrolase (FAAH) catalyzes the in vivo degradation of the
endocannabinoid anandamide, thus controlling its action at receptors. A novel FAAH inhibitor, …
endocannabinoid anandamide, thus controlling its action at receptors. A novel FAAH inhibitor, …
Novel 1′, 1′-chain substituted hexahydrocannabinols: 9β-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 …
SP Nikas, SO Alapafuja, I Papanastasiou… - Journal of medicinal …, 2010 - ACS Publications
In pursuit of a more detailed understanding of the structural requirements for the key side
chain cannabinoid pharmacophore, we have extended our SAR to cover a variety of …
chain cannabinoid pharmacophore, we have extended our SAR to cover a variety of …
Fluorescent probes for G-protein-coupled receptor drug discovery
…, RN Kulkarni, A Makriyannis, SP Nikas - Expert Opinion on …, 2018 - Taylor & Francis
Introduction: G-protein-coupled receptors (GPCRs) mediate the effects of approximately 33%
of all marketed drugs. The development of tools to study GPCR pharmacology is urgently …
of all marketed drugs. The development of tools to study GPCR pharmacology is urgently …
Cannabinoid CB2 agonist AM1710 differentially suppresses distinct pathological pain states and attenuates morphine tolerance and withdrawal
AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a
cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced …
cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced …