title: Novel Small Molecule Probes for Metastatic Melanoma.
abstract: Actively targeting probe1b, an unsymmetrical bivalent dipeptide mimic, selectively bound melanoma over healthy skin tissue in histological samples from patients and Sinclair swine. Modifications to1bgave agents2-4that contain a near-IR aza-BODIPY fluor. Contrary to our expectations, symmetrical probe3gave the highest melanoma-to-healthy skin selectivity in histochemistry and experiments with live cells; this was surprising because2, not3, is unsymmetrical like the original lead1. Optical imaging of3in a mouse melanoma model failed to show tumor accumulationin vivo, but the probe did selectively accumulate in the tumor (some in lung and less in the liver) as proven by analysis of the organs post mortem.
authors.affiliation: Department of Chemistry, Texas A & M University, Box 30012, College Station, Texas 77842, United States; Department of Radiology, University of Wisconsin-Madison, Madison, Wisconsin 53705, United States.
authors.forename: Anyanee
authors.initials: A
authors.lastname: Kamkaew
authors.affiliation: Department of Chemistry, Texas A & M University, Box 30012, College Station, Texas 77842, United States; Department of Chemistry, Fuzhou University, Fuzhou 350116, P. R. China.
authors.forename: Nanyan
authors.initials: N
authors.lastname: Fu
authors.affiliation: Department of Radiology, University of Wisconsin-Madison, Madison, Wisconsin 53705, United States; University of Wisconsin Carbone Cancer Center, University of Wisconsin-Madison, Madison, Wisconsin 53705, United States.
authors.forename: Weibo
authors.initials: W
authors.lastname: Cai
authors.affiliation: Department of Chemistry, Texas A & M University, Box 30012, College Station, Texas 77842, United States; Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.
authors.forename: Kevin
authors.initials: K
authors.lastname: Burgess
keywords: Targeting; cancer; melanoma; small molecule ligand