Abstract / Description of output
Mass spectrometry imaging (MSI) provides pharmaceutical researchers with a suite of technologies to screen and assess compound distributions and relative abundances directly from tissue sections and offer insight into drug discovery-applicable queries such as blood-brain barrier access, tumor penetration/retention, and compound toxicity related to drug retention in specific organs/cell types. Label-free MSI offers advantages over label-based assays, such as quantitative whole-body autoradiography (QWBA), in the ability to simultaneously differentiate and monitor both drug and drug metabolites. Such discrimination is not possible by label-based assays if a drug metabolite still contains the radiolabel. Here, we present data exemplifying the advantages of MSI analysis. Data of the distribution of AZD2820, a therapeutic cyclic peptide, are related to corresponding QWBA data. Distribution of AZD2820 and two metabolites is achieved by MSI, which [(14)C]AZD2820 QWBA fails to differentiate. Furthermore, the high mass-resolving power of Fourier transform ion cyclotron resonance MS is used to separate closely associated ions.
Original language | English |
---|---|
Pages (from-to) | 187-93 |
Number of pages | 7 |
Journal | Journal of Biomolecular Screening |
Volume | 21 |
Issue number | 2 |
Early online date | 23 Dec 2015 |
DOIs | |
Publication status | Published - 1 Feb 2016 |
Keywords / Materials (for Non-textual outputs)
- Animals
- Autoradiography
- Blood-Brain Barrier
- Diagnostic Imaging
- Drug Discovery
- Male
- Mice, Inbred C57BL
- Neoplasms
- Peptides
- Pharmaceutical Preparations
- Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization