Synthesis and biological evaluation of S-lipidated lipopeptides of a connexin 43 channel inhibitory peptide,RSC Medicinal Chemistry

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Synthesis and biological evaluation of S-lipidated lipopeptides of a connexin 43 channel inhibitory peptide
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-07-10 , DOI: 10.1039/d0md00172d
Sung-Hyun Yang _{1,

2} , Connor A Clemett ₃ , Margaret A Brimble _{1,

2,

4} , Simon J O'Carroll ₃ , Paul W R Harris _{1,

2,

4}

Affiliation

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.

中文翻译：

连接蛋白43通道抑制肽S-脂化脂肽的合成及生物学评价

描述了连接蛋白 43 通道抑制肽 5 的 42 种新型S-脂化类似物的合成和生物活性。未修饰的 Peptide5 可调节与神经系统疾病进展有关的半通道和间隙连接。 Peptide5 用半胱氨酸残基进行位点特异性修饰，然后进行硫醇-烯介导的S-脂化，得到含有直链、支链或芳香族脂质的S-脂化 Peptide5 类似物。评估了修饰肽对半通道开放的影响，并在血清稳定性研究中评估了最有前途的候选肽。

更新日期：2020-07-10

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