@article{MTMT:34043898,
	title = {Synthesis of tritium-labeled Lu-PSMA-617: Alternative tool for biological evaluation of radiometal-based pharmaceuticals},
	url = {https://m2.mtmt.hu/api/publication/34043898},
	author = {Bauder-Wuest, Ulrike and Schaefer, Martin and Winter, Ruth and Remde, Yvonne and Roscher, Mareike and Breyl, Heinz and Poethko, Thorsten and Tömböly, Csaba and Benesova-Schaefer, Martina},
	doi = {10.1016/j.apradiso.2023.110819},
	journal-iso = {APPL RADIAT ISOTOPES},
	journal = {APPLIED RADIATION AND ISOTOPES},
	volume = {197},
	unique-id = {34043898},
	issn = {0969-8043},
	abstract = {This project focuses on the generation and evaluation of functional alternatives to radiometal-based pharmaceuticals supporting basic research and the in vitro developmental phase. Employing robust tritium chemistry and non-radioactive metal surrogates in two synthetic and labeling strategies resulted in ([ring-3H]Nal)PSMA-617 and ([alpha,ss-3H]Nal)PSMA-617. In particular, ([alpha,ss-3H]Nal)Lu-PSMA-617 exhibited high radiolytic as well as metalcomplex stability and was compared to the clinically-established radiopharmaceutical [177Lu]Lu-PSMA-617. The cell-based assays confirmed the applicability of ([alpha,ss-3H]Nal)Lu-PSMA-617 as a substitute of [177Lu]Lu-PSMA617 in pre-clinical biological settings.},
	keywords = {Tritium; DRUG DISCOVERY; Prostate cancer; PROSTATE-CANCER; PHARMACEUTICAL DEVELOPMENT; Chemistry, Inorganic & Nuclear; Nuclear Science & Technology; radiometals; RADIATION-DOSIMETRY; PSMA-617; PSMA ligands; PSMA INHIBITOR},
	year = {2023},
	eissn = {1872-9800}
}

@article{MTMT:33831570,
	title = {Focusing on the 5F-MDMB-PICA, 4F-MDMB-BICA synthetic cannabinoids and their primary metabolites in analytical and pharmacological aspects},
	url = {https://m2.mtmt.hu/api/publication/33831570},
	author = {Dvorácskó, Szabolcs and Körmöczi, Tímea and Sija, Éva and Bende, Balázs and Weiczner, Roland and Varga, Tibor and Ilisz, István and Institóris, László and Kereszty, Éva Margit and Tömböly, Csaba and Berkecz, Róbert},
	doi = {10.1016/j.taap.2023.116548},
	journal-iso = {TOXICOL APPL PHARM},
	journal = {TOXICOLOGY AND APPLIED PHARMACOLOGY},
	volume = {470},
	unique-id = {33831570},
	issn = {0041-008X},
	year = {2023},
	eissn = {1096-0333},
	orcid-numbers = {Körmöczi, Tímea/0000-0002-0973-2473; Weiczner, Roland/0000-0002-5990-2661; Ilisz, István/0000-0001-8282-457X; Kereszty, Éva Margit/0000-0001-7196-6150; Berkecz, Róbert/0000-0002-9076-2177}
}

