Kumar Vajinder, Turnbull W Bruce
Department of Chemistry, Akal University, Talwandi Sabo, Punjab, India.
School of Chemistry and Astbury Centre for Structural Molecular Biology, University of Leeds, LS2 9JT, UK.
Beilstein J Org Chem. 2018 Feb 21;14:484-498. doi: 10.3762/bjoc.14.34. eCollection 2018.
Cholera is a diarrheal disease caused by a protein toxin released by in the host's intestine. The toxin enters intestinal epithelial cells after binding to specific carbohydrates on the cell surface. Over recent years, considerable effort has been invested in developing inhibitors of toxin adhesion that mimic the carbohydrate ligand, with particular emphasis on exploiting the multivalency of the toxin to enhance activity. In this review we introduce the structural features of the toxin that have guided the design of diverse inhibitors and summarise recent developments in the field.
霍乱是一种由霍乱弧菌在宿主肠道内释放的蛋白质毒素引起的腹泻疾病。该毒素在与细胞表面的特定碳水化合物结合后进入肠道上皮细胞。近年来,人们投入了大量精力来开发模仿碳水化合物配体的毒素黏附抑制剂,尤其注重利用毒素的多价性来增强活性。在这篇综述中,我们介绍了指导多种抑制剂设计的毒素结构特征,并总结了该领域的最新进展。