tubulin polymerization assay kit  (Cytoskeleton Inc)

Journal: Archiv Der Pharmazie

Article Title: Design, Synthesis, and Selective Antiproliferative Activity of Indolizine Derivatives as Microtubule Destabilizers

doi: 10.1002/ardp.70161

Figure Lengend Snippet: Docking interactions of the compounds 7f , BPR0L075 , and colchicine in the colchicine binding site of tubulin (PDB ID: 4O2B ). (Panel A) Structure of compound 7f , BPR0L075 , and colchicine. (Panel B) Superimposition of compound 7f (in blue), colchicine (in green), and BPR0L075 (in red). (Panel C) Interactions of the molecule 7f (in blue) and colchicine (in green) within the Cys241 of the binding pocket. ( Panel D ) Hydrophobicity surface of docked compounds 7f (in blue, C‐2 position highlighted), and colchicine (in orange, amide highlighted).

Article Snippet: To evaluate the effect of the compounds on tubulin polymerization, the Tubulin Polymerization Assay Kit (Cytoskeleton Inc.) was used according to the manufacturer's instructions.

Techniques: Binding Assay

Journal: Archiv Der Pharmazie

Article Title: Design, Synthesis, and Selective Antiproliferative Activity of Indolizine Derivatives as Microtubule Destabilizers

doi: 10.1002/ardp.70161

Figure Lengend Snippet: Docking interactions of the compounds 7f , 8e , and 8h in the colchicine binding site of tubulin (PDB ID: 4O2B ). (Panel A) Structure of compounds 7f , 8e , and 8h . (Panel B) Superimposition of compounds 7f (in blue), 8e (in yellow), and 8h (in the dark orange). (Panel C) Hydrophobicity surface of docked compounds 7f (in blue), 8e (in yellow), and 8h (in the dark orange). (Panel D) Interactions of the molecule 8e (in yellow) within the Cys241 of the binding pocket, and also hydrophobic contacts with Leu248, Lys 254, and Asn101 Panel E) Interactions of the molecule 8h (in the dark orange) within the Cys241 of the binding pocket, and also hydrophobic contacts with Leu248, Lys254, Ala180, and Asn101.

Article Snippet: To evaluate the effect of the compounds on tubulin polymerization, the Tubulin Polymerization Assay Kit (Cytoskeleton Inc.) was used according to the manufacturer's instructions.

Techniques: Binding Assay

Journal: Archiv Der Pharmazie

Article Title: Design, Synthesis, and Selective Antiproliferative Activity of Indolizine Derivatives as Microtubule Destabilizers

doi: 10.1002/ardp.70161

Figure Lengend Snippet: Antiproliferative effects of compounds 7f , 8e , and 8h on BT‐20 breast cancer cells. (Panel A) Cell‐cycle distribution after treatment with compounds (2.5 µM for 24 h) and vehicle control, showing G1, S, and G2/M phases. Statistical analysis was performed using two‐way ANOVA followed by Tukey's posttest. The indicated statistical differences refer to comparisons within the same treatment (**** p < 0.001). (Panel B) Tubulin polymerization assay performed with compounds (5 µM), compared with control (without treatment) and paclitaxel. (Panel C) Western blot analysis of key proteins involved in cell‐cycle regulation (Cyclin D1, p21), apoptosis (Bcl‐2), proliferation (c‐MYC), and signaling (p‐AKT), as well as β‐Tubulin and GAPDH as primary antibody controls, following treatment with 7f , 8e , and 8h (2.5 µM for 24 h).

Article Snippet: To evaluate the effect of the compounds on tubulin polymerization, the Tubulin Polymerization Assay Kit (Cytoskeleton Inc.) was used according to the manufacturer's instructions.

Techniques: Control, Polymerization Assay, Western Blot