@article{MTMT:33723359,
	title = {Rimonabant-Based Compounds Bearing Hydrophobic Amino Acid Derivatives as Cannabinoid Receptor Subtype 1 Ligands},
	url = {https://m2.mtmt.hu/api/publication/33723359},
	author = {Dvorácskó, Szabolcs and Dimmito, Marilisa Pia and Sebastiani, Jessica and La, Regina Giuseppe and Silvestri, Romano and Pieretti, Stefano and Stefanucci, Azzurra and Tömböly, Csaba and Mollica, Adriano},
	doi = {10.1021/acsmedchemlett.3c00024},
	journal-iso = {ACS MED CHEM LETT},
	journal = {ACS MEDICINAL CHEMISTRY LETTERS},
	volume = {14},
	unique-id = {33723359},
	issn = {1948-5875},
	abstract = {In this study, 1H-pyrazole-3-carboxylic acids related to the cannabinoid type 1 (CB1) receptor antagonist rimonabant were amidated with valine or tert-leucine, and the resulting acids were further diversified as methyl esters, amides, and N-methyl amides. In vitro receptor binding and functional assays demon-strated a wide series of activities related to the CB1 receptors (CB1Rs). Compound 34 showed a high CB1R binding affinity (Ki = 6.9 nM) and agonist activity (EC50 = 46 nM; Emax = 135%). Radioligand binding and [35S]GTP gamma S binding assays also demonstrated its selectivity and specificity to CB1Rs. Moreover, in vivo experiments revealed that 34 was slightly more effective than the CB1 agonist WIN55,212-2 in the early phase of the formalin test, indicating a short duration of the analgesic effect. Interestingly, in a mouse model of zymosan-induced hindlimb edema, 34 was able to maintain the percentage of paw volume below 75% for 24 h following subcutaneous injection. After intraperitoneal administration, 34 increased the food intake of mice, suggesting potential activity on CB1Rs.},
	keywords = {CB1; AGONIST; RISK-FACTORS; rimonabant; cannabinoid; ENDOCANNABINOID SYSTEM; Anti-nociception; orexigenic agent; anorexant},
	year = {2023},
	pages = {479-486}
}

@article{MTMT:32235213,
	title = {Characterization of a functional V-1B vasopressin receptor in the male rat kidne evidence for cross talk between V-1B and V-2 receptor signaling pathways},
	url = {https://m2.mtmt.hu/api/publication/32235213},
	author = {Hus-Citharel, Annette and Bouby, Nadine and Corbani, Maithe and Mion, Julie and Mendre, Christiane and Darusi, Judit and Tömböly, Csaba and Trueba, Miguel and Serradeil-Le, Gal Claudine and Llorens-Cortes, Catherine and Guillon, Gilles},
	doi = {10.1152/ajprenal.00081.2021},
	journal-iso = {AM J PHYSIOL RENAL},
	journal = {AMERICAN JOURNAL OF PHYSIOLOGY: RENAL PHYSIOLOGY},
	volume = {321},
	unique-id = {32235213},
	issn = {1931-857X},
	abstract = {Although vasopressin V-1B receptor (V1BR) mRNA has been detected in the kidney, the precise renal localization as well as pharmacological and physiological properties of this receptor remain unknown. Using the selective V-1B agonist d[Leu(4), Lys(8)]VP, either fluorescent or radioactive, we showed that V1BR is mainly present in principal cells of the inner medullary collecting duct (IMCD) in the male rat kidney. Protein and mRNA expression of V1BR were very low compared with the V-2 receptor (V2R). On the microdissected IMCD, d[Leu(4), Lys(8)]VP had no effect on cAMP production but induced a dose-dependent and saturable intracellular Ca2+ concentration increase mobilization with an EC50 value in the nanomolar range. This effect involved both intracellular Ca2+ mobilization and extracellular Ca2+ influx. The selective V-1B antagonist SSR149415 strongly reduced the ability of vasopressin to increase intracellular Ca2+ concentration but also cAMP, suggesting a cooperation between V1BR and V2R in IMCD cells expressing both receptors. This cooperation arises from a cross talk between second messenger cascade involving PKC rather than receptor heterodimerization, as supported by potentiation of arginine vasopressin-stimulated cAMP production in human embryonic kidney-293 cells coexpressing the two receptor isoforms and negative results obtained by bioluminescence resonance energy transfer experiments. In vivo, only acute administration of high doses of V-1B agonist triggered significant diuretic effects, in contrast with injection of selective V-2 agonist. This study brings new data on the localization and signaling pathways of V1BR in the kidney, highlights a cross talk between V1BR and V2R in the IMCD, and suggests that V1BR may counterbalance in some pathophysiological conditions the antidiuretic effect triggered by V2R activation. NEW & NOTEWORTHY Although V1BR mRNA has been detected in the kidney, the precise renal localization as well as pharmacological and physiological properties of this receptor remain unknown. Using original pharmaceutical tools, this study brings new data on the localization and signaling pathways of V1BR, highlights a cross talk between V1BR and V-2 receptor (V2R) in the inner medullary collecting duct, and suggests that V1BR may counterbalance in some pathophysiological conditions the antidiuretic effect triggered by V2R activation.},
	keywords = {PHARMACOLOGICAL CHARACTERIZATION; calcium; ADENYLATE-CYCLASE; ARGININE-VASOPRESSIN; OXYTOCIN; CA2+; WATER; physiology; Diuresis; V1b; inner medullary collecting duct; calcium and cAMP signaling; receptor heterodimerization; COLLECTING TUBULE CELLS},
	year = {2021},
	eissn = {1522-1466},
	pages = {F305-F321}
}

