Plasmodium gametocyte inhibition identified from a natural-product-based fragment library

Vu, Hoan, Roullier, Catherine, Campitelli, Marc, Trenholme, Katharine R., Gardiner, Donald L., Andrews, Katherine T., Skinner-Adams, Tina, Crowther, Gregory J., Van Voorhis, Wesley C. and Quinn, Ronald J. (2013) Plasmodium gametocyte inhibition identified from a natural-product-based fragment library. ACS Chemical Biology, 8 12: 2654-2659. doi:10.1021/cb400582b


Author Vu, Hoan
Roullier, Catherine
Campitelli, Marc
Trenholme, Katharine R.
Gardiner, Donald L.
Andrews, Katherine T.
Skinner-Adams, Tina
Crowther, Gregory J.
Van Voorhis, Wesley C.
Quinn, Ronald J.
Title Plasmodium gametocyte inhibition identified from a natural-product-based fragment library
Formatted title
Plasmodium gametocyte inhibition identified from a natural-product-based fragment library
Journal name ACS Chemical Biology   Check publisher's open access policy
ISSN 1554-8929
1554-8937
Publication date 2013-12-01
Year available 2013
Sub-type Article (original research)
DOI 10.1021/cb400582b
Open Access Status Not Open Access
Volume 8
Issue 12
Start page 2654
End page 2659
Total pages 6
Place of publication Washington, DCUnited States
Publisher American Chemical Society
Language eng
Formatted abstract
Fragment-based screening is commonly used to identify compounds with relatively weak but efficient localized binding to protein surfaces. We used mass spectrometry to study fragment-sized three-dimensional natural products. We identified seven securinine-related compounds binding to Plasmodium falciparum 2′-deoxyuridine 5′-triphosphate nucleotidohydrolase (PfdUTPase). Securinine bound allosterically to PfdUTPase, enhancing enzyme activity and inhibiting viability of both P. falciparum gametocyte (sexual) and blood (asexual) stage parasites. Our results provide a new insight into mechanisms that may be applicable to transmission-blocking agents.
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Publication Date (Web): September 30, 2013

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2014 Collection
School of Medicine Publications
 
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