Kurtz Keifer G, Lebedeva Irina, Pierre Stephanie A, Andrew David, Liao Yu-Rou, Ambriz Daisy, Vergnolle Olivia, Shen Leyi, Nyakatura Elizabeth, Baca Manuel, Scheinberg David A
Molecular Pharmacology Program, Sloan Kettering Institute, New York, United States of America.
Pharmacology Program, Weill Cornell Medicine, New York, United States of America.
PLoS One. 2025 May 23;20(5):e0321169. doi: 10.1371/journal.pone.0321169. eCollection 2025.
Several T cell immune checkpoint blockade therapies have shown initial successes in multiple cancers. However, significant issues remain, including tumor relapse, severe toxicities, and a lack of efficacy in most patients. SIRPα, commonly known as the "do not eat me signal", is a monocyte checkpoint cell surface protein. Agents that block the interaction of CD47 with SIRPα have recently shown clinical success in combination with monoclonal antibody therapy to potentiate macrophage phagocytosis of tumors. However, significant toxicities and logistical issues are associated with CD47-targeted agents due to the expression of CD47 on all human cells. In contrast, SIRPα has expression limited to myelomonocytic cells, meaning highly specific SIRPα blocking agents might reduce these toxicities and avoid the target antigen sink. Herein, we generated a high affinity and highly specific SIRPα-targeting monoclonal antibody, F05, that has enhanced SIRPα binding and reduced SIRPβ and SIRPγ binding capacity when compared to other available SIRPα antibodies. Furthermore, we show F05 reprograms immunosuppressive macrophages toward a phagocytic profile in vitro. F05 demonstrated efficacy in solid tumor animal models, providing a rationale for further development of the antibody.
几种T细胞免疫检查点阻断疗法已在多种癌症中初显成效。然而,仍存在重大问题,包括肿瘤复发、严重毒性以及大多数患者缺乏疗效。信号调节蛋白α(SIRPα),通常被称为“别吃我信号”,是一种单核细胞检查点细胞表面蛋白。阻断CD47与SIRPα相互作用的药物最近在与单克隆抗体疗法联合使用以增强巨噬细胞对肿瘤的吞噬作用方面显示出临床成效。然而,由于CD47在所有人类细胞上均有表达,靶向CD47的药物存在显著毒性和后勤保障问题。相比之下,SIRPα仅在骨髓单核细胞中表达,这意味着高度特异性的SIRPα阻断剂可能会降低这些毒性并避免靶抗原耗竭。在此,我们制备了一种高亲和力和高特异性的靶向SIRPα的单克隆抗体F05,与其他可用的SIRPα抗体相比,它具有增强的SIRPα结合能力以及降低的SIRPβ和SIRPγ结合能力。此外,我们发现F05在体外可将免疫抑制性巨噬细胞重编程为具有吞噬功能的细胞表型。F05在实体瘤动物模型中显示出疗效,为该抗体的进一步研发提供了理论依据。