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NMR fragment-based screening for development of the CD44-binding small molecules.
Bioorg. Chem. 82, 284-289 (2019)
The cell-surface protein CD44, a primary receptor for hyaluronic acid (HA), is one of the most promising targets for cancer therapies. It is prominently involved in the process of tumor growth and metastasis. The possibility of modulating the CD44-HA interaction with a pharmacological inhibitor is therefore of great importance, yet until now there are only few small molecules reported to bind to CD44. Here, we describe the results of the NMR fragment-based screening conducted against CD44 by which we found eight new hit compounds that bind to the receptor with the affinity in milimolar range. The NMR-based characterization revealed that there are two possible binding modes for these compounds, and for some of them the binding is no longer possible in the presence of hyaluronic acid. This could provide an interesting starting point for the development of new high-affinity ligands targeting the CD44-HA axis.
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Publication type
Article: Journal article
Document type
Scientific Article
Keywords
Cd44 ; Hyaluronic Acid ; Small-molecular Inhibitors ; Fragment-based Screening; Cell-surface Receptor; Chemical-shift Perturbation; Bivatuzumab Mertansine; Colorectal-cancer; Cd44 Expression; Binding Domain; Breast-cancer; Adhesion; Carcinoma; Antibody
Language
english
Publication Year
2019
Prepublished in Year
2018
HGF-reported in Year
2018
ISSN (print) / ISBN
0045-2068
e-ISSN
1090-2120
Journal
Bioorganic chemistry
Quellenangaben
Volume: 82,
Pages: 284-289
Publisher
Elsevier
Publishing Place
San Diego, Calif.
Reviewing status
Peer reviewed
Institute(s)
Institute of Structural Biology (STB)
POF-Topic(s)
30203 - Molecular Targets and Therapies
Research field(s)
Enabling and Novel Technologies
PSP Element(s)
G-503000-001
WOS ID
WOS:000455479600031
Scopus ID
85055903678
PubMed ID
30396062
Erfassungsdatum
2018-11-07