Identification of synthetic phosphatidylserine translocases from a combinatorial library prepared by directed split-and-pool synthesis

Journal of Combinatorial Chemistry
Rameshwer ShuklaBradley D Smith

Abstract

Simple sulfonamide and amide derivatives of tris(2-aminoethyl)amine (Tren) are known to promote the translocation or flip-flop of phosphatidylcholine, but not phosphatidylserine, across bilayer membranes. This paper describes the synthesis of a 300-member, spatially encoded library of Tren derivatives with appended peptide--sulfonamide and peptide--urea arms. The library was synthesized using the Encore method with SynPhase lanterns as the solid support. A high-throughput assay was developed to screen individual members of the library for an ability to translocate a fluorescent NBD derivative of phosphatidylserine across vesicle membranes. Several lead compounds were identified, and one was synthesized independently to confirm its high phosphatidylserine translocation activity.

References

Nov 14, 2000·Biopolymers·F RasoulN J Maeji
Feb 11, 2003·Journal of Lipid Research·David L Daleke
Jan 13, 2004·Journal of Combinatorial Chemistry·Marcel PatekPeter Strop

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Citations

Jul 13, 2006·Journal of the American Chemical Society·Christopher C ForbesBradley D Smith
Sep 8, 2007·Bioconjugate Chemistry·Christine A WinschelVladimir Sidorov
Nov 15, 2005·Journal of Combinatorial Chemistry·Roland E Dolle

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