Anticancer activity of drug conjugates in head and neck cancer cells.
We report the synthesis of water soluble nanosize conjugates of paclitaxel, branched PEG, and EGFR-targeting peptide by employing native chemical ligation. We performed a native chemical ligation between the N-hydroxy succinimide (NHS) ester of paclitaxel succinate and cysteine at pH 6.5 to give the cysteine-conjugated paclitaxel derivative. The thiol functionality of cysteine was activated and subsequently conjugated to multiarm thiol-PEG to obtain the paclitaxel branched PEG conjugate. Finally, we conjugated an EGFR-targeting peptide to obtain conjugates of paclitaxel, branched PEG, and EGFR-targeting peptide. These conjugates show anticancer activity against squamous cell carcinoma of head and neck cells (SCCHN, Tu212).
PMID: 27100344 [PubMed - in process]
Source: Frontiers in Bioscience - Elite - Category: Biomedical Science Tags: Front Biosci (Elite Ed) Source Type: research
More News: Biomedical Science | Breast Carcinoma | Cancer | Cancer & Oncology | Carcinoma | Cervical Cancer | Chemistry | Head and Neck Cancer | Human Papillomavirus (HPV) | Nanotechnology | Non-Small Cell Lung Cancer | Oral Cancer | Ovarian Cancer | Ovaries | Skin Cancer | Squamous Cell Carcinoma | STDs