Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …
structures or functions that are difficult to interfere with using conventional drug design …
Improving translation of animal models of addiction and relapse by reverse translation
Critical features of human addiction are increasingly being incorporated into complementary
animal models, including escalation of drug intake, punished drug seeking and taking …
animal models, including escalation of drug intake, punished drug seeking and taking …
The nucleus accumbens: mechanisms of addiction across drug classes reflect the importance of glutamate homeostasis
The nucleus accumbens is a major input structure of the basal ganglia and integrates
information from cortical and limbic structures to mediate goal-directed behaviors. Chronic …
information from cortical and limbic structures to mediate goal-directed behaviors. Chronic …
Animal models of drug relapse and craving after voluntary abstinence: a review
Relapse to drug use during abstinence is a defining feature of addiction. During the last
several decades, this clinical scenario has been studied at the preclinical level using classic …
several decades, this clinical scenario has been studied at the preclinical level using classic …
Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors
CW Lindsley, KA Emmitte, CR Hopkins… - Chemical …, 2016 - ACS Publications
Allosteric modulation of GPCRs has initiated a new era of basic and translational discovery,
filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique …
filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique …
Factors modulating the incubation of drug and non-drug craving and their clinical implications
It was suggested in 1986 that cue-induced cocaine craving increases progressively during
early abstinence and remains high during extended periods of time. Clinical evidence now …
early abstinence and remains high during extended periods of time. Clinical evidence now …
Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
SH Li, KS Abd-Elrahman, SSG Ferguson - Pharmacology & therapeutics, 2022 - Elsevier
Glutamate is the primary excitatory neurotransmitter in the brain and plays critical roles in all
aspects of neuronal function. Disruption of normal glutamate transmission has been …
aspects of neuronal function. Disruption of normal glutamate transmission has been …
Allosteric modulation of G protein-coupled receptor signaling
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins,
regulate a wide array of physiological processes in response to extracellular signals …
regulate a wide array of physiological processes in response to extracellular signals …
Discovery and development of varenicline for smoking cessation
Introduction: Tobacco use causes one premature death every six seconds. Current smoking
cessation aids include nicotine replacement therapies, bupropion, and varenicline. Although …
cessation aids include nicotine replacement therapies, bupropion, and varenicline. Although …
International union of basic and clinical pharmacology. CXI. Pharmacology, signaling, and physiology of metabotropic glutamate receptors
KJ Gregory, C Goudet - Pharmacological reviews, 2021 - ASPET
Metabotropic glutamate (mGlu) receptors respond to glutamate, the major excitatory
neurotransmitter in the mammalian brain, mediating a modulatory role that is critical for …
neurotransmitter in the mammalian brain, mediating a modulatory role that is critical for …