Synthesis and biological evaluation of S-lipidated lipopeptides of a connexin 43 channel inhibitory peptide

文献情報

出版日 2020-07-10

DOI 10.1039/D0MD00172D

インパクトファクター 0

著者

Connor A. Clemett, Simon J. O'Carroll

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要旨

The synthesis and biological activity of 42 novel S-lipidated analogues of a connexin 43 channel inhibitory Peptide5 is described. Unmodified Peptide5 moderates hemichannels and gap junctions that are both implicated in the progression of neurological disease. Peptide5 was site-specifically modified with a cysteine residue, which then underwent thiol–ene mediated S-lipidation to afford S-lipidated Peptide5 analogues containing straight-chain, branched, or aromatic lipids. The modified peptides were assessed for their effect on hemichannel opening and the most promising candidates were evaluated in serum stability studies.

掲載誌

RSC Medicinal Chemistry

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Synthesis and biological evaluation of S-lipidated lipopeptides of a connexin 43 channel inhibitory peptide

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RSC Medicinal Chemistry

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