Rader Christoph
Department of Cancer Biology, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #2C1, Jupiter, FL 33458, USA; Department of Molecular Therapeutics, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #2C1, Jupiter, FL 33458, USA.
Trends Biotechnol. 2014 Apr;32(4):186-97. doi: 10.1016/j.tibtech.2014.02.003. Epub 2014 Mar 11.
Due to their unlimited chemical diversity, small molecules can rival monoclonal antibodies (mAbs) with respect to specificity and affinity for target molecules. However, key pharmacological properties of mAbs remain unmatched by small molecules. Chemical programming strategies have been developed for site-specific and covalent conjugation of small molecules to mAbs with unique reactivity centers. In addition to blending favorable features of small molecules and mAbs, chemically programmed antibodies (cpAbs) are economically attractive because they utilize the same mAb for an almost unlimited number of target molecule specificities, reducing manufacturing costs and shortening drug discovery and development time. Preclinical studies and clinical trials have begun to demonstrate the broad utility of cpAbs for the treatment and prevention of human diseases.
由于小分子具有无限的化学多样性，在对靶分子的特异性和亲和力方面，小分子可与单克隆抗体（mAb）相媲美。然而，小分子仍无法匹配mAb的关键药理学特性。已开发出化学编程策略，用于将小分子与具有独特反应中心的mAb进行位点特异性和共价偶联。化学编程抗体（cpAb）除了融合了小分子和mAb的有利特性外，还具有经济吸引力，因为它们可利用相同的mAb针对几乎无限数量的靶分子特异性，从而降低制造成本并缩短药物研发时间。临床前研究和临床试验已开始证明cpAb在治疗和预防人类疾病方面具有广泛的用途。
