Quantitation and kinetics of CD51 surface receptor expression: implications for targeted delivery

The CD51 integrin subunit is important in many functions ranging from mediation of adenovirus attachment and internalization to facilitation of angiogenesis. CD51 has also gained interest as an attractive ligand for directed therapy studies, including those for targeted gene delivery. While the function and importance of several CD51-specific targeting molecules have been examined, studies are often carried out without quantitative assessment of the receptor. A lack of this data complicates further mathematical analysis of targeting data and elucidation of the mechanism(s) underlying specific targeting. We performed a quantitative evaluation of CD51 receptors on the surface of HeLa cells, a common cell line utilized in many receptor-based studies, and compared them to other similar and dissimilar cell types. Unstimulated HeLa cells strongly express the CD51 receptor at a level of 212,700 +/- 12,000 (mean +/- SD) antibody binding capacity (ABC) cell(-1) (n = 3). Following irradiation with 3 Gy, receptor expression increases dramatically, peaking at a value of 403,700 +/- 26,400 (n = 4). The utility of this quantitative information is highlighted by the application of our data to targeting studies from the literature. Taken together, the results yield more detailed information than is available with experimental targeting data alone.