4.6 Article

Solid-Phase Synthetic Route to Multiple Derivatives of a Fundamental Peptide Unit

期刊

MOLECULES
卷 15, 期 7, 页码 4961-4983

出版社

MDPI AG
DOI: 10.3390/molecules15074961

关键词

Distributed Drug Discovery (D3); fundamental peptide scaffold; biomimetics; solid-phase organic synthesis; combinatorial chemistry

资金

  1. National Institutes of Health [R01 GM028193]
  2. National Science Foundation [MRI CHE-0619254]
  3. Camille and Henry Dreyfus Foundation
  4. Central Indiana Community Foundation
  5. Polish Ministry of Science and Higher Education (MNiSW) [N N405 378437]
  6. Direct For Biological Sciences
  7. Div Of Biological Infrastructure [0821661] Funding Source: National Science Foundation

向作者/读者索取更多资源

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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