Journal: Molecular cancer therapeutics

Article Title: Characterization of a Dual Rac/Cdc42 Inhibitor MBQ-167 in Metastatic Cancer

doi: 10.1158/1535-7163.MCT-16-0442

Figure Lengend Snippet: Inhibitory effect of MBQ-167 on Rac and Cdc42 activation. MDA-MB-231 human breast cancer cells were treated for 24 h with 250 nM MBQ-167. A–C, The attached (A) and detached (D) cell populations were recovered and equal amounts of proteins subjected to pulldown assays using the p21-binding domain of PAK to isolate the GTP bound Rac and Cdc42. Cell lysates were western blotted with antibodies to Rac or Cdc42. Results from positive bands in western blots were quantified using image J. A, Left, Representative western blot for Rac1/2/; right, quantification of Rac activation at 24 h following 0 or 250nM MBQ-167. B, Left, Representative western blot for Cdc42; right, quantification of Cdc42 activation following 24 h treatment with 0 or 250 nM MBQ-167. The integrated density for active Rac or Cdc42 (GTP) was divided by the total Rac or Cdc42 from the same cell lysates. Rac or Cdc42 activity for each MBQ-167 treatment was divided by the vehicle controls for each experiment to obtain Relative Rac or Cdc42 activity. N=3, * = P < 0.05, *** = P < 0.001. Error bars represent ± S.E.M. C,D, MDA-MB-231 cells with vehicle control (0.1% DMSO) or varying concentrations of MBQ-167 (0–1000 nM) were treated for 24 hrs. Total cell lysates using combined attached and detached treated populations were subjected to the G-LISA Rac1/2/3 or Cdc42 activation assay. IC50 curves for percentage Rac (C) or Cdc42 (D) activation are relative to vehicle from three biological replicates each with two technical replicates. Error bars represent ± S.D. Four-parameter dose-response curves generated using GraphPad Prism® are shown.

Article Snippet: For the IC 50 curves Rac1/2/3 and Cdc42 activation was determined as described ( 16 ), using a G-LISA kit (Cytoskeleton, Inc., Denver, CO).

Techniques: Activation Assay, Binding Assay, Western Blot, Activity Assay, Control, Generated

Journal: ACS Omega

Article Title: A LRELHLNNN-Gal‑3 Modified Adipose Decellularized Scaffold To Construct Colorectal Cancer Model for Anticancer Drug Screening and Immunotherapy

doi: 10.1021/acsomega.5c07342

Figure Lengend Snippet: Evaluation of chemotherapy resistance in LoVo cells cultured in LRELHLNNN-Gal-3 modified adECM scaffolds. (A) Apoptosis results of LoVo cells seeded in 2D culture, LRELHLNNN-Gal-3 modified adECM scaffolds, and Gal-3 modified adECM scaffolds after treatment with 5-Fu for 12, 24, and 48 h. (B) Results for oxaliplatin treatment. (C) Results for capecitabine treatment. All samples were analyzed by CCK-8 assay. (D) Flow cytometry analysis of cell viability after 48 h treatment with 5-Fu (E), oxaliplatin (F), and capecitabine (G) in 2D culture, LRELHLNNN-Gal-3 modified adECM scaffolds, and Gal-3 modified adECM scaffolds. Data are presented as mean ± SD ( n = 3). Statistical significance: n.s. = not significant, * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001.

Article Snippet: The sensitivity of LoVo cells to chemotherapeutic drugs was assessed using 5-Fu (100 μM, MedChemExpress, HY-90006), oxaliplatin (20 μM, MedChemExpress, HY-17371), and capecitabine (1.7 mM, MedChemExpress, HY-B0016, Obtained from the IC50 curve of the drug, Figure S1 ) as model drugs under different culture conditions.

Techniques: Cell Culture, Modification, CCK-8 Assay, Flow Cytometry

Journal: Frontiers in Pharmacology

Article Title: Identification of oral therapeutics using an AI platform against the virus responsible for COVID-19, SARS-CoV-2

doi: 10.3389/fphar.2023.1297924

Figure Lengend Snippet: This table presents the prioritized list of drug therapies as determined by aggregate AI evaluations across multiple models. The “Score” column represents the comprehensive AI-derived rating, “SNet” denotes a weighted mean derived from the scores of the Siamese networks, and “Corona MLP” pertains to the ratings generated by the MLP model specifically trained for coronaviruses. Chemical structures of these compounds can be found at https://www.chemspider.com/ .

Article Snippet: Mebendazole, gefitinib, topotecan, and, to a lesser extent, carfilzomib showed conventional drug-response curves, with IC50 values near or below that of remdesivir with excellent confidence that were all above R2 > 0.91 with no cytotoxicity at the IC50 concentration ( ).

Techniques: Derivative Assay, Generated