在这项研究中,合成了一系列新颖的棉酚衍生物,并在体外对其抗HIV-1和抗H 5 N 1活性进行了筛选。用某些氨基酸取代棉酚的醛基,不仅可以降低细胞毒性,而且还可以增强对HIV-1和H 5 N 1的活性。与其他棉酚衍生物相比,化合物13 – 17对HIV-1和H 5 N 1的活性更强。同时,这些化合物还对H 5 N 1表现出更强的活性。比1-金刚烷胺。棉酚衍生物中缺少COONa基团会导致抗HIV-1活性的丧失,这表明该基团可能在介导抗病毒活性中起重要作用。添加时间分析表明,化合物13 – 17具有与T20相似的抗HIV-1作用机理。分子建模分析表明,化合物13 - 17可能适合的gp41的疏水口袋内通过氢键网络,疏水性接触性强的静电相互作用。
Peptide/Protein Stapling and Unstapling: Introduction of <i>s</i>-Tetrazine, Photochemical Release, and Regeneration of the Peptide/Protein
作者:Stephen P. Brown、Amos B. Smith
DOI:10.1021/ja512880g
日期:2015.4.1
Protocols have been achieved that permit facile introduction of s-tetrazine into unprotected peptides and the protein, thioredoxin, between two cysteine sulfhydryl groups (i.e., staple), followed by photochemical release (i.e., unstaple) and regeneration of the peptide/protein upon removal of the cyano groups from the derived bisthiocyanate. The S,S-tetrazine macrocycles in turn provide a convenient handle for probe introduction by exploiting the inverse electron demand Diels-Alder reactivity of the tetrazine.
586. Some derivatives of S-carboxyalkyl-cysteines and -homocysteines