Ultrafiltration LC-MS for high throughput screening of natural products to various molecular targets
- Ultrafiltration LC-MS for high throughput screening of natural products to various molecular targets
- 최용수; Richard B. van Breemen
- Ultrafiltration; LC-MS; High throughput screening; natural products
- Issue Date
- 한국질량분석학회 2012여름정기학술대회
- , 33-33
- High throughput screening (HTS) is a crucial technology in drug discovery, which has been routinely used since
1990s as pharmaceuticals hold dramatically increasing number of their own libraries (> several million compounds).
Conventional HTS based on spectrometric detection, however, has a serious drawback when applied for drug
discovery in natural products. Unlike synthetic single compound, natural product extracts contains complex matrix
and multiple compounds which show too many false positives. Aff,rnity based mass spectrometric technique can be
avery altraclive screening method because of its selectivity and sensitivity. In this presentation, a high throughput
ultrafiltration LC-MS and MALDI- MS techniques will be introduoed to screen natural products for bioactive
compounds to several macromolecular targets, such as quinon reductase-2, Keap-1, estrogen receptors, retinoid X
receptors, and vitamin D receptor. Screening results obtained by these techniques demonstrated that affinity based
MS can be used for screening complex natural products targeted to many other enzymes and proteins.
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