Journal article
Pseudoirreversible inhibition of prostate-specific membrane antigen by phosphoramidate peptidomimetics
Biochemistry (Easton), Vol.47(48), pp.12658-12660
12/02/2008
Handle:
https://hdl.handle.net/2376/102932
PMID: 18983168
Abstract
The mode of inhibition for phosphoramidate peptidomimetic inhibitors of prostate-specific membrane antigen was determined by inhibition reversibility experiments. The results revealed that these inhibitors can be classified into three types: pseudoirreversible (compounds 1-3), moderately reversible (compounds 4-9), and rapidly reversible inhibitors (compounds 10 and 11). Representative compounds from each class were further evaluated for their ability to induce cellular internalization of PSMA. Results from these experiments revealed that the pseudoirreversible inhibitor 1 induced the greatest PSMA internalization. The discovery of pseudoirreversible PSMA inhibitors is expected to provide a new avenue of investigation and therapeutic applications for prostate cancer and neurological disorders.
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Details
- Title
- Pseudoirreversible inhibition of prostate-specific membrane antigen by phosphoramidate peptidomimetics
- Creators
- Tiancheng Liu - Department of Chemistry, Washington State University, Pullman, Washington 99164-4630, USAYoko ToriyabeMarat KazakClifford E Berkman
- Publication Details
- Biochemistry (Easton), Vol.47(48), pp.12658-12660
- Academic Unit
- Chemistry, Department of
- Publisher
- United States
- Grant note
- S06-GM052588 / NIGMS NIH HHS 1R21CA122126-01 / NCI NIH HHS
- Identifiers
- 99900546565501842
- Language
- English
- Resource Type
- Journal article