Alex S. Evers
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View article: Properties of Acute Activation and Inhibition of the β3 Homomeric GABA<sub>A</sub> Receptor Mediated by Protonation of Conserved Histidine Residues
Properties of Acute Activation and Inhibition of the β3 Homomeric GABA<sub>A</sub> Receptor Mediated by Protonation of Conserved Histidine Residues Open
GABAA receptors are inhibitory transmitter-gated ion channels formed of various combinations of the 19 homologous subunits cloned to date. Changes in extracellular pH have been shown to directly activate the receptor or modulate…
View article: New directions in neurosteroid therapeutics in neuropsychiatry
New directions in neurosteroid therapeutics in neuropsychiatry Open
In recent years three neuroactive steroids (NAS), brexanolone (allopregnanolone, AlloP), ganaxolone and zuranolone, have been approved for the treatment of neuropsychiatric illnesses including postpartum depression and seizures in a neurod…
View article: A propofol binding site in the voltage sensor domain mediates inhibition of HCN1 channel activity
A propofol binding site in the voltage sensor domain mediates inhibition of HCN1 channel activity Open
Hyperpolarization-activated and cyclic nucleotide–gated (HCN) ion channels are members of the cyclic nucleotide–binding family and are crucial for regulating cellular automaticity in many excitable cells. HCN channel activation contributes…
View article: Stereospecific Properties and Intracellular Transport of Novel Intrinsically Fluorescent Neurosteroids
Stereospecific Properties and Intracellular Transport of Novel Intrinsically Fluorescent Neurosteroids Open
Allopregnanolone (AlloP) is an example of neuroactive steroids (NAS), which is a potent allosteric activator of the γ-aminobutyric acid A (GABAA) receptor. The mechanisms underlying the biological activity of AlloP and ot…
View article: Three classes of propofol binding sites on GABAA receptors
Three classes of propofol binding sites on GABAA receptors Open
Propofol is a widely used anesthetic and sedative that acts as a positive allosteric modulator of gamma-aminobutyric acid type A (GABAA) receptors. Several potential propofol binding sites that may mediate this effect have been …
View article: Inhibitory Actions of Potentiating Neuroactive Steroids in the Human α1β3γ2L γ-Aminobutyric Acid Type A Receptor
Inhibitory Actions of Potentiating Neuroactive Steroids in the Human α1β3γ2L γ-Aminobutyric Acid Type A Receptor Open
View article: Direct measurements of neurosteroid binding to specific sites on GABA<sub>A</sub> receptors
Direct measurements of neurosteroid binding to specific sites on GABA<sub>A</sub> receptors Open
Background and Purpose Neurosteroids are allosteric modulators of GABA A currents, acting through several functional binding sites although their affinity and specificity for each site are unknown. The goal of this study was to measure ste…
View article: Comparison of Behavioral Effects of GABAergic Low- and High-Efficacy Neuroactive Steroids in the Zebrafish Larvae Assay
Comparison of Behavioral Effects of GABAergic Low- and High-Efficacy Neuroactive Steroids in the Zebrafish Larvae Assay Open
Activation of the GABAA receptor is associated with numerous behavioral end points ranging from anxiolysis to deep anesthesia. The specific behavioral effect of a GABAergic compound is considered to correlate with the degree of …
View article: GPR161 structure uncovers the redundant role of sterol-regulated ciliary cAMP signaling in the Hedgehog pathway
GPR161 structure uncovers the redundant role of sterol-regulated ciliary cAMP signaling in the Hedgehog pathway Open
View article: Neurosteroids and their potential as a safer class of general anesthetics
Neurosteroids and their potential as a safer class of general anesthetics Open
View article: Synthesis and evaluation of photoaffinity labeling reagents for identifying binding sites of sulfated neurosteroids on NMDA and GABA<sub>A</sub> receptors
Synthesis and evaluation of photoaffinity labeling reagents for identifying binding sites of sulfated neurosteroids on NMDA and GABA<sub>A</sub> receptors Open
Photoaffinity labels (PALs) for sulfated steroid binding sites on GABA A and NMDA receptors. The PALs have varying profiles of positive and negative modulatory (PAM and NAM) actions.