@article{MTMT:32178981,
	title = {Selective antiproliferative effect of C-2 halogenated 13α-estrones on cells expressing Organic anion-transporting polypeptide 2B1 (OATP2B1)},
	url = {https://m2.mtmt.hu/api/publication/32178981},
	author = {Laczkó-Rigó, Réka and Bakos, Éva and Jójárt, Rebeka and Tömböly, Csaba and Mernyák, Erzsébet and Laczka, Csilla},
	doi = {10.1016/j.taap.2021.115704},
	journal-iso = {TOXICOL APPL PHARM},
	journal = {TOXICOLOGY AND APPLIED PHARMACOLOGY},
	volume = {429},
	unique-id = {32178981},
	issn = {0041-008X},
	abstract = {Organic anion-transporting polypeptide 2B1 (OATP2B1) is a multispecific transporter mediating the cellular uptake of steroids and numerous drugs. OATP2B1 is abundantly expressed in the intestine and is also present in various tumors. Increased steroid hormone uptake by OATP2B1 has been suggested to promote progression of hormone dependent tumors. 13 alpha-estrones are effective inhibitors of endogenous estrogen formation and are potential candidates to inhibit proliferation of hormone dependent cancers. Recently, we have identified a variety of 13 alpha/beta-estrone-based inhibitors of OATP2B1. However, the nature of this interaction, whether these inhibitors are potential transported substrates of OATP2B1 and hence may be enriched in OATP2B1overexpressing cells, has not yet been investigated. In the current study we explored the antiproliferative effect of the most effective OATP2B1 inhibitor 13 alpha/beta-estrones in control and OATP2B1-overexpressing A431 carcinoma cells. We found an increased antiproliferative effect of 3-O-benzyl 13 alpha/beta-estrones in both mock transfected and OATP2B1-overexpressing cells. However, C-2 halogenated 13 alpha-estrones had a selective OATP2B1-mediated cell growth inhibitory effect. In order to demonstrate that increased sensitization can be attributed to OATP2B1-mediated cellular uptake, tritium labeled 2-bromo-13 alpha-estrone was synthesized for direct transport measurements. These experiments revealed increased accumulation of [H-3]2-bromo-13 alpha-estrone due to OATP2B1 function. Our results indicate that C-2 halogenated 13 alpha-estrones are good candidates in the design of anti-cancer drugs targeting OATP2B1.},
	year = {2021},
	eissn = {1096-0333},
	orcid-numbers = {Mernyák, Erzsébet/0000-0003-4494-1817}
}

@article{MTMT:32128211,
	title = {Effects of aging on proteasomal-ubiquitin system, oxidative stress balance and calcium homeostasis in middle-aged female rat colon},
	url = {https://m2.mtmt.hu/api/publication/32128211},
	author = {Almási, Nikoletta and Murlasits, Zsolt and Al-Awar, Amin and Csonka, Ákos and Dvorácskó, Szabolcs and Tömböly, Csaba and Török, Szilvia and Bester, D. and Pósa, Anikó and Varga, Csaba and Kupai, Krisztina},
	doi = {10.1556/2060.2021.00012},
	journal-iso = {PHYSIOL INT},
	journal = {PHYSIOLOGY INTERNATIONAL},
	volume = {108},
	unique-id = {32128211},
	issn = {2498-602X},
	year = {2021},
	eissn = {2677-0164},
	pages = {27-42},
	orcid-numbers = {Almási, Nikoletta/0000-0002-7371-5272; Murlasits, Zsolt/0000-0003-4101-3417; Pósa, Anikó/0000-0003-2167-2888; Varga, Csaba/0000-0002-2678-665X; Kupai, Krisztina/0000-0002-0644-1718}
}

