We previously showed that the 5A peptide can promote cholesterol efflux by the ABCA1 transporter and reduce atherosclerosis in animal models. The peptide was licensed to KineMed Inc, who received a RAID grant for performing preclinical toxicology studies, which have commenced. We have done additional structure function studies on the 5A peptide and identified 2 key hydrophobic residues in the hinge region of this bi-helical peptide for it to be able to promote cholesterol efflux. Based on this finding, we developed a new membrane solubilization model for how apolipoprotein mimetic peptides interact with membranes and promote cholesterol efflux.

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National Heart, Lung, and Blood Institute
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Liu, Zheng; Thacker, Seth G; Fernandez-Castillejo, Sara et al. (2014) Synthesis of cholesterol analogues bearing BODIPY fluorophores by Suzuki or Liebeskind-Srogl cross-coupling and evaluation of their potential for visualization of cholesterol pools. Chembiochem 15:2087-96
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