Search Results - "Wrobel, Tomasz M."

Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment by Wróbel, Tomasz M., Jørgensen, Flemming Steen, Pandey, Amit V., Grudzińska, Angelika, Sharma, Katyayani, Yakubu, Jibira, Björkling, Fredrik

“…CYP17A1 is an enzyme that plays a major role in steroidogenesis and is critically involved in the biosynthesis of steroid hormones. Therefore, it remains an…”
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Experimental and Computational Structural Studies of 2,3,5-Trisubstituted and 1,2,3,5-Tetrasubstituted Indoles as Non-Competitive Antagonists of GluK1/GluK2 Receptors by Bartyzel, Agata, Kaczor, Agnieszka A, Mahmoudi, Ghodrat, Masoudiasl, Ardavan, Wróbel, Tomasz M, Pitucha, Monika, Matosiuk, Dariusz

“…The blockade of kainate receptors, in particular with non-competitive antagonists, has-due to their anticonvulsant and neuroprotective properties-therapeutic…”
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Synthesis, Structural and Behavioral Studies of Indole Derivatives D2AAK5, D2AAK6 and D2AAK7 as Serotonin 5-HT1A and 5-HT2A Receptor Ligands by Kaczor, Agnieszka A., Kędzierska, Ewa, Wróbel, Tomasz M., Grudzińska, Angelika, Pawlak, Angelika, Laitinen, Tuomo, Bartyzel, Agata

“…Serotonin receptors are involved in a number of physiological functions and regulate aggression, anxiety, appetite, cognition, learning, memory, mood, nausea,…”
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Bitopic Ligands Support the Presence of a Metastable Binding Site at the β2 Adrenergic Receptor by Gaiser, Birgit Isabel, Danielsen, Mia, Xu, Xinyu, Røpke Jørgensen, Kira, Fronik, Philipp, Märcher-Rørsted, Emil, Wróbel, Tomasz M., Liu, Xiangyu, Mosolff Mathiesen, Jesper, Sejer Pedersen, Daniel

“…Metastable binding sites (MBS) have been observed in a multitude of molecular dynamics simulations and can be considered low affinity allosteric binding sites…”
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Discovery and in vitro Evaluation of Novel Serotonin 5‐HT2A Receptor Ligands Identified Through Virtual Screening by Zięba, Agata, Bartuzi, Damian, Stępnicki, Piotr, Matosiuk, Dariusz, Wróbel, Tomasz M., Laitinen, Tuomo, Castro, Marián, Kaczor, Agnieszka A.

“…The 5‐HT2A receptor is a molecular target of high pharmacological importance. Ligands of this protein, particularly atypical antipsychotics, are useful in the…”
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Development and Characterization of Novel Selective, Non-Basic Dopamine D2 Receptor Antagonists for the Treatment of Schizophrenia by Stępnicki, Piotr, Wośko, Sylwia, Bartyzel, Agata, Zięba, Agata, Bartuzi, Damian, Szałaj, Klaudia, Wróbel, Tomasz M., Fornal, Emilia, Carlsson, Jens, Kędzierska, Ewa, Poleszak, Ewa, Castro, Marián, Kaczor, Agnieszka A.

“…The dopamine D2 receptor, which belongs to the family of G protein-coupled receptors (GPCR), is an important and well-validated drug target in the field of…”
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Thermal and spectroscopic studies of 2,3,5-trisubstituted and 1,2,3,5-tetrasubstituted indoles as non-competitive antagonists of GluK1/GluK2 receptors by Bartyzel, Agata, Kaczor, Agnieszka A., Głuchowska, Halina, Pitucha, Monika, Wróbel, Tomasz M., Matosiuk, Dariusz

“…This paper reports the thermal stability and thermal degradation of six derivatives of indole by means of TG-DSC (in air) and TG-FTIR (in nitrogen) techniques…”
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Funnel metadynamics and behavioral studies reveal complex effect of D2AAK1 ligand on anxiety-like processes by Bartuzi, Damian, Kędzierska, Ewa, Targowska-Duda, Katarzyna M., Koszła, Oliwia, Wróbel, Tomasz M., Jademyr, Simon, Karcz, Tadeusz, Szczepańska, Katarzyna, Stępnicki, Piotr, Wronikowska-Denysiuk, Olga, Biała, Grażyna, Handzlik, Jadwiga, Kristensen, Jesper L., Poso, Antti, Kaczor, Agnieszka A.

