Synthesis and in vitro evaluation of α-synuclein ligands

L Yu, J Cui, PK Padakanti, L Engel, DP Bagchi…

Index: Yu, Lihai; Cui, Jinquan; Padakanti, Prashanth K.; Engel, Laura; Bagchi, Devika P.; Kotzbauer, Paul T.; Tu, Zhude Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 15 p. 4625 - 4634

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Citation Number: 11

Abstract

Accumulation of misfolded α-synuclein in Lewy bodies and Lewy neurites is the pathological hallmark of Parkinson's disease (PD). To identify ligands having high binding potency toward aggregated α-synuclein, we synthesized a series of phenothiazine derivatives and assessed their binding affinity to recombinant α-synuclein fibrils using a fluorescent thioflavin T competition assay. Among 16 new analogues, the in vitro data suggest that ...