Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent

Authors: Szczepańska, Katarzyna, Pockes, Steffen, Podlewska, Sabina, Höring, Carina, Mika, Kamil, Latacz, Gniewomir, Bednarski, Marek, Siwek, Agata, Karcz, Tadeusz, Nagl, Martin, Bresinsky, Merlin, Mönnich, Denise, Seibel, Ulla, Kuder, Kamil J., Kotańska, Magdalena, Stark, Holger, Elz, Sigurd, Kieć-Kononowicz, Katarzyna

Source: In European Journal of Medicinal Chemistry 5 March 2021 213

Dual-targeting Approach on Histamine H3 and Sigma-1 Receptor Ligands as Promising Pharmacological Tools in the Treatment of CNS-linked Disorders

Authors: Szczepańska, Katarzyna, Kuder, Kamil J., Kieć-Kononowicz, Katarzyna

Source: Current medicinal chemistry. 28(15):2974-2995

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100123193894.0x000001&indx=1&recIds=ETOCvdc_100123193894.0x000001

Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands

Authors: Szczepańska, Katarzyna, Karcz, Tadeusz, Siwek, Agata, Kuder, Kamil J., Latacz, Gniewomir, Bednarski, Marek, Szafarz, Małgorzata, Hagenow, Stefanie, Lubelska, Annamaria, Olejarz-Maciej, Agnieszka, Sobolewski, Michał, Mika, Kamil, Kotańska, Magdalena, Stark, Holger, Kieć-Kononowicz, Katarzyna

Source: In Bioorganic Chemistry October 2019 91

KSK19 – Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice

Authors: Kotańska, Magdalena, Mika, Kamil, Reguła, Karolina, Szczepańska, Katarzyna, Szafarz, Małgorzata, Bednarski, Marek, Olejarz-Maciej, Agnieszka, Nowak, Katarzyna, Latacz, Gniewomir, Mogilski, Szczepan, Kuder, Kamil J., Kieć-Kononowicz, Katarzyna, Sapa, Jacek

Source: In Biochemical Pharmacology October 2019 168:193-203

Novel, Dual Target‐Directed Annelated Xanthine Derivatives Acting on Adenosine Receptors and Monoamine Oxidase B

Authors: Kuder, Kamil J., Załuski, Michał, Schabikowski, Jakub, Latacz, Gniewomir, Olejarz‐Maciej, Agnieszka, Jaśko, Piotr, Doroz‐Płonka, Agata, Brockmann, Andreas, Müller, Christa E., Kieć‐Kononowicz, Katarzyna

Source: ChemMedChem. 15(9):772-786

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100107081522.0x000001&indx=1&recIds=ETOCvdc_100107081522.0x000001

A Taxicab geometry quantification system to evaluate the performance of in silico methods: a case study on adenosine receptors ligands

Authors: Kuder, Kamil J., Michalik, Ilona, Kieć-Kononowicz, Katarzyna, Kolb, Peter

Source: Journal of computer-aided molecular design. 34(6):697-707

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100171378511.0x000001&indx=1&recIds=ETOCvdc_100171378511.0x000001

Perry Disease: Current Outlook and Advances in Drug Discovery Approach to Symptomatic Treatment.

Authors: Gajda, Zbigniew, Hawrylak, Magdalena, Handzlik, Jadwiga, Kuder, Kamil J.

Source: International Journal of Molecular Sciences; Oct2024, Vol. 25 Issue 19, p10652, 35p

Subject Terms: COMPUTER-assisted drug design, DRUG discovery, DNA-binding proteins, PHARMACEUTICAL chemistry, MONOAMINE oxidase

AR71, Histamine H 3 Receptor Ligand—In Vitro and In Vivo Evaluation (Anti-Inflammatory Activity, Metabolic Stability, Toxicity, and Analgesic Action).

