Please use this identifier to cite or link to this item:
|Title:||Isolation and synthesis of falcitidin, a novel myxobacterial-derived acyltetrapeptide with activity against the malaria target falcipain-2|
Yan Leong, C.
|Citation:||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|
Show full item record
Files in This Item:
There are no files associated with this item.
checked on Jul 14, 2018
WEB OF SCIENCETM
checked on Jun 19, 2018
checked on Jul 6, 2018
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.