Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 20, Issue 25, Pages 5076-5085Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d2ob00717g
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Funding
- National Natural Science Foundation of China [82174161]
- Department of Education of Guangdong Province [2021ZDZX2030, 2020ZDZX2017]
- Guangdong Basic and Applied Basic Research Foundation [2021A1515110115]
- Foundation of Guangzhou Basic and Applied Basic Research [202102020548, 202102010257]
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In this study, a fluorescent probe TTPy was prepared and shown to bind with human serum albumin, enabling fluorescent labeling under visible light irradiation. Competitive binding assay revealed its interaction with a group of non-steroidal anti-inflammatory drugs at their binding site.
Human serum albumin (HSA) can bind with numerous drugs, leading to a significant influence on drug pharmacokinetics as well as undesirable drug-drug interactions due to competitive binding. Probing the HSA drug binding site thus offers great opportunities to reveal drug-HSA binding profiles. In the present study, a fluorescent probe (E)-4-(2-(5-(4-(diphenylamino)phenyl)thiophen-2-yl)vinyl)-1-propylpyridin-1-ium (TTPy) has been prepared, which exhibits enhancement of deep-red to near-infrared (NIR) fluorescence upon HSA binding. The competitive binding assay indicated that TTPy can target the HSA binding site of fenamates, a group of non-steroidal anti-inflammatory drugs (NSAIDs), with moderate binding affinity (1.95 x 10(6) M-1 at 303 K). More interestingly, TTPy enables fluorescent labeling of HSA upon visible light irradiation. This study provides promising ways for HSA drug binding site identification and photochemical protein labeling.
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