Abstract

Structural Biochemistry Program, SAIC Frederick, National Cancer Institute-Frederick Cancer Research and Development Center, P.O Box B, Frederick, MD 21702-1201. Present Address: Tibotec Inc., 1330 Piccard Dr., Rockville, MD, 20850. 1Present Address: Gilford Pharmaceuticals Inc., 6611 Tributary Street, Baltimore, MD, 21224. Plasmepsin 2 is a malarial aspartic proteinase that has been implicated in initial steps of hemoglobin degradation in parasite and thus represents an attractive antimalarial target. We designed and synthesized a number of quenched fluorogenic substrates and measured the kinetic constants of their cleavage by plasmepsin-2. High sensitivity and superior kinetic properties make the substrates suitable for different application including fluorescence plate reader.