Novel Small Molecule Probes for Metastatic Melanoma. Academic Article

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.

authors

• Burgess, Kevin

published proceedings

• ACS Med Chem Lett

author list (cited authors)

• Kamkaew, A., Fu, N., Cai, W., & Burgess, K.

citation count

• 11

complete list of authors

• Kamkaew, Anyanee||Fu, Nanyan||Cai, Weibo||Burgess, Kevin

publication date

• February 2017

publisher

• American Chemical Society (ACS)  Publisher

published in

• ACS Medicinal Chemistry Letters  Journal

keywords

• Cancer
• Melanoma
• Small Molecule Ligand
• Targeting

PubMed Central ID

• 28197308

Digital Object Identifier (DOI)

• 10.1021/acsmedchemlett.6b00368

start page

• 179

end page

• 184

volume

• 8

issue

• 2

URL

• http://dx.doi.org/10.1021/acsmedchemlett.6b00368