“…Anxiety is a troublesome symptom for many patients, especially those suffering from schizophrenia. Its regulation involves serotonin receptors, targeted e.g…”
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Novel multi-target ligands of dopamine and serotonin receptors for the treatment of schizophrenia based on indazole and piperazine scaffolds-synthesis, biological activity, and structural evaluation by Stępnicki, Piotr, Wronikowska-Denysiuk, Olga, Zięba, Agata, Targowska-Duda, Katarzyna M., Bartyzel, Agata, Wróbel, Martyna Z., Wróbel, Tomasz M., Szałaj, Klaudia, Chodkowski, Andrzej, Mirecka, Karolina, Budzyńska, Barbara, Fornal, Emilia, Turło, Jadwiga, Castro, Marián, Kaczor, Agnieszka A.

“…Schizophrenia is a chronic mental disorder that is not satisfactorily treated with available antipsychotics. The presented study focuses on the search for new…”
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Thermal behavior and determination of physicochemical properties of novel candidates for antipsychotic drugs by Stępnicki, Piotr, Gwarda, Radosław Ł., Bartyzel, Agata, Karcz, Tadeusz, Szczepańska, Katarzyna, Wróbel, Tomasz M., Kaczor, Agnieszka A.

“…Treatment of schizophrenia with currently available drugs is often ineffective or results in several adverse reactions. In previous studies focusing on the…”
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Synthesis, pharmacological and structural studies of 5-substituted-3-(1-arylmethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as multi-target ligands of aminergic GPCRs by Kondej, Magda, Wróbel, Tomasz M., Silva, Andrea G., Stępnicki, Piotr, Koszła, Oliwia, Kędzierska, Ewa, Bartyzel, Agata, Biała, Grażyna, Matosiuk, Dariusz, Loza, Maria I., Castro, Marián, Kaczor, Agnieszka A.

“…Schizophrenia is a complex disease with not fully understood pathomechanism, involving many neurotransmitters and their receptors. This is why it is best…”
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Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents by Wróbel, Tomasz M, Rogova, Oksana, Andersen, Kasper L, Yadav, Rahul, Brixius-Anderko, Simone, Scott, Emily E, Olsen, Lars, Jørgensen, Flemming Steen, Björkling, Fredrik

“…The current study presents the design, synthesis, and evaluation of novel cytochrome P450 17A1 (CYP17A1) ligands. CYP17A1 is a key enzyme in the steroidogenic…”
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Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents – Design, synthesis, structural studies and pharmacological profiling by Stępnicki, Piotr, Targowska-Duda, Katarzyna M., Martínez, Antón L., Zięba, Agata, Wronikowska-Denysiuk, Olga, Wróbel, Martyna Z., Bartyzel, Agata, Trzpil, Alicja, Wróbel, Tomasz M., Chodkowski, Andrzej, Mirecka, Karolina, Karcz, Tadeusz, Szczepańska, Katarzyna, Loza, Maria I., Budzyńska, Barbara, Turło, Jadwiga, Handzlik, Jadwiga, Fornal, Emilia, Poleszak, Ewa, Castro, Marián, Kaczor, Agnieszka A.