Authors: Stasiak, Anna, Honkisz-Orzechowska, Ewelina, Gajda, Zbigniew, Wagner, Waldemar, Popiołek-Barczyk, Katarzyna, Kuder, Kamil J., Latacz, Gniewomir, Juszczak, Michał, Woźniak, Katarzyna, Karcz, Tadeusz, Szczepańska, Katarzyna, Jóźwiak-Bębenista, Marta, Kieć-Kononowicz, Katarzyna, Łażewska, Dorota

Source: International Journal of Molecular Sciences; Aug2024, Vol. 25 Issue 15, p8035, 30p

Subject Terms: MONONUCLEAR leukocytes, HISTAMINE receptors, CYTOTOXINS, MOLECULAR docking, LABORATORY animals, H2 receptor antagonists

Optimization and preclinical evaluation of novel histamine H3 receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives

Authors: Szczepańska, Katarzyna, Karcz, Tadeusz, Kotańska, Magdalena, Siwek, Agata, Kuder, Kamil J., Latacz, Gniewomir, Mogilski, Szczepan, Hagenow, Stefanie, Lubelska, Annamaria, Sobolewski, Michał, Stark, Holger, Kieć-Kononowicz, Katarzyna

Source: In Bioorganic & Medicinal Chemistry 15 December 2018 26(23-24):6056-6066

Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands

Authors: Szczepańska, Katarzyna, Karcz, Tadeusz, Mogilski, Szczepan, Siwek, Agata, Kuder, Kamil J., Latacz, Gniewomir, Kubacka, Monika, Hagenow, Stefanie, Lubelska, Annamaria, Olejarz, Agnieszka, Kotańska, Magdalena, Sadek, Bassem, Stark, Holger, Kieć-Kononowicz, Katarzyna

Source: In European Journal of Medicinal Chemistry 25 May 2018 152:223-234

Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine H3R ligands

Authors: Kuder, Kamil J., Łażewska, Dorota, Kaleta, Maria, Latacz, Gniewomir, Kottke, Tim, Olejarz, Agnieszka, Karcz, Tadeusz, Fruziński, Andrzej, Szczepańska, Katarzyna, Karolak-Wojciechowska, Janina, Stark, Holger, Kieć-Kononowicz, Katarzyna

Source: In Bioorganic & Medicinal Chemistry 15 May 2017 25(10):2701-2712

Structure Prediction, Evaluation, and Validation of GPR18 Lipid Receptor Using Free Programs.

Authors: Michalik, Ilona¹ (AUTHOR), Kuder, Kamil J.¹ (AUTHOR) kamil.kuder@uj.edu.pl, Kieć-Kononowicz, Katarzyna¹ (AUTHOR) ilona.michalik@vp.pl, Handzlik, Jadwiga¹ (AUTHOR)

Source: International Journal of Molecular Sciences. Jul2022, Vol. 23 Issue 14, p7917-7917. 25p.

Subject Terms: *PROTEIN structure prediction, *MOLECULAR dynamics, *MOLECULAR docking, *PROTEIN structure, *COMPUTER-assisted drug design

Optimization and preclinical evaluation of novel histamine H3receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives

Authors: Szczepańska, Katarzyna, Karcz, Tadeusz, Kotańska, Magdalena, Siwek, Agata, Kuder, Kamil J., Latacz, Gniewomir, Mogilski, Szczepan, Hagenow, Stefanie, Lubelska, Annamaria, Sobolewski, Michał, Stark, Holger, Kieć-Kononowicz, Katarzyna

Source: Bioorganic & medicinal chemistry. 26(23-24):6056-6066

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100072276382.0x000001&indx=1&recIds=ETOCvdc_100072276382.0x000001

The histamine H3 receptor inverse agonist pitolisant reduces body weight in obese mice

Authors: Kotańska, Magdalena, Kuder, Kamil J., Szczepańska, Katarzyna, Sapa, Jacek, Kieć-Kononowicz, Katarzyna

Source: Naunyn-Schmiedeberg's archives of pharmacology. 391(8):875-881

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100125606455.0x000001&indx=1&recIds=ETOCvdc_100125606455.0x000001

N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H3 receptor and cancer resistance proteins

Authors: Szczepańska, Katarzyna, Kincses, Annamária, Vincze, Klaudia, Szymańska, Ewa, Latacz, Gniewomir, Kuder, Kamil J., Stark, Holger, Spengler, Gabriella, Handzlik, Jadwiga, Kieć-Kononowicz, Katarzyna

Source: Bioorganic & medicinal chemistry letters. 30(22)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100111457915.0x000001&indx=1&recIds=ETOCvdc_100111457915.0x000001

Metabolic and cardiovascular benefits and risks of 4-hydroxy guanabenz hydrochloride: α2-adrenoceptor and trace amine-associated receptor 1 ligand.

