期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 6, 页码 1514-1517出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm801481y
关键词
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资金
- NIH [R21 NS059669, GM 48677]
- Epilepsy Therapy Project
- Epilepsy Research Foundation
- University of Utah Startup Funds
Conjugated polyamines are potential carriers for biotherapeutics targeting the central nervous system. We describe an efficient synthesis of a polyamine-based amino acid, lysine-trimethylene(diNo-syl)-spermine(triBoc) with Dde or Fmoc orthogonal protecting groups. This nonnatural amino acid was incorporated into a neurotensin analogue using standard Fmoc-based protocols. The analogue maintained high affinity and agonist potency for neurotensin receptors and exhibited dramatically improved analgesia in mice. Our work provides a basis for use of polyamine amino acids in polypeptides.
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