School of Ophthalmology & Optometry, School of Biomedical Engineering, Institute of Advanced Materials for Nano-Bio Applications, Wenzhou Medical University, Wenzhou 325027, China
ZHOU Chaoqun,TANG Shipeng,QIAN Liangliang, et al. Synthesis of Schiff base of adenosine 3’, 5’-cyclicmonophosphoric acid with xanthone and its binding to LC3B[J]. JOURNAL OF WEZHOU MEDICAL UNIVERSITY, 2021, 51(7): 570-573.
Abstract：Objective: To design the potential proteolysis targeting chimeras (PROTAC) drug S1 synthesized from adenosine 3’, 5’-cyclicmonophosphoric acid and xanthone. Methods: The binding kinetics of S1 and LC3B was characterized by UV-Vis spectroscopy. The resulted data were fitted to first order reaction kinetics.The binding constants and thermodynamic constants of the S1-LC3B complex were determined by fluorescence spectroscopy, and the molecular binding mechanism was deduced. Results: S1 bound to LC3B fast within 160 s.The binding kinetics obeyed the first order reaction kinetics equation and specific transport rule. Thermodynamic
study found that the Gibbs free energy change was negative, indicating a spontaneous binding process. And negative enthalpy change suggested a static attraction between S1 and LC3B. Such course was attributed to the interaction of C=N at S1 with LC3B, resulting in fluorescence quenching. Conclusion: The Schiff base S1 can
spontaneously bind to LC3B.
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