口服肽类药物的人工合成

Engineered enzymes enable kilogram-scale synthesis of drug for high-cholesterol conditions Rebecca Buller1 and Joelle N. Pelletier2 Biologics are nature-inspired pharmaceutical compounds for treating diseases such as cancer, chronic autoimmune disorders, and high-cholesterol conditions. They are often based on proteins in which amino acids are linked by amide bonds that undergo rapid degradation by digestive enzymes if taken orally. Biologics are therefore primarily administered through intravenous injection. Orally available alternatives can improve patients’ quality of life and adherence to health management. Peptide-based drugs can be chemically modified to withstand degradation and are simpler alternatives to biologics. However, their synthesis often involves many steps and is inefficient (1). On page 643 of this issue, Klapars et al. …