New directions in neurosteroid therapeutics in neuropsychiatry

Authors: Zorumski, Charles F. ^{a, d, ⁎}, Covey, Douglas F. ^{a, b, c, d}, Izumi, Yukitoshi ^{a, d}, Evers, Alex S. ^{b, c, d}, Maguire, Jamie L. ^e, Mennerick, Steven J. ^d

Source: In Neuroscience and Biobehavioral Reviews May 2025 172

Inhibitory Actions of Potentiating Neuroactive Steroids in the Human α1β3γ2L γ-Aminobutyric Acid Type A Receptor

Authors: Pierce, Spencer R., Germann, Allison L., Covey, Douglas F., Evers, Alex S., Steinbach, Joe Henry, Akk, Gustav ^*

Source: In Molecular Pharmacology November 2024 106(5):264-277

Three classes of propofol binding sites on GABAA receptors

Authors: Chen, Zi-Wei, Chintala, Satyanarayana M., Bracamontes, John, Sugasawa, Yusuke, Pierce, Spencer R., Varga, Balazs R., Smith, Edward H., Edge, Christopher J., Franks, Nicholas P., Cheng, Wayland W.L., Akk, Gustav, Evers, Alex S.

Source: In Journal of Biological Chemistry October 2024 300(10)

Neurosteroids and their potential as a safer class of general anesthetics.

Authors: Tateiwa, Hiroki¹ (AUTHOR), Evers, Alex S.² (AUTHOR) eversa@wustl.edu

Source: Journal of Anesthesia. Apr2024, Vol. 38 Issue 2, p261-274. 14p.

Subject Terms: *ANESTHETICS, *NEUROTRANSMITTERS, *CENTRAL nervous system, *BINDING sites, *GENERAL anesthesia, *NEURAL development, *PREGNANOLONE

Neurosteroid enantiomers as potentially novel neurotherapeutics

Authors: Covey, Douglas F., Evers, Alex S., Izumi, Yukitoshi, Maguire, Jamie L., Mennerick, Steven J., Zorumski, Charles F.

Source: In Neuroscience and Biobehavioral Reviews June 2023 149

Perspective on the Relationship between GABAA Receptor Activity and theApparent Potency of an Inhibitor

Authors: Germann, Allison L., Pierce, Spencer R., Evers, Alex S., Steinbach, Joe Henry, Akk, Gustav

Source: CURRENT NEUROPHARMACOLOGY. 20(1):90-93

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100140379221.0x000001&indx=1&recIds=ETOCvdc_100140379221.0x000001

Neurosteroid Modulation of GABAA Receptor Function by IndependentAction at Multiple Specific Binding Sites

Authors: Wang, Lei, Covey, Douglas F., Akk, Gustav, Evers, Alex S.

Source: CURRENT NEUROPHARMACOLOGY. 20(5):886-890

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100150140020.0x000001&indx=1&recIds=ETOCvdc_100150140020.0x000001

Intrasubunit and Intersubunit Steroid Binding Sites Independently and Additively Mediate α1β2γ2L GABAA Receptor Potentiation by the Endogenous Neurosteroid Allopregnanolone

Authors: Germann, Allison L., Pierce, Spencer R., Tateiwa, Hiroki, Sugasawa, Yusuke, Reichert, David E., Evers, Alex S., Steinbach, Joe Henry, Akk, Gustav ^*

Source: In Molecular Pharmacology July 2021 100(1):19-31

Stereospecific Properties and Intracellular Transport of Novel Intrinsically Fluorescent Neurosteroids.

Authors: Akkerman, Vibeke, Reinholdt, Peter, Schnoor-Madsen, Rasmus, Lauritsen, Line, Bader, Jad, Qian, Minxing, Xu, Yuanjiang, Akk, Gustav, Scheidt, Holger A., Müller, Peter, Covey, Douglas F., Evers, Alex S., Kongsted, Jacob, Wüstner, Daniel

Source: ACS Chemical Neuroscience; 12/4/2024, Vol. 15 Issue 23, p4322-4336, 15p

Direct measurements of neurosteroid binding to specific sites on GABAA receptors.

Authors: Chintala, Satyanarayana M., Tateiwa, Hiroki, Qian, Mingxing, Xu, Yuanjian, Amtashar, Fatima, Chen, Zi‐Wei, Kirkpatrick, Charles C., Bracamontes, John, Germann, Allison L., Akk, Gustav, Covey, Douglas F., Evers, Alex S.

