@article{MTMT:30883393,
	title = {Calcilytic NPS 2143 Reduces Amyloid Secretion and Increases sAβPPα Release from PSEN1 Mutant iPSC-Derived Neurons},
	url = {https://m2.mtmt.hu/api/publication/30883393},
	author = {Lo Giudice, Maria and Mihalik, Balázs and Turi, Zs and Dinnyés, András and Kobolák, Julianna},
	doi = {10.3233/JAD-190602},
	journal-iso = {J ALZHEIMERS DIS},
	journal = {JOURNAL OF ALZHEIMER'S DISEASE},
	volume = {72},
	unique-id = {30883393},
	issn = {1387-2877},
	abstract = {Despite numerous efforts and studies over the last three decades, Alzheimer's disease (AD) remains a disorder not fully understood and incurable so far. Development of induced pluripotent stem cell (iPSC) technology to obtain terminally differentiated neurons from adult somatic cells revolutionized the study of AD, providing a powerful tool for modelling the disease and for screening candidate drugs. Indeed, iPSC reprogramming allowed generation of neurons from both sporadic and familial AD patients with the promise to recapitulate the early pathological mechanisms in vitro and to identify novel targets. Interestingly, NPS 2143, a negative allosteric modulator of the calcium sensing receptor, has been indicated as a possible therapeutic for AD. In the present study, we assessed the potential of our iPSC-based familial AD cellular model as a platform for drug testing. We found that iPSC-derived neurons respond to treatment with gamma-secretase inhibitor, modifying the physiological amyloid-beta protein precursor (A beta PP) processing and amyloid-beta (A beta) secretion. Moreover, we demonstrated the expression of calcium sensing receptor (CaSR) protein in human neurons derived from healthy and familial AD subjects. Finally, we showed that calcilytic NPS 2143 induced a changing of A beta and sA beta PP alpha secreted into conditioned media and modulation of CaSR and PSEN1 expression at the plasma membrane of AD neurons. Overall, our findings suggest that NPS 2143 affects important AD processes in a relevant in vitro system of familial AD.},
	keywords = {Alzheimer's disease; amyloid; Calcium-sensing receptor; calcilytic; induced pluripotent stem cell-derived neurons; sA beta PP alpha},
	year = {2019},
	eissn = {1875-8908},
	pages = {885-899},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567; Kobolák, Julianna/0000-0002-0986-9517}
}

@misc{MTMT:30877040,
	title = {Human induced pluripotent stem cell based in vitro neurotoxicology model. Poster at The 20th International Congress on In Vitro Toxicology (ESTIV 2018) Berlin, Germany, 15-18 October 2018},
	url = {https://m2.mtmt.hu/api/publication/30877040},
	author = {Dinnyés, András and Janstova, Z and Mihalik, Balázs and Bódi-Jakus, M and Kobolák, Julianna},
	unique-id = {30877040},
	year = {2018},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567; Kobolák, Julianna/0000-0002-0986-9517}
}

@misc{MTMT:30876967,
	title = {Expression of the Calcium sensing receptor (CaSR) in neuronal cultures generated from healthy and familial Alzheimer’s disease iPSCs. Poster at Federation of European Neuroscience Societies (FENS) Berlin, Germany, 7-11 July 2018},
	url = {https://m2.mtmt.hu/api/publication/30876967},
	author = {Lo Giudice, Maria and Mihalik, Balázs and Kobolák, Julianna and Riccardi, D and Kemp, PJ. and Dinnyés, András},
	unique-id = {30876967},
	year = {2018},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567; Kobolák, Julianna/0000-0002-0986-9517}
}

@article{MTMT:27110255,
	title = {Loop F of the GABA(A) receptor alpha subunit governs GABA potency},
	url = {https://m2.mtmt.hu/api/publication/27110255},
	author = {Pálvölgyi, Adrienn and Moricz, K and Pataki, A and Mihalik, Balázs and Gigler, Gábor and Megyeri, K and Udvari, Szabolcs and Gacsályi, István and Antoni, Ferenc András},
	doi = {10.1016/j.neuropharm.2017.10.042},
	journal-iso = {NEUROPHARMACOLOGY},
	journal = {NEUROPHARMACOLOGY},
	volume = {128},
	unique-id = {27110255},
	issn = {0028-3908},
	year = {2018},
	eissn = {1873-7064},
	pages = {408-415},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567; Udvari, Szabolcs/0000-0002-0855-7845}
}