View article: GPR161 structure uncovers the redundant role of sterol-regulated ciliary cAMP signaling in the Hedgehog pathway
GPR161 structure uncovers the redundant role of sterol-regulated ciliary cAMP signaling in the Hedgehog pathway Open
The orphan G protein-coupled receptor (GPCR) GPR161 is enriched in primary cilia, where it plays a central role in suppressing Hedgehog signaling 1 . GPR161 mutations lead to developmental defects and cancers 2,3,4 . The fundamental basis …
View article: Neurosteroid enantiomers as potentially novel neurotherapeutics
Neurosteroid enantiomers as potentially novel neurotherapeutics Open
View article: The Mechanism of Enantioselective Neurosteroid Actions on GABAA Receptors
The Mechanism of Enantioselective Neurosteroid Actions on GABAA Receptors Open
The neurosteroid allopregnanolone (ALLO) and pregnanolone (PREG), are equally effective positive allosteric modulators (PAMs) of GABAA receptors. Interestingly, the PAM effects of ALLO are strongly enantioselective, whereas those of PREG a…
View article: Lysosomal GPCR-like protein LYCHOS signals cholesterol sufficiency to mTORC1
Lysosomal GPCR-like protein LYCHOS signals cholesterol sufficiency to mTORC1 Open
Lysosomes coordinate cellular metabolism and growth upon sensing of essential nutrients, including cholesterol. Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling (LYCHOS, previously annota…
View article: Roles for Anesthesiologists in the Future of Medicine in the United States
Roles for Anesthesiologists in the Future of Medicine in the United States Open
See Articles, p 235 and p 242 In this issue of Anesthesia & Analgesia, 2 articles focus on future roles for anesthesiologists and the future of anesthesiology as a specialty. The first, "Anesthesiologists as Health System Leaders: Why It W…
View article: Neurosteroid Modulation of GABA<sub>A</sub> Receptor Function by IndependentAction at Multiple Specific Binding Sites
Neurosteroid Modulation of GABA<sub>A</sub> Receptor Function by IndependentAction at Multiple Specific Binding Sites Open
: Neurosteroids are endogenous modulators of GABAA receptors that mediate anxiety, pain, mood and arousal. The 3-hydroxyl epimers, allopregnanolone (3α-OH) and epiallopregnanolone (3β-OH) are both prevalent in the mammalian brain and produ…
View article: Validation of Trifluoromethylphenyl Diazirine Cholesterol Analogues As Cholesterol Mimetics and Photolabeling Reagents
Validation of Trifluoromethylphenyl Diazirine Cholesterol Analogues As Cholesterol Mimetics and Photolabeling Reagents Open
Aliphatic diazirine analogues of cholesterol have been used previously to elaborate the cholesterol proteome and identify cholesterol binding sites on proteins. Cholesterol analogues containing the trifluoromethylphenyl diazirine (TPD) gro…
View article: Intrasubunit and Intersubunit Steroid Binding Sites Independently and Additively Mediate α1β2γ2L GABAA Receptor Potentiation by the Endogenous Neurosteroid Allopregnanolone
Intrasubunit and Intersubunit Steroid Binding Sites Independently and Additively Mediate α1β2γ2L GABAA Receptor Potentiation by the Endogenous Neurosteroid Allopregnanolone Open
View article: Protocol for a proof-of-concept observational study evaluating the potential utility and acceptability of a telemedicine solution for the post-anesthesia care unit
Protocol for a proof-of-concept observational study evaluating the potential utility and acceptability of a telemedicine solution for the post-anesthesia care unit Open
Introduction: The post-anesthesia care unit (PACU) is a clinical area designated for patients recovering from invasive procedures. There are typically several geographically dispersed PACUs within hospitals. Patients in the PACU can be uns…
View article: Reduced Activation of the Synaptic-Type GABAA Receptor Following Prolonged Exposure to Low Concentrations of Agonists: Relationship between Tonic Activity and Desensitization
Reduced Activation of the Synaptic-Type GABAA Receptor Following Prolonged Exposure to Low Concentrations of Agonists: Relationship between Tonic Activity and Desensitization Open
View article: Site-specific effects of neurosteroids on GABAA receptor activation and desensitization
Site-specific effects of neurosteroids on GABAA receptor activation and desensitization Open
This study examines how site-specific binding to three identified neurosteroid-binding sites in the α 1 β 3 GABA A receptor (GABA A R) contributes to neurosteroid allosteric modulation. We found that the potentiating neurosteroid, allopreg…
View article: Author response: Site-specific effects of neurosteroids on GABAA receptor activation and desensitization
Author response: Site-specific effects of neurosteroids on GABAA receptor activation and desensitization Open
Article Figures and data Abstract Introduction Results Discussion Materials and methods Data availability References Decision letter Author response Article and author information Metrics Abstract This study examines how site-specific bind…
View article: Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABAA Receptor: Relating Occupancy to State Functions
Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABAA Receptor: Relating Occupancy to State Functions Open
View article: Analysis of Modulation of the ρ1 GABAA Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites
Analysis of Modulation of the ρ1 GABAA Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites Open
View article: Site-specific effects of neurosteroids on GABA<sub>A</sub>receptor activation and desensitization
Site-specific effects of neurosteroids on GABA<sub>A</sub>receptor activation and desensitization Open
This study examines how site-specific binding to the three identified neurosteroid binding sites in the α 1 β 3 GABA A receptor (GABA A R) contributes to neurosteroid allosteric modulation. We found that the potentiating neurosteroid, allo…
View article: The Molecular Mechanisms of Cholesterol Regulation of Kir Channels Revealed by Direct and Quantitative Approaches
The Molecular Mechanisms of Cholesterol Regulation of Kir Channels Revealed by Direct and Quantitative Approaches Open
View article: Multiple neurosteroid and cholesterol binding sites in voltage-dependent anion channel-1 determined by photo-affinity labeling
Multiple neurosteroid and cholesterol binding sites in voltage-dependent anion channel-1 determined by photo-affinity labeling Open
View article: The molecular determinants of neurosteroid binding in the GABA(A) receptor
The molecular determinants of neurosteroid binding in the GABA(A) receptor Open
View article: Multiple functional neurosteroid binding sites on GABAA receptors
Multiple functional neurosteroid binding sites on GABAA receptors Open
Neurosteroids are endogenous modulators of neuronal excitability and nervous system development and are being developed as anesthetic agents and treatments for psychiatric diseases. While gamma amino-butyric acid Type A (GABAA) receptors a…