Kamdem, Nestor published the artcileSmall-molecule inhibitors of the PDZ domain of Dishevelled proteins interrupt Wnt signalling, Computed Properties of 61551-49-3, the publication is Magnetic Resonance (2021), 2(1), 355-374, database is CAplus.
Dishevelled (Dvl) proteins are important regulators of the Wnt signalling pathway, interacting through their PDZ domains with the Wnt receptor Frizzled. Blocking the Dvl PDZ-Frizzled interaction represents a potential approach for cancer treatment, which stimulated the identification of small-mol. inhibitors, among them the anti-inflammatory drug Sulindac and Ky-02327. Aiming to develop tighter binding compounds without side effects, we investigated structure-activity relationships of sulfonamides. X-ray crystallog. showed high complementarity of anthranilic acid derivatives in the GLGF loop cavity and space for ligand growth toward the PDZ surface. Our best binding compound inhibits Wnt signalling in a dose-dependent manner as demonstrated by TOP-GFP assays (IC50 ∼ 50 μM) and Western blotting of β-catenin levels. Realtime PCR showed reduction in the expression of Wnt-specific genes. Our compound interacted with Dvl-1 PDZ (KD = 2.4 μM) stronger than Ky-02327 and may be developed into a lead compound interfering with the Wnt pathway.
Magnetic Resonance published new progress about 61551-49-3. 61551-49-3 belongs to chlorides-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 5,6,7,8-Tetrahydronaphthalene-2-sulfonyl chloride, and the molecular formula is C10H11ClO2S, Computed Properties of 61551-49-3.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics