Lasarte J J, Sarobe P, Golvano J, Prieto I, Civeira M P, Gullón A, Sarin P S, Prieto J, Borrás-Cuesta F
Departamento de Medicina Interna, Facultad de Medicina, Universidad de Navarra, Pamplona, Spain.
J Acquir Immune Defic Syndr (1988). 1994 Feb;7(2):129-34.
Phenylalanine-containing peptides from CD4 were synthesized based on chemical similarity with active CD4(81-92)-benzylated peptides. The synthetic peptide FYIFFVEDQKEEDD blocked the binding of gp120 to CD4 and inhibited 50% human immunodeficiency virus (HIV)-induced syncytia formation at a concentration (IC50) of approximately 40-50 microM and HIV p17 expression with an IC50 of approximately 67 microM. The peptide is not toxic to cells in vitro. Moreover, acute toxicity studies carried out in Swiss mice showed the peptide to be nontoxic at a dose of 2,000 mg/kg. This phenylalanine-substituted CD4 peptide may prove to be useful in the treatment of AIDS.
基于与活性CD4(81 - 92) - 苄基化肽的化学相似性，合成了含苯丙氨酸的CD4肽。合成肽FYIFFVEDQKEEDD在浓度（IC50）约为40 - 50微摩尔时可阻断gp120与CD4的结合，并抑制50%的人类免疫缺陷病毒（HIV）诱导的合胞体形成，在IC50约为67微摩尔时可抑制HIV p17表达。该肽在体外对细胞无毒。此外，在瑞士小鼠中进行的急性毒性研究表明，该肽在剂量为2000毫克/千克时无毒。这种苯丙氨酸取代的CD4肽可能被证明对艾滋病治疗有用。
