IMR Press / FBE / Volume 8 / Issue 3 / DOI: 10.2741/E772

Frontiers in Bioscience-Elite (FBE) is published by IMR Press from Volume 13 Issue 2 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Article

Anticancer activity of drug conjugates in head and neck cancer cells

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1 Department of Hematology and Medical Oncology, Winship Cancer Institute, Emory University School of Medicine, Emory University, 1365 C Clifton Road, Atlanta, GA 30322
2 Glycosyn LLC, Medford, MA 02155

*Author to whom correspondence should be addressed.

Academic Editor: Indrajit Chowdhury

Front. Biosci. (Elite Ed) 2016, 8(3), 358–369; https://doi.org/10.2741/E772
Published: 1 June 2016
(This article belongs to the Special Issue Recent progress in reproductive biology)
Abstract

Sexually transmitted oral cancer/head and neck cancer is increasing rapidly. Human papilloma virus (HPV) is playing a role in the pathogenesis of a subset of squamous cell carcinoma of head and neck (SCCHN). Paclitaxel is a widely used anticancer drug for breast, ovarian, testicular, cervical, non-small cell lung, head and neck cancer. However, it is water insoluble and orally inactive. 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).

Keywords
Cancer
Head
Neck
Cancer
Squamous Cell Carcinoma
SCCHN
Paclitaxel
Human Papillomavirus
Oropharynx
Epidermal Growth Factor Receptor
EGFR
Polyethylene Glycol Ether
PEG
Native Chemical Ligation
Peptide
Ligand
Antibody
Cancer Therapy
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