Jarosław Ciekot

Poland

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Articles (11)

Despite many years of research, human neutrophil elastase (HNE) still remains an area of interest for many researchers. This multifunctional representative of neutrophil serine proteases is one of the most destructive enzymes found in the human body which can degrade most of the extracellular matrix. Overexpression or dysregulation of HNE may lead to the development of several inflammatory diseases. Previously, we presented the HNE inhibitor with kinact/KI value over 2,000,000 [M−1s−1]. In order to optimize its structure, over 100 novel tripeptidyl derivatives of α-aminoalkylphosphonate diaryl esters were synthesized, and their activity toward HNE was checked. To confirm the selectivity of the resultant compounds, several of the most active were additionally checked against the two other neutrophil proteases: proteinase 3 and cathepsin G. The developed modifications allowed us to obtain a compound with significantly increased inhibitory activity against human neutrophil elastase with high selectivity toward cathepsin G, but none toward proteinase 3.

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2024

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2024

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2024

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2023

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2023

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2022

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2022

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2021

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2021

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2020

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2020

Collaborators (21)

Joanna Majewska

Research and Teaching Assistant

University of Wrocław

POLAND

Jarosław Ciekot

Research Interests

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Articles (11)

Targeted Library of Phosphonic-Type Inhibitors of Human Neutrophil Elastase

Discovery of a new bacterium, Microbacterium betulae sp. nov., in birch wood associated with hypersensitivity pneumonitis in woodworkers

Coelimycin inside out — negative feedback regulation by its intracellular precursors

Glycoalkaloid Composition and Flavonoid Content as Driving Forces of Phytotoxicity in Diploid Potato

Polysaccharide BAP1 of Bifidobacterium adolescentis CCDM 368 is a biologically active molecule with immunomodulatory properties

φYeO3-12 phage tail fiber Gp17 as a promising high specific tool for recognition of Yersinia enterocolitica pathogenic serotype O:3

Correction to: Transcriptional and proteomic insights into phytotoxic activity of interspecific potato hybrids with low glycoalkaloid contents

Immune Response to Therapeutic Staphylococcal Bacteriophages in Mammals: Kinetics of Induction, Immunogenic Structural Proteins, Natural and Induced Antibodies

Transcriptional and proteomic insights into phytotoxic activity of interspecific potato hybrids with low glycoalkaloid contents

Hydroxyethylcellulose as a methotrexate carrier in anticancer therapy

Structure-based design, synthesis, and evaluation of the biological activity of novel phosphoroorganic small molecule IAP antagonists

Collaborators (21)

Joanna Majewska

Lukasz Winiarski

Martin Schwarzer

Marcin Sieńczyk

Paweł Kędzierski

Dorota Soltys-Kalina

Karolina Filik-Matyjaszczyk

Paulina Smyda-Dajmund

Jacek Wojaczyński

Krystyna Dąbrowska

Janusz Boratynski

Paulina Miernikiewicz

Agnieszka Razim

Bożena Szermer-Olearnik

Krzysztof Pawlik

Mariola Paściak, Pasciak

Marek Harhala

Katarzyna Pacyga-Prus

Marek Drab

Katarzyna Leszczyńska

Waldemar Marczewski

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