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Publikationen - sortiert nach Labs

• Milica Gajić Bojić, Marco Treven, Kamal P. Pandey, V.V.N. Phani Babu Tiruveedhula, Anja Santrač, Đorđe Đukanović , Nataša Vojinović, Ljiljana Amidžić,Ranko Škrbić, Petra Scholze, Margot Ernst, James M. Cook,Miroslav M. Savić (2023) Vascular effects of midazolam, flumazenil, and a novel imidazobenzodiazepine MP-III-058 on isolated rat aorta Can.J.Physiol.Pharmacol, (19): 2482-2499
• Koniuszewski F, Vogel F, Dajić I, Seidel T, Kunze M, Willeit M, Ernst M (2023) Navigating the complex landscape of benzodiazepine- and Z-drug diversity: insights from comprehensive FDA adverse event reporting system analysis and beyond Front Psychiatry, 14: 1188101
• Mortensen M, Xu Y, Shehata M, Krall J, Ernst M, Frølund B, Smart T (2023) Pregnenolone sulfate analogues differentially modulate GABA_A receptor closed/desensitised states Br J Pharmacol,
• Bampali K, Koniuszewski F, Vogel F, Fabjan J, Andronis C, Lekka E, Virvillis V, Seidel T, Delaunois A, Royer L, Rolf M, Giuliano C, Traebert M, Roussignol G, Fric-Bordat M, Mazelin-Winum L, Bryant S, Langer T, Ernst M (2023) GABAA receptor-mediated seizure liabilities: a mixed-methods screening approach JCB, (6): 2793-2819

• Schmiedhofer P, Vogel F, Koniuszewski F, Ernst M (2022) Cys-loop receptors on cannabinoids: All high? Front Physiol, 13: 1044575
• Garifulina A, Friesacher T, Stadler M, Zangerl-Plessl E, Ernst M, Stary-Weinzinger A, Willam A, Hering S (2022) β subunits of GABAA receptors form proton-gated chloride channels: Insights into the molecular basis Commun Biol, 5 (1)
• Simeone X, Ernst M, Seidel T, Heider J, Enz D, Monticelli S, Vogel F, Koniuszewski F, Langer T, Scholze P, Pace V, Miele M (2022) Novel alpha6 preferring GABA-A receptor ligands based on loreclezole Bioorg Med Chem, 244: 114780
• Koniuszewski F, Vogel F, Bampali K, Fabjan J, Seidel T, Scholze P, Schmiedhofer P, Langer T, Ernst M (2022) Molecular Mingling: Multimodal Predictions of Ligand Promiscuity in Pentameric Ligand-Gated Ion Channels MB, 9: 860246
• Bampali K, Koniuszewski F, Silva L, Rehman S, Vogel F, Seidel T, Scholze P, Zirpel F, Garon A, Langer T, Willeit M, Ernst M (2022) Tricyclic antipsychotics and antidepressants can inhibit α5‐containing GABA _A receptors by two distinct mechanisms Br J Pharmacol, 0: 1-18
• Vogel F, Krenn M, Westphal D, Graf E, Wagner M, Leiz S, Koniuszewski F, Augé‐Stock M, Kramer G, Scholze P, Ernst M (2022) A de novo missense variant in GABRA4 alters receptor function in an epileptic and neurodevelopmental phenotype Epilepsia, 0: 1-7

• Sieghart W, Chiou LC, Ernst M, Fabjan J, M Savić M, Lee MT (2022) α6-Containing GABAA Receptors: Functional Roles and Therapeutic Potentials Pharmacol Rev, 74(1): 238-270

• Fabjan J, Koniuszewski F, Schaar B, Ernst M (2021) Structure-Guided Computational Methods Predict Multiple Distinct Binding Modes for Pyrazoloquinolinones in GABAA Receptors Front Neurosci, 14: 611953
• Simeone X, Koniuszewski F, Müllegger M, Smetka A, Steudle F, Puthenkalam R, Ernst M, Scholze P (2021) A Benzodiazepine Ligand with Improved GABAA Receptor α5-Subunit Selectivity Driven by Interactions with Loop C Mol Pharmacol, 99 (1): 39-48

