Pyrene‐Based Self‐Assembling Peptide for Ratiometric Detection of Heparin

Heparin is a commonly used anticoagulant in clinical practice; however, excessive heparin can cause serious adverse reactions. Convenient and accurate detection of heparin levels is thus very important. In this research, a pyrene‐based self‐assembling fluorescent peptide PyFFRRR was designed for simple, selective, and efficient heparin detection. The guanidine groups in the arginine residues of PyFFRRR bind tightly with heparin, which is highly sulfated, through electrostatic interactions. Charge neutralization facilitated the self‐assembly of PyFFRRR, resulting in its spectral response changing from deep blue monomer fluorescence to green excimer fluorescence. PyFFRRR exhibited excellent sensitivity and selectivity for ratiometric detection of heparin. The binding mechanism was investigated by using spectral and simulation tools, and structural observation. Finally, PyFFRRR was employed in human serum samples for ratiometric detection of heparin. Sample serum simply: A new pyrene peptide fluorescence probe based on 1‐pyrenebutanoic acid, phenylalanine and arginine, PyFFRRR, can be used to detect heparin content in aqueous solution and human serum samples quickly, simply and accurately.