“…Schizophrenia is a mental disorder with a complex pathomechanism involving many neurotransmitter systems. Among the currently used antipsychotics, classical…”
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The Antipsychotic D2AAK1 as a Memory Enhancer for Treatment of Mental and Neurodegenerative Diseases by Koszła, Oliwia, Sołek, Przemysław, Woźniak, Sylwia, Kędzierska, Ewa, Wróbel, Tomasz M, Kondej, Magda, Archała, Aneta, Stępnicki, Piotr, Biała, Grażyna, Matosiuk, Dariusz, Kaczor, Agnieszka A

“…The treatment of memory impairments associated with the central nervous system diseases remains an unmet medical need with social and economic implications…”
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WaterMap‐Guided Structure‐Based Virtual Screening for Acetylcholinesterase Inhibitors by Targowska‐Duda, Katarzyna M., Maj, Maciej, Drączkowski, Piotr, Budzyńska, Barbara, Boguszewska‐Czubara, Anna, Wróbel, Tomasz M., Laitinen, Tuomo, Kaczmar, Patrycja, Poso, Antti, Kaczor, Agnieszka A.

“…Structure‐based virtual screening of the Enamine database of 1.7 million compounds followed by WaterMap calculations (a molecular‐dynamics‐simulation‐based…”
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Multitarget Derivatives of D2AAK1 as Potential Antipsychotics: The Effect of Substitution in the Indole Moiety by Kondej, Magda, Wróbel, Tomasz M., Targowska‐Duda, Katarzyna M., Leandro Martínez, Antón, Koszła, Oliwia, Stępnicki, Piotr, Zięba, Agata, Paz, Alba, Wronikowska‐Denysiuk, Olga, Loza, Maria I., Castro, Marián, Kaczor, Agnieszka A.

“…Schizophrenia is a complex disease which is best treated with multitarget drugs, such as atypical antipsychotics. Previously, using structure‐based virtual…”
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A comprehensive assessment of palmatine as anticonvulsant agent – In vivo and in silico studies by Nieoczym, Dorota, Marszalek-Grabska, Marta, Szalak, Radoslaw, Kundap, Uday, Kaczor, Agnieszka A., Wrobel, Tomasz M., Kosheva, Nataliia, Komar, Malgorzata, Abram, Michal, Esguerra, Camila V., Samarut, Eric, Pieróg, Mateusz, Jakubiec, Marcin, Kaminski, Krzysztof, Kukula-Koch, Wirginia, Gawel, Kinga

“…Previously, we demonstrated that palmatine (PALM) – an isoquinoline alkaloid from Berberis sibrica radix, exerted antiseizure activity in the…”
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Synthesis, Structural Studies and Molecular Modelling of a Novel Imidazoline Derivative with Antifungal Activity by Wróbel, Tomasz M, Kosikowska, Urszula, Kaczor, Agnieszka A, Andrzejczuk, Sylwia, Karczmarzyk, Zbigniew, Wysocki, Waldemar, Urbańczyk-Lipkowska, Zofia, Morawiak, Maja, Matosiuk, Dariusz

“…Six novel imidazoline derivatives were synthesized and tested in antifungal assays. One of the compounds,…”
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Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis by Wróbel, Tomasz M, Sharma, Katyayani, Mannella, Iole, Oliaro-Bosso, Simonetta, Nieckarz, Patrycja, Du Toit, Therina, Voegel, Clarissa Daniela, Rojas Velazquez, Maria Natalia, Yakubu, Jibira, Matveeva, Anna, Therkelsen, Søren, Jørgensen, Flemming Steen, Pandey, Amit V, Pippione, Agnese C, Lolli, Marco L, Boschi, Donatella, Björkling, Fredrik

“…This study reports on the synthesis and evaluation of novel compounds replacing the nitrogen-containing heterocyclic ring on the chemical backbone structure of…”
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Synthesis and Structure-Activity Relationships of Novel Non-Steroidal CYP17A1 Inhibitors as Potential Prostate Cancer Agents by Wróbel, Tomasz M, Rogova, Oksana, Sharma, Katyayani, Rojas Velazquez, Maria Natalia, Pandey, Amit V, Jørgensen, Flemming Steen, Arendrup, Frederic S, Andersen, Kasper L, Björkling, Fredrik

“…Twenty new compounds, targeting CYP17A1, were synthesized, based on our previous work on a benzimidazole scaffold, and their biological activity evaluated…”
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