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Your search keyword '"Zagozdzon, Agnieszka"' showing total 4 results
Start Over Author "Zagozdzon, Agnieszka" Journal journal of medicinal chemistry
4 results on '"Zagozdzon, Agnieszka"'

1. Discovery of OATD-01, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis

Author

Koralewski, Robert, primary, Dymek, Barbara, additional, Mazur, Marzena, additional, Sklepkiewicz, Piotr, additional, Olejniczak, Sylwia, additional, Czestkowski, Wojciech, additional, Matyszewski, Krzysztof, additional, Andryianau, Gleb, additional, Niedziejko, Piotr, additional, Kowalski, Michal, additional, Gruza, Mariusz, additional, Borek, Bartłomiej, additional, Jedrzejczak, Karol, additional, Bartoszewicz, Agnieszka, additional, Pluta, Elżbieta, additional, Rymaszewska, Aleksandra, additional, Kania, Magdalena, additional, Rejczak, Tomasz, additional, Piasecka, Sylwia, additional, Mlacki, Michal, additional, Mazurkiewicz, Marcin, additional, Piotrowicz, Michał, additional, Salamon, Magdalena, additional, Zagozdzon, Agnieszka, additional, Napiorkowska-Gromadzka, Agnieszka, additional, Bartlomiejczak, Aneta, additional, Mozga, Witold, additional, Dobrzański, Paweł, additional, Dzwonek, Karolina, additional, Golab, Jakub, additional, Nowotny, Marcin, additional, Olczak, Jacek, additional, and Golebiowski, Adam, additional

Published
2020
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2. Development of Dual Chitinase Inhibitors as Potential New Treatment for Respiratory System Diseases

Author

Mazur, Marzena, primary, Dymek, Barbara, additional, Koralewski, Robert, additional, Sklepkiewicz, Piotr, additional, Olejniczak, Sylwia, additional, Mazurkiewicz, Marcin, additional, Piotrowicz, Michał, additional, Salamon, Magdalena, additional, Jędrzejczak, Karol, additional, Zagozdzon, Agnieszka, additional, Czestkowski, Wojciech, additional, Matyszewski, Krzysztof, additional, Borek, Bartłomiej, additional, Bartoszewicz, Agnieszka, additional, Pluta, Elżbieta, additional, Rymaszewska, Aleksandra, additional, Mozga, Witold, additional, Stefaniak, Filip, additional, Dobrzański, Paweł, additional, Dzwonek, Karolina, additional, Golab, Jakub, additional, Golebiowski, Adam, additional, and Olczak, Jacek, additional

Published
2019
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3. Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma

Author

Mazur, Marzena, primary, Olczak, Jacek, additional, Olejniczak, Sylwia, additional, Koralewski, Robert, additional, Czestkowski, Wojciech, additional, Jedrzejczak, Anna, additional, Golab, Jakub, additional, Dzwonek, Karolina, additional, Dymek, Barbara, additional, Sklepkiewicz, Piotr L., additional, Zagozdzon, Agnieszka, additional, Noonan, Tom, additional, Mahboubi, Keyvan, additional, Conway, Bruce, additional, Sheeler, Ryan, additional, Beckett, Paul, additional, Hungerford, William M., additional, Podjarny, Alberto, additional, Mitschler, Andre, additional, Cousido-Siah, Alexandra, additional, Fadel, Firas, additional, and Golebiowski, Adam, additional

Published
2018
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4. Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma

Author

Mazur, Marzena, Olczak, Jacek, Olejniczak, Sylwia, Koralewski, Robert, Czestkowski, Wojciech, Jedrzejczak, Anna, Golab, Jakub, Dzwonek, Karolina, Dymek, Barbara, Sklepkiewicz, Piotr L., Zagozdzon, Agnieszka, Noonan, Tom, Mahboubi, Keyvan, Conway, Bruce, Sheeler, Ryan, Beckett, Paul, Hungerford, William M., Podjarny, Alberto, Mitschler, Andre, Cousido-Siah, Alexandra, Fadel, Firas, and Golebiowski, Adam

Abstract

This article highlights our work toward the identification of a potent, selective, and efficacious acidic mammalian chitinase (AMCase) inhibitor. Rational design, guided by X-ray analysis of several inhibitors bound to human chitotriosidase (hCHIT1), led to the identification of compound 7fas a highly potent AMCase inhibitor (IC50values of 14 and 19 nM against human and mouse enzyme, respectively) and selective (>150× against mCHIT1) with very good PK properties. This compound dosed once daily at 30 mg/kg po showed significant anti-inflammatory efficacy in HDM-induced allergic airway inflammation in mice, reducing inflammatory cell influx in the BALF and total IgE concentration in plasma, which correlated with decrease of chitinolytic activity. Therapeutic efficacy of compound 7fin the clinically relevant aeroallergen-induced acute asthma model in mice provides a rationale for developing AMCase inhibitor for the treatment of asthma.

Published
2024
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