Development of a fluorescent cardiomyocyte specific binding probe.

TitleDevelopment of a fluorescent cardiomyocyte specific binding probe.
Publication TypeJournal Article
Year of Publication2016
AuthorsPes L, Kim Y, Tung C-H
JournalBioorg Med Chem
Volume24
Issue8
Pagination1706-17
Date Published2016 Apr 15
ISSN1464-3391
KeywordsAnimals, Fluorescent Dyes, Mice, Molecular Structure, Myocytes, Cardiac, Structure-Activity Relationship, Substrate Specificity
Abstract

Cardiomyocytes are the major component of the heart. Their dysfunction or damage could lead to serious cardiovascular diseases, which have claimed numerous lives around the world. A molecule able to recognize cardiomyocytes would have significant value in diagnosis and treatment. Recently a novel peptide termed myocyte targeting peptide (MTP), with three residues of a non-natural amino acid biphenylalanine (Bip), showed good affinity to cardiomyocytes. Its selectivity towards cardiac tissues was concluded to be due to the ability of Bip to bind cardiac troponin I. With the aim of optimizing the affinity and the specificity towards cardiac myocytes and to better understand structure-activity relationship, a library of MTP derivatives was designed. Exploiting a fluorescent tag, the selectivity of the MTP analogs to myocardium over skeletal and stomach muscle tissues was assayed by fluorescence imaging. Among the tested sequences, the peptide probe Bip2, H-Lys(FITC)-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Ser-Gly-Ser-Bip-Bip-NH2, displayed the best selectivity for cardiomyocytes.

DOI10.1016/j.bmc.2016.02.042
Alternate JournalBioorg Med Chem
PubMed ID26964676
Grant ListS10OD016320-01 / OD / NIH HHS / United States
Related Institute: 
Molecular Imaging Innovations Institute (MI3)

Weill Cornell Medicine
Department of Radiology
525 East 68th Street New York, NY 10065