Journal
MOLECULES
Volume 15, Issue 7, Pages 4961-4983Publisher
MDPI AG
DOI: 10.3390/molecules15074961
Keywords
Distributed Drug Discovery (D3); fundamental peptide scaffold; biomimetics; solid-phase organic synthesis; combinatorial chemistry
Funding
- National Institutes of Health [R01 GM028193]
- National Science Foundation [MRI CHE-0619254]
- Camille and Henry Dreyfus Foundation
- Central Indiana Community Foundation
- Polish Ministry of Science and Higher Education (MNiSW) [N N405 378437]
- Direct For Biological Sciences
- Div Of Biological Infrastructure [0821661] Funding Source: National Science Foundation
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Amino acids are Nature's combinatorial building blocks. When substituted on both the amino and carboxyl sides they become the basic scaffold present in all peptides and proteins. We report a solid-phase synthetic route to large combinatorial variations of this fundamental scaffold, extending the variety of substituted biomimetic molecules available to successfully implement the Distributed Drug Discovery (D3) project. In a single solid-phase sequence, compatible with basic amine substituents, three-point variation is performed at the amino acid alpha-carbon and the amino and carboxyl functionalities.
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