Development of a fluorescent cardiomyocyte specific binding probe
| Autor: | Lara Pes, Young Tai Kim, Ching-Hsuan Tung |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Fluorescence-lifetime imaging microscopy Cardiac troponin Clinical Biochemistry Pharmaceutical Science Peptide 030204 cardiovascular system & hematology Biochemistry Substrate Specificity Mice Structure-Activity Relationship 03 medical and health sciences 0302 clinical medicine Drug Discovery Animals Myocyte Structure–activity relationship Myocytes Cardiac Molecular Biology Fluorescent Dyes chemistry.chemical_classification Molecular Structure Chemistry Organic Chemistry Fluorescence Amino acid 030104 developmental biology Molecular Medicine Fluorescent tag |
| Zdroj: | Bioorganic & Medicinal Chemistry. 24:1706-1717 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2016.02.042 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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