RGD-conjugated two-photon absorbing near-IR emitting fluorescent probes for tumor vasculature imaging

Xiling Yue, Alma R. Morales, Grace W. Githaiga, Adam W. Woodward, Simon Tang, Junko Sawada, Masanobu Komatsu, Xuan Liu, Kevin D. Belfield

Research output: Contribution to journalArticlepeer-review

17 Scopus citations


Observation of the activation and inhibition of angiogenesis processes is important in the progression of cancer. Application of targeting peptides, such as a small peptide that contains adjacent l-arginine (R), glycine (G) and l-aspartic acid (D) residues can afford high selectivity and deep penetration in vessel imaging. To facilitate deep tissue vasculature imaging, probes that can be excited via two-photon absorption (2PA) in the near-infrared (NIR) and subsequently emit in the NIR are essential. In this study, the enhancement of tissue image quality with RGD conjugates was investigated with new NIR-emitting pyranyl fluorophore derivatives in two-photon fluorescence microscopy. Linear and nonlinear photophysical properties of the new probes were comprehensively characterized; significantly the probes exhibited good 2PA over a broad spectral range from 700-1100 nm. Cell and tissue images were then acquired and examined, revealing deep penetration and high contrast with the new pyranyl RGD-conjugates up to 350 μm in tumor tissue.

Original languageEnglish (US)
Pages (from-to)10716-10725
Number of pages10
JournalOrganic and Biomolecular Chemistry
Issue number43
StatePublished - 2015

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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