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|Title:||Isolation and synthesis of falcitidin, a novel myxobacterial-derived acyltetrapeptide with activity against the malaria target falcipain-2|
Yan Leong, C.
|Source:||Somanadhan, B., Kotturi, S.R., Yan Leong, C., Glover, R.P., Huang, Y., Flotow, H., Buss, A.D., Lear, M.J., Butler, M.S. (2013-05). Isolation and synthesis of falcitidin, a novel myxobacterial-derived acyltetrapeptide with activity against the malaria target falcipain-2. Journal of Antibiotics 66 (5) : 259-264. ScholarBank@NUS Repository. https://doi.org/10.1038/ja.2012.123|
|Abstract:||A 384-well microtitre plate fluorescence cleavage assay was developed to identify inhibitors of the cysteine protease falcipain-2, an important antimalarial drug target. Bioassay-guided isolation of a MeOH extract from a myxobacterium Chitinophaga sp. Y23 isolated from soil collected in Singapore, led to the identification of a new acyltetrapeptide, falcitidin (1), which displayed an IC 50 value of 6 μM against falcipain-2. The planar structure of 1 was secured by NMR and MS/MS analysis. Attempts to isolate further material for biological testing were hampered by inconsistent production and by a low yield (<100 μg l -1). The absolute configuration of 1 was determined by Marfey's analysis and the structure was confirmed through total synthesis as isovaleric acid-D-His-L-Ile-L-Val-L-Pro-NH 2. Falcitidin (1) is the first member of a new class of falcipain-2 inhibitors and, unlike other peptide-based inhibitors, does not contain reactive groups that irreversibly bind to active cysteine sites. © 2013 Japan Antibiotics Research Association All rights reserved.|
|Source Title:||Journal of Antibiotics|
|Appears in Collections:||Staff Publications|
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