• Scholze P, Pökl M, Längle S, Steudle F, Fabjan J, Ernst M (2020) Two Distinct Populations of α1α6-Containing GABAA-Receptors in Rat Cerebellum Front.Synaptic Neuroscience, 12: 1-10
• Steudle F, Rehman S, Bampali K, Simeone X, Rona Z, Hauser E, Schmidt W, Scholze P, Ernst M (2020) A novel de novo variant of GABRA1 causes increased sensitivity for GABA in vitro Sci Rep, 10 (1): 2379
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• Iorio M, Vogel F, Koniuszewski F, Scholze P, Rehman S, Simeone X, Schnürch M, Mihovilovic M, Ernst M (2020) GABAA Receptor Ligands Often Interact with Binding Sites in the Transmembrane Domain and in the Extracellular Domain—Can the Promiscuity Code Be Cracked? Int J Mol Sci, 21 (1): 334

• Knutson D, Kodali R, Divović B, Treven M, Stephen M, Zahn N, Dobričić V, Huber A, Meirelles M, Verma R, Wimmer L, Witzigmann C, Arnold L, Chiou L, Ernst M, Mihovilovic M, Savić M, Sieghart W, Cook J (2018) Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability J Med Chem, 61 (6): 2422-2446
• Chiou L, Lee H, Ernst M, Huang W, Chou J, Chen H, Mouri A, Chen L, Treven M, Mamiya T, Fan P, Knutson D, Witzigmann C, Cook J, Sieghart W, Nabeshima T (2018) Cerebellar α6-subunit-containing GABAAreceptors: a novel therapeutic target for disrupted prepulse inhibition in neuropsychiatric disorders Br J Pharmacol, 175 (12): 2414-2427
• Fan P, Lai T, Hor C, Lee M, Huang P, Sieghart W, Ernst M, Knutson D, Cook J, Chiou L (2018) The α6 subunit-containing GABAA receptor: A novel drug target for inhibition of trigeminal activation Neuropharmacology, 140: 1-13
• Treven M, Siebert D, Holzinger R, Bampali K, Fabjan J, Varagic Z, Wimmer L, Steudle F, Scholze P, Schnürch M, Mihovilovic M, Ernst M (2018) Towards Functional Selectivity for α6β3γ2 GABAA Receptors: A Series of Novel Pyrazoloquinolinones Br J Pharmacol, 175 (3): 419-428

• Ernst M, Sieghart W (2015) GABAA – Rezeptorsubtypen: Strukturelle Vielfalt gibt Hoffnung auf neue Therapiekonzepte Neuroforum, 21 (4): 144-151
• Ernst M, Sieghart W (2015) GABAA receptor subtypes: structural variety raises hope for new therapy concepts e-Neuroforum, 6 (4): 97-103

• Mirheydari P, Ramerstorfer J, Varagic Z, Scholze P, Wimmer L, Mihovilovic MM, Sieghart W, Ernst M (2014) Unexpected properties of delta-containing GABA-A receptors in response to ligands interacting with the alpha+beta-site Neurochem Res, 39 (6): 1057-1067

• Baur R, Kielar M, Richter L, Ernst M, Ecker G, Sigel E (2013) Molecular analysis of the site for 2-arachidonylglycerol (2-AG) on the β 2 subunit of GABA A receptors J Neurochem, 126 (1): 29-36
• Joksimovic S, Varagic Z, Kovacevic J, Van Linn M, Milic M, Rallapali S, Timic T, Sieghart W, Cook JM, Savic MM (2013) Insights into functional pharmacology of alpha1 GABA-A receptors: how much does partial activation at the benzodiazepine site matter? Psychopharmycol, 230: 113-123
• Varagic Z, Ramerstorfer J, Huang S, Rallapalli S, Sarto-Jackson I, Cook J, Sieghart W, Ernst M (2013) Subtype selectivity of alpha+beta-site ligands of GABA-A receptors - identification of the first highly specific positive modulators at alpha6beta2/3gamma2 receptors Br J Pharmacol, 169(2): 384-399
• Varagic Z, Wimmer L, Schnuerch M, Mihovilovic MD, Huang S, Rallapalli S, Cook JM, Mirheydari P, Ecker GF, Sieghart W, Ernst M (2013) Identification of novel positive allosteric modulators and null modulators at the GABA-a receptor alpha+beta-interface Br J Pharmacol, 169(2): 371-383
• Namjoshi OA, Wang Z-J, Rallapalli SK, Johnson EM Jr, Johnson Y-T, Ng H, Ramerstorfer J, Varagic Z, Sieghart W, Majumder S, Roth BL, Rowlett JK, Cook JM (2013) Search for alpha3beta2/3gamma2 subtype selective ligands that are stableon human liver microsomes Bioorg Med Chem, 21: 93-101

