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Updated: Mar 7, 2026
A Robust Discovery Platform for the Identification of Novel Mediators of Melanoma Metastasis
Published on: March 8, 2022
Novel Small Molecule Probes for Metastatic Melanoma
Anyanee Kamkaew1, Nanyan Fu2, Weibo Cai3
1Department 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.
Abstract:
Actively targeting probe 1b, an unsymmetrical bivalent dipeptide mimic, selectively bound melanoma over healthy skin tissue in histological samples from patients and Sinclair swine. Modifications to 1b gave agents 2-4 that contain a near-IR aza-BODIPY fluor. Contrary to our expectations, symmetrical probe 3 gave the highest melanoma-to-healthy skin selectivity in histochemistry and experiments with live cells; this was surprising because 2, not 3, is unsymmetrical like the original lead 1. Optical imaging of 3 in a mouse melanoma model failed to show tumor accumulation in 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.