@article{MTMT:32123857,
	title = {Novel High Affinity Sigma-1 Receptor Ligands from Minimal Ensemble Docking-Based Virtual Screening},
	url = {https://m2.mtmt.hu/api/publication/32123857},
	author = {Dvorácskó, Szabolcs and Lázár, László and Fülöp, Ferenc and Palkó, Márta and Zalán, Zita and Penke, Botond and Fülöp, Lívia and Tömböly, Csaba and Bogár, Ferenc},
	doi = {10.3390/ijms22158112},
	journal-iso = {INT J MOL SCI},
	journal = {INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES},
	volume = {22},
	unique-id = {32123857},
	issn = {1661-6596},
	year = {2021},
	eissn = {1422-0067},
	orcid-numbers = {Lázár, László/0000-0002-2135-8496; Fülöp, Ferenc/0000-0003-1066-5287; Palkó, Márta/0000-0002-8265-7377; Zalán, Zita/0000-0002-7146-3024; Penke, Botond/0000-0003-0938-0567; Fülöp, Lívia/0000-0002-8010-0129; Bogár, Ferenc/0000-0002-0611-1452}
}

@article{MTMT:32053101,
	title = {Pro-Inflammatory Cytokines: Potential Links between the Endocannabinoid System and the Kynurenine Pathway in Depression},
	url = {https://m2.mtmt.hu/api/publication/32053101},
	author = {Zádor, Ferenc and Joca, Sâmia and Nagy-Grócz, Gábor and Dvorácskó, Szabolcs and Szűcs, Edina and Tömböly, Csaba and Benyhe, Sándor and Vécsei, László},
	doi = {10.3390/ijms22115903},
	journal-iso = {INT J MOL SCI},
	journal = {INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES},
	volume = {22},
	unique-id = {32053101},
	issn = {1661-6596},
	year = {2021},
	eissn = {1422-0067},
	orcid-numbers = {Joca, Sâmia/0000-0003-0255-5889; Nagy-Grócz, Gábor/0000-0003-2121-4625; Vécsei, László/0000-0001-8037-3672}
}

@article{MTMT:32040557,
	title = {N,N-Dimethyltryptamine attenuates spreading depolarization and restrains neurodegeneration by sigma-1 receptor activation in the ischemic rat brain},
	url = {https://m2.mtmt.hu/api/publication/32040557},
	author = {Szabó, Írisz and Varga, Viktória Éva and Dvorácskó, Szabolcs and Farkas, Elek Attila and Körmöczi, Tímea and Berkecz, Róbert and Kecskés, Szilvia and Menyhárt, Ákos and Frank, Rita and Hantosi, Dóra and Cozzi, Nicholas V. and Frecska, Ede and Tömböly, Csaba and Krizbai, István Adorján and Bari, Ferenc and Farkas, Eszter},
	doi = {10.1016/j.neuropharm.2021.108612},
	journal-iso = {NEUROPHARMACOLOGY},
	journal = {NEUROPHARMACOLOGY},
	volume = {192},
	unique-id = {32040557},
	issn = {0028-3908},
	year = {2021},
	eissn = {1873-7064},
	orcid-numbers = {Körmöczi, Tímea/0000-0002-0973-2473; Berkecz, Róbert/0000-0002-9076-2177; Menyhárt, Ákos/0000-0002-1355-3208; Farkas, Eszter/0000-0002-8478-9664}
}

@article{MTMT:31365295,
	title = {Steroidal ferrocenes as potential enzyme inhibitors of the estrogen biosynthesis},
	url = {https://m2.mtmt.hu/api/publication/31365295},
	author = {Herman, Bianka Edina and Gardi, János and Julesz, János and Tömböly, Csaba and Szánti-Pintér, Eszter and Fehér, Klaudia and Skodáné Földes, Rita and Szécsi, Mihály},
	doi = {10.1007/s42977-020-00023-7},
	journal-iso = {BIOL FUTURA},
	journal = {BIOLOGIA FUTURA},
	volume = {71},
	unique-id = {31365295},
	issn = {2676-8615},
	year = {2020},
	eissn = {2676-8607},
	pages = {249-264},
	orcid-numbers = {Szánti-Pintér, Eszter/0000-0001-8263-9884; Skodáné Földes, Rita/0000-0002-9810-1509; Szécsi, Mihály/0000-0002-4272-1362}
}