@article{MTMT:26877031,
	title = {Selective inhibition of extra-synaptic alpha 5-GABA(A) receptors by S44819, a new therapeutic agent},
	url = {https://m2.mtmt.hu/api/publication/26877031},
	author = {Etherington, Lori-An and Mihalik, Balázs and Pálvölgyi, Adrienn and Ling, István and Pallagi, Katalin and Kertesz, Szabolcs and Varga, Peter and Gunn, Ben G and Brown, Adam R and Livesey, Matthew R and Monteiro, Olivia and Belelli, Delia and Barkoczy, Jozsef and Spedding, Michael and Gacsályi, István and Antoni, Ferenc András and Lambert, Jeremy J},
	doi = {10.1016/j.neuropharm.2017.08.012},
	journal-iso = {NEUROPHARMACOLOGY},
	journal = {NEUROPHARMACOLOGY},
	volume = {125},
	unique-id = {26877031},
	issn = {0028-3908},
	abstract = {In the mammalian central nervous system (CNS) GABAA receptors (GABAARs) mediate neuronal inhibition and are important therapeutic targets. GABAARs are composed of 5 subunits, drawn from 19 proteins, underpinning expression of 20–30 GABAAR subtypes. In the CNS these isoforms are heterogeneously expressed and exhibit distinct physiological and pharmacological properties. We report the discovery of S44819, a novel tricyclic oxazolo-2,3-benzodiazepine-derivative, that selectively inhibits α5-subunit-containing GABAARs (α5-GABAARs). Current α5-GABAAR inhibitors bind to the “benzodiazepine site”. However, in HEK293 cells expressing recombinant α5-GABAARs, S44819 had no effect on 3H-flumazenil binding, but displaced the GABAAR agonist 3H-muscimol and competitively inhibited the GABA-induced responses. Importantly, we reveal that the α5-subunit selectivity is uniquely governed by amino acid residues within the α-subunit F-loop, a region associated with GABA binding. In mouse hippocampal CA1 neurons, S44819 enhanced long-term potentiation (LTP), blocked a tonic current mediated by extrasynaptic α5-GABAARs, but had no effect on synaptic GABAARs. In mouse thalamic neurons, S44819 had no effect on the tonic current mediated by δ-GABAARs, or on synaptic (α1β2γ2) GABAARs. In rats, S44819 enhanced object recognition memory and reversed scopolamine-induced impairment of working memory in the eight-arm radial maze. In conclusion, S44819 is a first in class compound that uniquely acts as a potent, competitive, selective antagonist of recombinant and native α5-GABAARs. Consequently, S44819 enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy. Given this profile, S44819 may improve cognitive function in neurodegenerative disorders and facilitate post-stroke recovery. © 2017 Elsevier Ltd},
	year = {2017},
	eissn = {1873-7064},
	pages = {353-364},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567}
}

@article{MTMT:3193426,
	title = {Loop-F of the alpha-subunit determines the pharmacologic profile of novel competitive inhibitors of GABA(A) receptors},
	url = {https://m2.mtmt.hu/api/publication/3193426},
	author = {Mihalik, Balázs and Pálvölgyi, Adrienn and Bogár, Ferenc and Megyeri, Katalin and Ling, István and Barkóczy, József and Bartha, Ferenc and Martinek, Tamás and Gacsályi, István and Antoni, Ferenc András},
	doi = {10.1016/j.ejphar.2017.01.033},
	journal-iso = {EUR J PHARMACOL},
	journal = {EUROPEAN JOURNAL OF PHARMACOLOGY},
	volume = {798},
	unique-id = {3193426},
	issn = {0014-2999},
	keywords = {GABA; molecular modelling; Nootropic Agents; GABAA antagonists; Extrasynaptic receptors; Loop-F},
	year = {2017},
	eissn = {1879-0712},
	pages = {129-136},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567; Bogár, Ferenc/0000-0002-0611-1452; Martinek, Tamás/0000-0003-3168-8066}
}

@CONFERENCE{MTMT:30611333,
	title = {Selective targeting of extra-synaptic α5-GABAreceptors by S44819 (Egis-13529), a novel competitive GABA receptorinhibitor compound},
	url = {https://m2.mtmt.hu/api/publication/30611333},
	author = {PALVOLGYI, A and ETHERINGTON, L and Mihalik, Balázs and LING, I and PALLAGI, K and KERTESZ, S and GUNN, BG and BROWN, AR and LIVESEY, MR and BELELLI, D and BARKOCZI, J and VARGA, P and SPEDDING, M and GACSALY, I and LAMBERT, JJ and Antoni, Ferenc András},
	booktitle = {Neuroscience Meeting Planner Soc. for Neuroscience},
	unique-id = {30611333},
	year = {2016},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567}
}

