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Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand
We evolved muscarinic receptors in yeast to generate a family of G protein-coupled receptors (GPCRs) that are activated solely by a pharmacologically inert drug-like and bioavailable compoundExpand
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A SARS-CoV-2 Protein Interaction Map Reveals Targets for Drug-Repurposing
A newly described coronavirus named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which is the causative agent of coronavirus disease 2019 (COVID-19), has infected over 2.3 millionExpand
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Rapid, reversible activation of AgRP neurons drives feeding behavior in mice.
Several different neuronal populations are involved in regulating energy homeostasis. Among these, agouti-related protein (AgRP) neurons are thought to promote feeding and weight gain; however, theExpand
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Relating protein pharmacology by ligand chemistry
The identification of protein function based on biological information is an area of intense research. Here we consider a complementary technique that quantitatively groups and relates proteins basedExpand
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Remote Control of Neuronal Activity in Transgenic Mice Expressing Evolved G Protein-Coupled Receptors
Examining the behavioral consequences of selective CNS neuronal activation is a powerful tool for elucidating mammalian brain function in health and disease. Newly developed genetic, pharmacological,Expand
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DREADDs for Neuroscientists
  • B. Roth
  • Biology, Medicine
  • Neuron
  • 17 February 2016
To understand brain function, it is essential that we discover how cellular signaling specifies normal and pathological brain function. In this regard, chemogenetic technologies represent valuableExpand
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The expanded biology of serotonin.
Serotonin is perhaps best known as a neurotransmitter that modulates neural activity and a wide range of neuropsychological processes, and drugs that target serotonin receptors are used widely inExpand
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Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia
Most common central nervous system disorders — such as depression, bipolar disorder and schizophrenia — seem to be polygenic in origin, and the most effective medications have exceedingly complexExpand
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Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology
Atypical antipsychotic drugs have revolutionized the treatment of schizophrenia and related disorders. The current clinically approved atypical antipsychotic drugs are characterized by havingExpand
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Functional Selectivity and Classical Concepts of Quantitative Pharmacology
The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century, yet recent data have revealed that many ligands can differentially activate signaling pathways mediated viaExpand
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