Design, Synthesis and Biological Evaluation of Ketoprofen Conjugated To RGD/NGR for Targeted Cancer Therapy

Synthesis and biological evaluation of RGD-conjugated MEK1/2 kinase inhibitors for integrin-targeted cancer therapy.

Two novel series of RGD-MEKI conjugates derived from a MEK1/2 kinase inhibitor--PD0325901--have been developed for integrin receptor mediated anticancer therapy. The first series, alkoxylamine analog RGD-MEKI conjugates 9a-g showed anti-proliferation activity in melanoma A375 cells by the same mechanism as that of PD0325901. PEGylation increased the IC50 value of 9f three-fold in the A375 assay...

synthesis of pegylated zinc protoporphyrin conjugated with folate: for targeted cancer therapy

Folate-Conjugated Gold Nanoparticles (Synthesis, Characterization and Design for Cancer Cells Nanotechnology-based Targeting)

A new folate-conjugated gold nanoparticle (AuNP) has been designed to selectively target the folate receptor that is overexpressed on the surface of tumoral cells. For this purpose, we made 4-aminothiophenol, as a bifunctional linker to react with HAuCl4 in the presence of sodium borohydride and it was binded to the AuNP surface through its thiol group. Then, we conjugated amino-terminated nano...

Production and Evaluation of Specific Single-Chain Antibodies against CTLA-4 for Cancer-Targeted Therapy

Background:  Cytotoxic T lymphocyte–associated antigen 4 (CTLA-4) molecules are expressed on T-cells and inhibit their function by inhibiting activation of subsequent T-cell molecular pathways. Blocking of CTLA-4 inhibits the growth of malignant tumor cells. Anti-CTLA-4 monoclonal antibodies activate the immune system against cancer. Due to several advantages of single-chain antibodi...

AS1411 Aptamer Conjugated Gold Nanoclusters as a Targeted Radiosensitizer for Megavoltage Radiation Therapy of 4T1 Breast Cancer Cells

Introduction: In the present study, AS1411 aptamer conjugated gold nanoclusters (GNCs) have been introduced as a targeted radiosensitizer for enhancing megavoltage radiation therapy efficacy. RT has identified as an effective therapeutic modality for many different types of solid tumors. However, equal radiation beams absorption by tumor and surrounding healthy tissues is still...