Source: British Journal of Pharmacology; Nov2024, Vol. 181 Issue 21, p4229-4244, 16p

Subject Terms: FLUORESCENCE resonance energy transfer, TRANSMEMBRANE domains, BINDING sites, BINDING site assay, STEROID receptors

Reduced Activation of the Synaptic-Type GABAA Receptor Following Prolonged Exposure to Low Concentrations of Agonists: Relationship between Tonic Activity and Desensitization

Authors: Pierce, Spencer R., Germann, Allison L., Evers, Alex S., Steinbach, Joe Henry, Akk, Gustav ^*

Source: In Molecular Pharmacology December 2020 98(6):762-769

Analysis of Modulation of the ρ1 GABAA Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites

Authors: Germann, Allison L., Reichert, David E., Burbridge, Ariel B., Pierce, Spencer R., Evers, Alex S., Steinbach, Joe Henry, Akk, Gustav ^*

Source: In Molecular Pharmacology October 2020 98(4):280-291

Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABAA Receptor: Relating Occupancy to State Functions

Authors: Akk, Gustav ^*, Germann, Allison L., Sugasawa, Yusuke, Pierce, Spencer R., Evers, Alex S., Steinbach, Joe Henry

Source: In Molecular Pharmacology October 2020 98(4):303-313

Roles for Anesthesiologists in the Future of Medicine in the United States

Authors: Evers, Alex S., Wiener-Kronish, Jeanine P.

Source: Anesthesia & analgesia. 134(2):231-233

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100194378251.0x000001&indx=1&recIds=ETOCvdc_100194378251.0x000001

Multiple neurosteroid and cholesterol binding sites in voltage-dependent anion channel-1 determined by photo-affinity labeling

Authors: Cheng, Wayland W.L., Budelier, Melissa M., Sugasawa, Yusuke, Bergdoll, Lucie, Queralt-Martín, María, Rosencrans, William, Rostovtseva, Tatiana K., Chen, Zi-Wei, Abramson, Jeff, Krishnan, Kathiresan, Covey, Douglas F., Whitelegge, Julian P., Evers, Alex S.

Source: In BBA - Molecular and Cell Biology of Lipids October 2019 1864(10):1269-1279

The molecular determinants of neurosteroid binding in the GABA(A) receptor

Authors: Sugasawa, Yusuke, Bracamontes, John R., Krishnan, Kathiresan, Covey, Douglas F., Reichert, David E., Akk, Gustav, Chen, Qiang, Tang, Pei, Evers, Alex S., Cheng, Wayland W.L.

Source: In Journal of Steroid Biochemistry and Molecular Biology September 2019 192

Common binding sites for cholesterol and neurosteroids on a pentameric ligand-gated ion channel

Authors: Budelier, Melissa M., Cheng, Wayland W.L., Chen, Zi-Wei, Bracamontes, John R., Sugasawa, Yusuke, Krishnan, Kathiresan, Mydock-McGrane, Laurel, Covey, Douglas F., Evers, Alex S.

Source: In BBA - Molecular and Cell Biology of Lipids February 2019 1864(2):128-136

Mapping two neurosteroid-modulatory sites in the prototypic pentameric ligand-gated ion channel GLIC

Alternate Title: Neurosteroid-binding sites in GLIC (English)

Authors: Cheng, Wayland W.L., Chen, Zi-Wei, Bracamontes, John R., Budelier, Melissa M., Krishnan, Kathiresan, Shin, Daniel J., Wang, Cunde, Jiang, Xin, Covey, Douglas F., Akk, Gustav, Evers, Alex S.

Source: In Journal of Biological Chemistry 23 February 2018 293(8):3013-3027

Photoaffinity labeling with cholesterol analogues precisely maps a cholesterol-binding site in voltage-dependent anion channel-1

Alternate Title: Cholesterol-binding sites in VDAC (English)

Authors: Budelier, Melissa M., Cheng, Wayland W.L., Bergdoll, Lucie, Chen, Zi-Wei, Janetka, James W., Abramson, Jeff ^**, Krishnan, Kathiresan, Mydock-McGrane, Laurel, Covey, Douglas F., Whitelegge, Julian P., Evers, Alex S.

Source: In Journal of Biological Chemistry 2 June 2017 292(22):9294-9304

SmartTots Update Regarding Anesthetic Neurotoxicity in the Developing Brain

Authors: Orser, Beverley A., Suresh, Santhanam, Evers, Alex S.

Source: Anesthesia & analgesia. 126(4):1393-1396

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100173566759.0x000001&indx=1&recIds=ETOCvdc_100173566759.0x000001