• Richter L, de Graaf C, Sieghart W, Varagic Z, Mörzinger M, de Esch IJP, Ecker GF, Ernst M (2012) Diazepam-bound GABA-A receptor models identify new benzodiazepine binding-site ligands Nature Chem Biol, 8: 455-464
• Spurny R, Ramerstorfer J, Price K, Brams M, Ernst M, Nury H, Verheij M, Legrand P, Bertrand D, Bertrand S, Dougherty DA, de Esch IJ, Corringer PJ, Sieghart W, Lummis SC, Ulens C (2012) Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines Proc Natl Acad Sci USA, 109(44): E3028-34
• Joksimovic S, Divljakovic J, Van Linn ML, Varagic Z, Brajkovic G, Milinkovic MM, Yin W, Timic T, Sieghart W, Cook JM, Savic MM (2012) Benzodiazepine-induced spatial learning deficits in rats are regulated by the degree of modulation of a1 GABA-A receptors Eur Neuropsychopharmacol, 23: 390-399
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• Richter L, de Graaf C, Sieghart W, Varagic Z, Mörzinger M, de Esch IJP, Ecker GF, Ernst M (2012) Diazepam-bound GABA-A receptor models identify new benzodiazepine binding site ligands Nature Chem Biol, 8: 455-464
• Sieghart W, Ramerstorfer J, Sarto-Jackson I, Varagic Z, Ernst M (2012) A novel GABA-A receptor pharmacology: drugs interacting with the alpha+beta-interface Br J Pharmacol, 166: 476-485

• Ramerstorfer J, Furtmüller R, Sarto-Jackson I, Varagic Z, Sieghart W, Ernst M (2011) The GABA-A receptor alpha+beta-interface: a novel target for subtype-selective drugs J Neurosci, 31: 870-877

• Tan KR, Gonthier A, Baur R, Ernst M, Goeldner M, Sigel E (2007) Proximity-Accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators J Biol Chem, 282: 26316-26325
• Sarto-Jackson I, Furtmüller R, Ernst M, Huck S, Sieghart W (2007) Spontaneous cross-link of mutated alpha1 subunits during GABA-A receptor assembly J Biol Chem, 282: 4354-4363
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• Clayton T, Chen JL, Ernst M, Richter L, Cromer BA, Morton CJ, Ng H, Kaczorowski CC, Helmstetter FJ, Furtmüller R, Ecker G, Parker MW, Sieghart W, Cook JM (2007) An updated unified pharmacophore model of the benzodiazepine binding site of gamma-aminobutyric acid(a) receptors: correlation with comparative models Current Topics in Medicinal Chemistry, 14: 2755-2775
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• Sarto-Jackson I, Ramerstorfer J, Ernst M, Sieghart W (2006) Identification of amino acid residues important for assembly of GABA-A receptor alpha1 and gamma2 subunits J Neurochem, 96: 983-995
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• Ernst M, Bruckner S, Boresch S, Sieghart W (2005) Comparative models of GABA-A receptor extracellular and transmembrane domains: important insights in pharmacology and function Mol Pharmacol, 68: 1291-1300
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• Sieghart W, Ernst M (2005) Heterogeneity of GABA-A receptors: revived interest in the development of subtype-selective drugs Curr Med Chem - Centr Nervous Syst, 5: 217-242
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• Ogris W, Pöltl A, Hauer B, Ernst M, Oberto A, Wulff P, Höger H,Wisden W, Sieghart W (2004) Affinity of various benzodiazepine site ligands in mice with a point mutation in the GABAA receptor gamma2 subunit Biochem Pharmacol, 68: 1621-1629
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• Ernst M, Brauchart D, Boresch S, and Sieghart W (2003) Comparative modeling of GABAA receptors: limits, insights, future developments Neuroscience, 119: 933-943