One-bead one-compound combinatorial library derived targeting ligands for detection and treatment of oral squamous cancer


The cover for issue 52 of Oncotarget features Figure 6, "Confocal images of LLY13 peptide-dye conjugates taken up by live cells in culture," by Yang, et al.

By screening combinatorial one-bead one-compound peptide libraries against oral squamous cancer cell lines, two cyclic peptide ligands, LLY12 and LLY13 were previously identified.

In vivo and ex vivo near infra-red fluorescence imaging studies confirmed the in vivo targeting efficiency and specificity of LLY13 in oral cancer orthotopic murine xenograft model.

In vivo studies also showed that LLY13 was able to accumulate in the OSC tumors and demarcate the tumor margins in orthotopic xenograft model.

Together, the author's data supports LLY13 as a promising theranostic agent against OSC.

Figure 1: MTS assay evaluation of cytotoxicity of LLY12 and LLY13 on normal human keratinocytes (NHK).

Dr. Fan Yang from the Department of Oral Medicine, Infection and Immunity, at Harvard School of Dental Medicine, in Boston, MA, USA and Dr. Kit S. Lam from the Department of Biochemistry and Molecular Medicine, at the University of California, Davis, in CA, USA said "Despite the current aggressive treatment strategies with chemotherapy, radiation therapy and surgery, oral cancer remains the third most lethal cancer, accounting for 18% of all cancer deaths and a 5-year survival of less than 50%"

Histopathologically, oral squamous cancer is by far the most common cancer type of the oropharynx and oral cavity, representing more than 90% of all oral cancer.

Oral squamous cancer of the tongue is the most common subtype of cancer diagnosed in the oral cavity comprising 25‐40% of oral cancer.

X1 focused OBOC library is a cyclic peptide library with a motif which binds preferentially to ovarian cancer with high specificity against α3β1 integrin.

The Yang/Lam research team concluded, "These focused libraries can then be screened under higher stringency by lowering the bead surface substitution, shortening the incubation time or by adding soluble competing receptor specific antagonist against OSC, such that peptides with higher affinity and higher specificity against OSC might be identified."

Full text - https://www.oncotarget.com/article/27189/text/

Correspondence to - Fan Yang - [email protected] and Kit S. Lam - [email protected]

Keywords - oral squamous cancer, α3 integrin, optical imaging, cancer-targeting peptide, orthotopic xenograft model

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