Authors: Kotańska, Magdalena, Marcinkowska, Monika, Kuder, Kamil J., Walczak, Maria, Bednarski, Marek, Siwek, Agata, Kołaczkowski, Marcin

Source: Pharmacological Reports; Oct2023, Vol. 75 Issue 5, p1211-1229, 19p

Anti-Inflammatory Activities of 8-Benzylaminoxanthines Showing High Adenosine A 2A and Dual A 1 /A 2A Receptor Affinity.

Authors: Załuski, Michał, Łażewska, Dorota, Jaśko, Piotr, Honkisz-Orzechowska, Ewelina, Kuder, Kamil J., Brockmann, Andreas, Latacz, Gniewomir, Zygmunt, Małgorzata, Kaleta, Maria, Greser, Beril Anita, Olejarz-Maciej, Agnieszka, Jastrzębska-Więsek, Magdalena, Vielmuth, Christin, Müller, Christa E., Kieć-Kononowicz, Katarzyna

Source: International Journal of Molecular Sciences; Sep2023, Vol. 24 Issue 18, p13707, 30p

Subject Terms: ADENOSINE derivatives, ADENOSINES, ANTI-inflammatory agents, PARKINSON'S disease, MOLECULAR dynamics, XANTHINE, NEURODEGENERATION

The Potent and Selective Histamine H3 Receptor Antagonist E169 Counteracts Cognitive Deficits and Mitigates Disturbances in the PI3K/AKT/GSK-3β Signaling Pathway in MK801-Induced Amnesia in Mice.

Authors: Abdalla, Sabna, Eissa, Nermin, Jayaprakash, Petrilla, Beiram, Rami, Kuder, Kamil J., Łażewska, Dorota, Kieć-Kononowicz, Katarzyna, Sadek, Bassem

Source: International Journal of Molecular Sciences; Aug2023, Vol. 24 Issue 16, p12719, 17p

Subject Terms: HISTAMINE receptors, ANTIHISTAMINES, CELLULAR signal transduction, AMNESIA, ALZHEIMER'S disease, PHOSPHATIDYLINOSITOL 3-kinases

Metabolic and cardiovascular benefits and risks of 4-hydroxy guanabenz hydrochloride: α2-adrenoceptor and trace amine-associated receptor 1 ligand

Authors: Kotańska, Magdalena, Marcinkowska, Monika, Kuder, Kamil J., Walczak, Maria, Bednarski, Marek, Siwek, Agata, Kołaczkowski, Marcin

Source: Pharmacological Reports; October 2023, Vol. 75 Issue: 5 p1211-1229, 19p

Benzophenone Derivatives with Histamine H 3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer's Disease.

Authors: Godyń, Justyna, Zaręba, Paula, Stary, Dorota, Kaleta, Maria, Kuder, Kamil J., Latacz, Gniewomir, Mogilski, Szczepan, Reiner-Link, David, Frank, Annika, Doroz-Płonka, Agata, Olejarz-Maciej, Agnieszka, Sudoł-Tałaj, Sylwia, Nolte, Tobias, Handzlik, Jadwiga, Stark, Holger, Więckowska, Anna, Malawska, Barbara, Kieć-Kononowicz, Katarzyna, Łażewska, Dorota, Bajda, Marek

Source: Molecules; Jan2023, Vol. 28 Issue 1, p238, 33p

Subject Terms: HISTAMINE receptors, ALZHEIMER'S disease, TACRINE, LIGANDS (Biochemistry), HISTAMINE, LIVER microsomes, PERMEABILITY