通过对源自合成天然人抗体文库且靶向gp41内部三聚体卷曲螺旋的单克隆Fab的CDR-H2环进行靶向多样化实现亲和力成熟,从而产生了一组具有更高HIV-1中和效力和广度的Fab。
Affinity maturation by targeted diversification of the CDR-H2 loop of a monoclonal Fab derived from a synthetic naïve human antibody library and directed against the internal trimeric coiled-coil of gp41 yields a set of Fabs with improved HIV-1 neutralization potency and breadth.
作者信息
Gustchina Elena, Louis John M, Frisch Christian, Ylera Francisco, Lechner Annette, Bewley Carole A, Clore G Marius
机构信息
Laboratory of Chemical Physics, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0520, USA.
出版信息
Virology. 2009 Oct 10;393(1):112-9. doi: 10.1016/j.virol.2009.07.019. Epub 2009 Aug 19.
Previously we reported a broadly HIV-1 neutralizing mini-antibody (Fab 3674) of modest potency that was derived from a human non-immune phage library by panning against the chimeric gp41-derived construct N(CCG)-gp41. This construct presents the N-heptad repeat of the gp41 ectodomain as a stable, helical, disulfide-linked trimer that extends in helical phase from the six-helix bundle of gp41. In this paper, Fab 3674 was subjected to affinity maturation against the N(CCG)-gp41 antigen by targeted diversification of the CDR-H2 loop to generate a panel of Fabs with diverse neutralization activity. Three affinity-matured Fabs selected for further study, Fabs 8060, 8066 and 8068, showed significant increases in both potency and breadth of neutralization against HIV-1 pseudotyped with envelopes of primary isolates from the standard subtype B and C HIV-1 reference panels. The parental Fab 3674 is 10-20-fold less potent in monovalent than bivalent format over the entire B and C panels of HIV-1 pseudotypes. Of note is that the improved neutralization activity of the affinity-matured Fabs relative to the parental Fab 3674 was, on average, significantly greater for the Fabs in monovalent than bivalent format. This suggests that the increased avidity of the Fabs for the target antigen in bivalent format can be partially offset by kinetic and/or steric advantages afforded by the smaller monovalent Fabs. Indeed, the best affinity-matured Fab (8066) in monovalent format ( approximately 50 kDa) was comparable in HIV-1 neutralization potency to the parental Fab 3674 in bivalent format ( approximately 120 kDa) across the subtype B and C reference panels.
此前我们报道了一种具有中等效力的广谱HIV-1中和微型抗体(Fab 3674),它是通过筛选人非免疫噬菌体文库获得的,筛选对象是嵌合gp41衍生构建体N(CCG)-gp41。该构建体将gp41胞外域的N-七肽重复序列呈现为一种稳定的、螺旋状的、二硫键连接的三聚体,它从gp41的六螺旋束以螺旋相位延伸。在本文中,通过对互补决定区H2环进行靶向多样化,使Fab 3674针对N(CCG)-gp41抗原进行亲和力成熟,以产生一组具有不同中和活性的Fab。选择用于进一步研究的三种亲和力成熟的Fab,即Fab 8060、8066和8068,对来自标准B型和C型HIV-1参考面板的原代分离株包膜假型化的HIV-1的中和效力和广度均有显著提高。在整个HIV-1假型的B型和C型面板中,亲本Fab 3674单价形式的效力比二价形式低10至20倍。值得注意的是,相对于亲本Fab 3674,亲和力成熟的Fab的中和活性提高,平均而言,单价形式的Fab比二价形式的Fab显著更大。这表明二价形式的Fab对靶抗原亲和力的增加可被较小的单价Fab所提供的动力学和/或空间优势部分抵消。实际上,在整个B型和C型参考面板中,单价形式(约50 kDa)的最佳亲和力成熟Fab(8066)在HIV-1中和效力方面与二价形式(约120 kDa)的亲本Fab 3674相当。
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