Doxycycline derivatives binds efficiently to α-synuclein fibrils: Towards novel positron emission tomography probes

MACHIN, MB; SANDOBAL, J; MESSINA, G; CASALE, G; FERRARIO, J; BASTIANELLO, M; VARELA, O; AVILA, CL; CHEHIN, RN

Lima

Encuentro; Thematic Meeting "Revisiting the Central Dogma of Molecular Biology at the Single-Molecule Level; 2019

Biophysical Society

The evolution and prognosis of Parkinson's disease (PD) correlates with the deposition of α-synuclein (AS) aggregates in the brain. This fact opens the door to monitor the progression of patients with PD using state of the art imaging studies such as positron emission tomography (PET). Unfortunately, nowadays there is no PET marker for the selective detection of pathological α-synuclein in this disorder.The aim of this study was to evaluate novel chemical entities that could have high affinity and selectivity for AS aggregates and which could serve as compounds for PET radiotracers development. We have previously reported that doxycycline can bind to α-synuclein aggregates but not to monomeric α-synuclein. For this reason, we propose the doxycycline and novel synthetic analogues as candidates for α-synuclein imaging PET radiotracers