专利号:US-5859191-A 优先权日:1996-12-05 标 题:Method for the site-specific modification of peptide alpha amines 发明人:MILLER STEPHEN; SCANLAN THOMAS S 权利人:UNIV CALIFORNIA 摘要:A peptide comprising a free terminal alpha amine is treated with an aryl sulfonamide activating agent, resulting in an activated amide. The resulting activated amide is deprotonated with a base and modified by the addition of a substituent group. The aryl sulfonamide activating group is cleaved using a nucleophilic substitution reaction. The method is particularly useful for the modification of peptides at specific N-alpha positions, and is compatible with conventional solid phase peptide synthesis, including those that utilize Fmoc protecting groups.
参考文献:10.1097/00005344-199310000-00015 摘要:Ku DD, Zaleski JK. Receptor Mechanism of Thrombin-Induced Endothelium-Dependent and Endothelium-Independent Coronary Vascular Effects in Dogs. Journal of Cardiovascular Pharmacology. 1993 Oct;22(4):609–76. doi: 10.1097/00005344-199310000-00015. 参考文献:10.1016/s0021-9258(17)37225-3 摘要:Mari B, Imbert V, Belhacene N, Far DF, Peyron JF, Pouysségur J, Van Obberghen-Schilling E, Rossi B, Auberger P. Thrombin and thrombin receptor agonist peptide induce early events of T cell activation and synergize with TCR cross-linking for CD69 expression and interleukin 2 production. Journal of Biological Chemistry. 1994 Mar;269(11):8517–23. doi: 10.1016/s0021-9258(17)37225-3. 参考文献:10.1016/s0021-9258(17)36738-8 摘要:Shankar R, de la Motte CA, Poptic EJ, DiCorleto PE. Thrombin receptor-activating peptides differentially stimulate platelet-derived growth factor production, monocytic cell adhesion, and E-selectin expression in human umbilical vein endothelial cells. Journal of Biological Chemistry. 1994 May;269(19):13936–41. doi: 10.1016/s0021-9258(17)36738-8. 参考文献:10.1016/0014-2999(94)90613-0 摘要:Antonaccio MJ, Normandin D. Role of Ca2+ in the vascular contraction caused by a thrombin receptor activating peptide. Eur J Pharmacol. 1994 Apr 11;256(1):37–44. doi: 10.1016/0014-2999(94)90613-0.