화학공학소재연구정보센터
학회 한국공업화학회
학술대회 2017년 봄 (05/10 ~ 05/12, 광주 김대중컨벤센센터(Kimdaejung Convention Center))
권호 21권 1호
발표분야 생체재료
제목 Design and synthesis of cyclic peptide-peptoid hybrid macrocycles
초록  Cyclic peptide has been to the fore as a privileged structure recently with excellent properties such as stability and membrane permeability. Cyclosporin A (CsA) and daptomycin are naturally occurring cyclic peptides, which demonstrated their versatile pharmacological activity such as immunosuppressant or antibacterial activity. Recent studies show peptidomimetic macrocycles demonostrated improved bioactivity and pharmacokinetic profiles compared to natural compound. Herein, a new class of peptide-peptoid hybrid macrocycle was designed. Basic scaffold was adopted from CsA, and peptoid residues, N-substituted glycines, substituted for some part of the cyclic peptide sequence at the β-turn positions. Macrocyclic peptide-peptoid hybrids were synthesized via standard SPPS, while cyclization was performed in a solution phase. Employing the framework of peptide-peptoid hybrid, molecular diversity can be achieved providing a library of privileged structures in the bRo5 chemical space.
저자 이동재, 서지원
소속 광주과학기술원
키워드 cyclic peptide; peptoid; macrocycle
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