@{MTMT:3102671,
	title = {New dihydro-oxazinobenzodiazepine compounds, a process for their preparation and pharmaceutical compositions containing them},
	url = {https://m2.mtmt.hu/api/publication/3102671},
	author = {Kenéz, A and Bertha, Ferenc and Barkóczy, J and Antoni, Ferenc András and Gacsályi, István and Mihalik, Balázs and Gigler, Gábor and Móricz , Krisztina and Németh, Gábor and Angyalné, Pataki A and Kapus, G L and Pálvölgyi, Adrienn and Ling, István and Pethő, J and Simig, Gyula and Volk, Balázs and Koványiné Lax, Györgyi and Dancsó, András},
	unique-id = {3102671},
	year = {2015},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567; Németh, Gábor/0000-0003-3114-5125; Simig, Gyula/0000-0002-2569-6476; Volk, Balázs/0000-0002-2019-1874; Dancsó, András/0000-0001-8460-217X}
}

@article{MTMT:2920540,
	title = {A novel GABAA alpha 5 receptor inhibitor with therapeutic potential},
	url = {https://m2.mtmt.hu/api/publication/2920540},
	author = {Ling, István and Mihalik, Balázs and Etherington, LA and Kapus, G and Pálvölgyi, Adrienn and Gigler, Gábor and Kertesz, S and Gaal, A and Pallagi, K and Kiricsi, P and Szabo, E and Szénási, Gábor and Papp, L and Hársing, László Gábor and Lévay, György István and Spedding, M and Lambert, JJ and Belelli, D and Barkoczy, J and Volk, Balázs and Simig, Gyula and Gacsályi, István and Antoni, Ferenc András},
	doi = {10.1016/j.ejphar.2015.07.005},
	journal-iso = {EUR J PHARMACOL},
	journal = {EUROPEAN JOURNAL OF PHARMACOLOGY},
	volume = {764},
	unique-id = {2920540},
	issn = {0014-2999},
	abstract = {Novel 2,3-benzodiazepine and related isoquinoline derivatives, substituted at position 1 with a 2-benzothiophenyl moiety, were synthesized to produce compounds that potently inhibited the action of GABA on heterologously expressed GABAA receptors containing the alpha 5 subunit (GABAA alpha5), with no apparent affinity for the benzodiazepine site. Substitutions of the benzothiophene moiety at position 4 led to compounds with drug-like properties that were putative inhibitors of extra-synaptic GABAA alpha5 receptors and had substantial blood-brain barrier permeability. Initial characterization in vivo showed that 8-methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo [4,5-h][2,3]benzodiazepin-2-one was devoid of sedative, pro-convulsive or motor side-effects, and enhanced the performance of rats in the object recognition test. In summary, we have discovered a first-in-class GABA-site inhibitor of extra-synaptic GABAA alpha5 receptors that has promising drug-like properties and warrants further development.},
	year = {2015},
	eissn = {1879-0712},
	pages = {497-507},
	orcid-numbers = {Mihalik, Balázs/0000-0002-4302-7567; Szénási, Gábor/0000-0002-7350-6091; Hársing, László Gábor/0000-0003-1670-8591; Volk, Balázs/0000-0002-2019-1874; Simig, Gyula/0000-0002-2569-6476}
}

@article{MTMT:2506863,
	title = {Optical waveguide lightmode spectroscopic techniques for investigating membrane-bound ion channel activities.},
	url = {https://m2.mtmt.hu/api/publication/2506863},
	author = {Székács, Inna and Mike-Kaszás, Nóra and Gróf, Pál and Erdelyi, K and Szendro, I and Mihalik, Balázs and Pataki, A and Antoni, Ferenc András and Madarász, Emilia},
	doi = {10.1371/journal.pone.0081398},
	journal-iso = {PLOS ONE},
	journal = {PLOS ONE},
	volume = {8},
	unique-id = {2506863},
	issn = {1932-6203},
	abstract = {Optical waveguide lightmode spectroscopic (OWLS) techniques were probed for monitoring ion permeation through channels incorporated into artificial lipid environment. A novel sensor set-up was developed by depositing liposomes or cell-derived membrane fragments onto hydrophilic polytetrafluoroethylene (PTFE) membrane. The fibrous material of PTFE membrane could entrap lipoid vesicles and the water-filled pores provided environment for the hydrophilic domains of lipid-embedded proteins. The sensor surface was kept clean from the lipid holder PTFE membrane by a water- and ion-permeable polyethylene terephthalate (PET) mesh. The sensor set-up was tested with egg yolk lecithin liposomes containing gramicidin ion channels and with cell-derived membrane fragments enriched in GABA-gated anion channels. The method allowed monitoring the move of Na(+) and organic cations through gramicidin channels and detecting the Cl(-)-channel functions of the (alpha5beta2gamma2) GABAA receptor in the presence or absence of GABA and the competitive GABA-blocker bicuculline.},
	year = {2013},
	eissn = {1932-6203},
	orcid-numbers = {Mike-Kaszás, Nóra/0000-0002-7047-942X; Gróf, Pál/0000-0002-6488-893X; Mihalik, Balázs/0000-0002-4302-7567}
}