Roberts Sophie E, Martin Heather L, Al-Qallaf Danah, Tang Anna A, Tiede Christian, Gaule Thembaninkosi G, Dobon-Alonso Albor, Overman Ross, Shah Sachin, Peyret Hadrien, Saunders Keith, Bon Robin, Manfield Iain W, Bell Sandra M, Lomonossoff George P, Speirs Valerie, Tomlinson Darren C
School of Molecular and Cellular Biology, University of Leeds, Leeds, UK.
Astbury Centre for Structural and Molecular Biology, University of Leeds, Leeds, UK.
iScience. 2024 Jul 5;27(8):110461. doi: 10.1016/j.isci.2024.110461. eCollection 2024 Aug 16.
Monoclonal antibodies have revolutionized therapies, but non-immunoglobulin scaffolds are becoming compelling alternatives owing to their adaptability. Their ability to be labeled with imaging or cytotoxic compounds and to create multimeric proteins is an attractive strategy for therapeutics. Focusing on HER2, a frequently overexpressed receptor in breast cancer, this study addresses some limitations of conventional targeting moieties by harnessing the potential of these scaffolds. HER2-binding Affimers were isolated and characterized, demonstrating potency as binding reagents and efficient internalization by HER2-overexpressing cells. Affimers conjugated with cytotoxic agent achieved dose-dependent reductions in cell viability within HER2-overexpressing cell lines. Bispecific Affimers, targeting HER2 and virus-like particles, facilitated efficient internalization of virus-like particles carrying enhanced green fluorescent protein (eGFP)-encoding RNA, leading to protein expression. Anti-HER2 affibody or designed ankyrin repeat protein (DARPin) fusion constructs with the anti-VLP Affimer further underscore the adaptability of this approach. This study demonstrates the versatility of scaffolds for precise delivery of cargos into cells, advancing biotechnology and therapeutic research.
单克隆抗体彻底改变了治疗方法,但非免疫球蛋白支架因其适应性正成为引人注目的替代方案。它们能够用成像或细胞毒性化合物进行标记并生成多聚体蛋白,这是一种颇具吸引力的治疗策略。本研究聚焦于HER2(一种在乳腺癌中经常过度表达的受体),通过利用这些支架的潜力解决了传统靶向部分的一些局限性。分离并表征了与HER2结合的Affimer,证明其作为结合试剂的效力以及在HER2过表达细胞中的有效内化。与细胞毒性剂偶联的Affimer在HER2过表达细胞系中实现了细胞活力的剂量依赖性降低。靶向HER2和病毒样颗粒的双特异性Affimer促进了携带增强型绿色荧光蛋白(eGFP)编码RNA的病毒样颗粒的有效内化,从而导致蛋白表达。抗HER2亲和体或与抗病毒样颗粒Affimer设计的锚蛋白重复蛋白(DARPin)融合构建体进一步强调了这种方法的适应性。本研究证明了支架在将货物精确递送至细胞方面的多功能性,推动了生物技术和治疗研究的发展。