Novel Small Molecule Probes for Metastatic Melanoma.

ACS Med Chem Lett

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.

Published: February 2017

Actively targeting probe , an unsymmetrical bivalent dipeptide mimic, selectively bound melanoma over healthy skin tissue in histological samples from patients and Sinclair swine. Modifications to gave agents - that contain a near-IR aza-BODIPY fluor. Contrary to our expectations, symmetrical probe gave the highest melanoma-to-healthy skin selectivity in histochemistry and experiments with live cells; this was surprising because , not , is unsymmetrical like the original lead . Optical imaging of in a mouse melanoma model failed to show tumor accumulation , 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.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5304293PMC
http://dx.doi.org/10.1021/acsmedchemlett.6b00368DOI Listing

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