Sortiert nach Autor

Publikationen - sortiert nach Autor

• 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.,
• 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
• 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,

• Schmiedhofer P, Vogel F, Koniuszewski F, Ernst M (2022) Cys-loop receptors on cannabinoids: All high? Front Physiol, 13
• 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
• 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

• Krenn M, Ernst M, Tomschik M, Treven M, Wagner M, Westphal D, Meitinger T, Pataraia E, Zimprich F, Aull‐Watschinger S (2019) Phenotypic variability of GABRA1 ‐related epilepsy in monozygotic twins Ann Clin Transl Neurol, 6 (11): 2317-2322
• Vasović D, Divović B, Treven M, Knutson D, Steudle F, Scholze P, Obradović A, Fabjan J, Brković B, Sieghart W, Ernst M, Cook J, Savić M (2019) Trigeminal neuropathic pain development and maintenance in rats are suppressed by a positive modulator of α6 GABA A receptors Eur. J. Pain, 23(5): 973-984

• 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
• Siebert D, Bampali K, Puthenkalam R, Varagic Z, Sarto-Jackson I, Scholze P, Sieghart W, Mihovilovic M, Schnürch M, Ernst M (2018) Engineered Flumazenil Recognition Site Provides Mechanistic Insight Governing Benzodiazepine Modulation in GABAA Receptors ACS Chem Biol, 13: 2040-2047
• Siebert D, Wieder M, Schlener L, Scholze P, Boresch S, Langer T, Schnürch M, Mihovilovic M, Richter L, Ernst M, Ecker G (2018) SAR-Guided Scoring Function and Mutational Validation Reveal Binding Mode of CGS-8216 at the α1+/γ2- Benzodiazepine Site J Chem Inf Model., 58 (8): 1682-1696
• Szodorai E, Bampali K, Romanov R, Kasper S, Hökfelt T, Ernst M, Lubec G, Harkany T (2018) Diversity matters: combinatorial information coding by GABA A receptor subunits during spatial learning and its allosteric modulation Cell Signal, 50: 142-159
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• Elgarf A, Siebert D, Steudle F, Draxler A, Li G, Huang S, Cook J, Ernst M, Scholze P (2018) Different Benzodiazepines Bind with Distinct Binding Modes to GABAA Receptors ACS Chem Biol, 13 (8): 2033-2039
• Batinić B, Stanković T, Stephen M, Kodali R, Tiruveedhula V, Li G, Scholze P, Marković B, Obradović A, Ernst M, Cook J, Savić M (2018) Attaining in vivo selectivity of positive modulation of α3βγ2 GABA A receptors in rats: A hard task! Eur Neuropsychopharmacol, 28 (8): 903-914
• 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

• Wongsamitkul N, Maldifassi M, Simeone X, Baur R, Ernst M, Sigel E (2017) α subunits in GABAA receptors are dispensable for GABA and diazepam action Sci Rep, 7 (1)
• Simeone X, Siebert D, Bampali K, Varagic Z, Treven M, Rehman S, Pyszkowski J, Holzinger R, Steudle F, Scholze P, Mihovilovic M, Schnürch M, Ernst M (2017) Molecular tools for GABAA receptors: High affinity ligands for β1-containing subtypes Sci Rep, 7 (1) : 5674

• Puthenkalam R, Hieckel M, Simeone X, Suwattanasophon C, Feldbauer R, Ecker G, Ernst M (2016) Structural Studies of GABAA Receptor Binding Sites: Which Experimental Structure Tells us What? Front Mol Neurosci, 16;9:44
• Hoerbelt P, Ramerstorfer J, Ernst M, Sieghart W, Thomson JL, Hough LB, Fleck MW (2016) Mutagenesis and computational docking studies support the existence of a histamine binding site at the extracellular b3+b3- interface of homooligomeric b3 GABA-A receptors Neuropharmacology, 108: 252-263
• Jonas O, Calligaris D, Methuku K, Poe M, Francois J, Tranghese F, Changelian A, Sieghart W, Ernst M, Pomeranz Krummel D, Cook J, Pomeroy S, Cima M, Agar N, Langer R, Sengupta S (2016) First In Vivo Testing of Compounds Targeting Group 3 Medulloblastomas Using an Implantable Microdevice as a New Paradigm for Drug Development J Biomed Nanotech, 12 (6): 1297-1302
• Stamenić T, Poe M, Rehman S, Santrač A, Divović B, Scholze P, Ernst M, Cook J, Savić M (2016) Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABAA receptors containing the α5 subunit Eur J Pharmacol, 791: 433-443

• 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
• Rycek L, Puthenkalam R, Schnürch M, Ernst M, Mihovilovic M (2015) Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands Bioorg Med Chem Lett, 25 (2): 400-403
• Yocum GT, Gallos G, Zhang Y, Jahan R, Stephen MR, Varagic Z, Puthenkalam R, Ernst M, Cook JM, Emala CW (2015) Targeting the GABAA Receptor α4 Subunit in Airway Smooth Muscle to Alleviate Bronchoconstriction Am J Respir Cell Mol Biol, Sept 25: Epub ahead of print

• Middendorp S, Puthenkalam R, Baur R, Ernst M, Sigel E (2014) Accelerated Discovery of Novel Benzodiazepine Ligands by Experiment-Guided Virtual Screening ACS Chem Biol, 9 (8): 1854-1859
• Carta V, Pangerl M, Baur R, Puthenkalam R, Ernst M, Trauner D, Sigel E (2014) A Pentasymmetric Open Channel Blocker for Cys-Loop Receptor Channels PLoS One, 9 (9): e106688
• 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
• 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

• 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
• 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