Wojciech Czestkowski, Łukasz Krzemiński, Michał C Piotrowicz, Marzena Mazur, Elżbieta Pluta, Gleb Andryianau, Robert Koralewski, Krzysztof Matyszewski, Sylwia Olejniczak, Michał Kowalski, Katarzyna Lisiecka, Rafał Kozieł, Katarzyna Piwowar, Diana Papiernik, Marcin Nowotny, Agnieszka Napiórkowska-Gromadzka, Elżbieta Nowak, Dorota Niedziałek, Grzegorz Wieczorek, Anna Siwińska, Tomasz Rejczak, Karol Jędrzejczak, Krzysztof Mulewski, Jacek Olczak, Zbigniew Zasłona, Adam Gołębiowski, Katarzyna Drzewicka, Agnieszka Bartoszewicz
Chitinase-3-like-1 (CHI3L1), also known as YKL-40, is a glycoprotein linked to inflammation, fibrosis, and cancer. This study explored CHI3L1's interactions with various oligosaccharides using microscale thermophoresis (MST) and AlphaScreen (AS). These investigations guided the development of high-throughput screening assays to assess interference of small molecules in binding between CHI3L1 and biotinylated small molecules or heparan sulfate-based probes. Small molecule binders of YKL-40 were identified in our chitotriosidase inhibitors library with MST and confirmed through X-ray crystallography...
March 1, 2024: Journal of Medicinal Chemistry