Turku Centre for Biotechnology, University of Turku and Åbo Akademi University, Turku, Finland.
Adv Exp Med Biol. 2019;1148:81-103. doi: 10.1007/978-981-13-7709-9_4.
Enzymes are key biological macromolecules that support life by accelerating the conversion of target molecules to desired products in many biochemical reactions. Enzymes are characterized by high affinity, specificity and great catalytic efficiency. Owing to their unique characteristics, enzymes have attracted significant attention for use in therapeutic settings as a distinct class of drugs different from other types of medicines. Enzyme-based therapies are currently in use for the treatment of a wide range of diseases, including leukemia, metabolic disorders, inflammation and cardiovascular disease. However, several challenges, such as immunogenicity and stability, remain. X-ray crystallography has provided key structural insights into the understanding of the molecular basis of diseases and development of enzyme-based therapies. Here, the role of X-ray crystallography in the development of therapeutic enzymes is examined and several examples are provided.
酶是关键的生物大分子，通过在许多生化反应中加速靶分子向所需产物的转化，支持生命。酶的特点是高亲和力、特异性和高效催化活性。由于其独特的特性，酶作为一种不同于其他类型药物的独特药物类别，在治疗领域引起了广泛关注。基于酶的疗法目前用于治疗广泛的疾病，包括白血病、代谢紊乱、炎症和心血管疾病。然而，仍存在一些挑战，如免疫原性和稳定性。X 射线晶体学为理解疾病的分子基础和开发基于酶的疗法提供了关键的结构见解。在这里，考察了 X 射线晶体学在治疗性酶开发中的作用，并提供了几个例子。
