Effects of the Integrin-Linked Kinase Inhibitor QLT0267 on Squamous Cell Carcinoma of the Head and Neck

Abstract

To study the expression of integrin-linked kinase (ILK) in human squamous cell carcinoma of the head and neck (SCCHN) tumor specimens and cell lines and the efficacy of the novel small molecule QLT0267. Design: Immunohistochemical analysis of 17 SCCHN tumor tissue specimens and 3 normal tongue tissue specimens for ILK expression and in vitro analysis of the effectiveness of QLT0267 on SCCHN cells. Setting: Academic medical center. Main Outcome Measures: Expression levels of ILK in SCCHN tumor specimens and cell lines and the efficacy of QLT0267 in inhibiting cell growth and inducing apoptosis in SCCHN cell lines. Results: Most SCCHN tumor specimens stained for ILK, whereas none of the 3 normal tongue tissue specimens stained for ILK. Integrin-linked kinase was expressed in all 6 SCCHN cell lines tested. In 4 pairs of normal and SCCHN tumor specimens, ILK expression and activity

Focal adhesion complex proteins in epidermis and squamous cell carcinoma

“…1B). 79 These data are highly suggestive that ILK plays a key role in tumor malignancy, and that targeting ILK's kinase activity may be an effective therapeutic strategy. Perhaps ILK kinase activity plays a more important role during tumorigenesis than normal skin homeostasis.…”

Integrins as therapeutic targets: lessons and opportunities

“…A number of small-molecule inhibitors of ILK have been tested in in vitro models of cancer and metastasis [174][175] .…”

ILK (integrin-linked kinase)

“…Targeting ILK with the small-molecule ILK inhibitor QLT0267 inhibits cell growth and induces apoptosis in SCCHN cell lines by reducing ILK activity and Akt phosphorylation (Younes et al, 2007).…”