Application of ring-closing metathesis macrocyclization to the development of Tsg101-binding antagonists

…, AG Stephen, AA Waheed, EO Freed, RJ Fisher…

文献索引：Liu, Fa; Stephen, Andrew G.; Waheed, Abdul A.; Freed, Eric O.; Fisher, Robert J.; Burke Jr., Terrence R. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 1 p. 318 - 321

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被引用次数: 8

摘要

HIV-1 viral budding involves binding of the viral Gagp6 protein to the ubiquitin E2 variant domain of the human tumor susceptibility gene 101 protein (Tsg101). Recognition of p6 by Tsg101 is mediated in part by a proline-rich motif that contains the sequence 'Pro-Thr-Ala- Pro'('PTAP'). Using the p6-derived 9-mer sequence 'PEPTAPPEE', we had previously improved peptide binding affinity by employing N-alkylglycine ('peptoid') residues. The ...