Department of Bioinformatics, Caris Life Sciences, Phoenix, Arizona, United States of America.
Center for Innovations in Medicine, Biodesign Institute, Arizona State University, Tempe, Arizona, United States of America.
PLoS One. 2020 Mar 20;15(3):e0229080. doi: 10.1371/journal.pone.0229080. eCollection 2020.
Therapeutic monoclonal antibodies have the potential to work as biological therapeutics. OKT3, Herceptin, Keytruda and others have positively impacted healthcare. Antibodies evolved naturally to provide high specificity and high affinity once mature. These characteristics can make them useful as therapeutics. However, we may be missing characteristics that are not obvious. We present a means of measuring antibodies in an unbiased manner that may highlight therapeutic activity. We propose using a microarray of random peptides to assess antibody properties. We tested twenty-four different commercial antibodies to gain some perspective about how much information can be derived from binding antibodies to random peptide libraries. Some monoclonals preferred to bind shorter peptides, some longer, some preferred motifs closer to the C-term, some nearer the N-term. We tested some antibodies with clinical activity but whose function was blinded to us at the time. We were provided with twenty-one different monoclonal antibodies, thirteen mouse and eight human IgM. These antibodies produced a variety of binding patterns on the random peptide arrays. When unblinded, the antibodies with polyspecific binding were the ones with the greatest therapeutic activity. The protein target to these therapeutic monoclonals is still unknown but using common sequence motifs from the peptides we predicted several human and mouse proteins. The same five highest proteins appeared in both mouse and human lists.
治疗性单克隆抗体具有成为生物治疗药物的潜力。OKT3、赫赛汀、可瑞达等药物已对医疗保健产生积极影响。抗体在成熟后自然进化,以提供高度特异性和高亲和力。这些特性使它们成为有用的治疗药物。然而,我们可能忽略了一些不明显的特性。我们提出了一种以无偏倚的方式测量抗体的方法,这可能突出治疗活性。我们建议使用随机肽微阵列来评估抗体特性。我们测试了 24 种不同的商业抗体,以了解从结合抗体到随机肽库中获得多少信息。一些单克隆抗体更喜欢结合较短的肽,一些较长的肽,一些更喜欢靠近 C 端的基序,一些靠近 N 端。我们测试了一些具有临床活性但当时对我们来说功能未知的抗体。我们提供了 21 种不同的单克隆抗体,13 种是小鼠的,8 种是人类的 IgM。这些抗体在随机肽阵列上产生了各种结合模式。当揭盲时,具有多特异性结合的抗体是具有最大治疗活性的抗体。这些治疗性单克隆抗体的蛋白质靶标仍然未知,但我们使用来自肽的常见序列基序预测了几种人类和小鼠蛋白质。前五个最高的蛋白质同时出现在小鼠和人类的列表中。