دورية أكاديمية

Rational Design of Anticytoadherence Inhibitors for Plasmodium falciparum Based on the Crystal Structure of Human Intercellular Adhesion Molecule 1

التفاصيل البيبلوغرافية
العنوان: Rational Design of Anticytoadherence Inhibitors for Plasmodium falciparum Based on the Crystal Structure of Human Intercellular Adhesion Molecule 1
المؤلفون: Dormeyer, Matthias, Adams, Yvonne, Kramer, Bernd, Chakravorty, Srabasti, Tse, Man Tsuey, Pegoraro, Stefano, Whittaker, Lisa, Lanzer, Michael, Craig, Alister
المصدر: Antimicrobial Agents and Chemotherapy ; volume 50, issue 2, page 724-730 ; ISSN 0066-4804 1098-6596
بيانات النشر: American Society for Microbiology
سنة النشر: 2006
الوصف: Adhesion of Plasmodium falciparum -infected erythrocytes (IE) to host endothelium has been associated with pathology in malaria. Although the interaction with endothelial cells can be complex due to the relatively large number of host receptors available for binding, specific proteins have been identified that are more commonly used than others. For example, binding to intercellular adhesion molecule 1 (ICAM 1) is found frequently in parasites from pediatric cases of malaria. The binding site for P. falciparum -infected erythrocytes on ICAM 1 has been mapped in some detail and is distinct from the site for lymphocyte function-associated antigen 1 (LFA-1). Part of the ICAM 1 binding site for P. falciparum -infected erythrocytes (the DE loop) was used to screen a library of compounds based on its structure (derived from the crystal structure of human ICAM 1). This resulted in the identification of 36 structural mimeotopes as potential competitive inhibitors of binding. One of these compounds, (+)-epigalloyl-catechin-gallate [(+)-EGCG], was found to inhibit IE adhesion to ICAM 1 in a dose-dependent manner with two variant ICAM 1-binding parasite lines, providing the first example of a potential mimeotope-based anticytoadherence inhibitor for Plasmodium falciparum .
نوع الوثيقة: article in journal/newspaper
اللغة: English
DOI: 10.1128/aac.50.2.724-730.2006
DOI: 10.1128/AAC.50.2.724-730.2006
الإتاحة: https://doi.org/10.1128/aac.50.2.724-730.2006Test
حقوق: https://journals.asm.org/non-commercial-tdm-licenseTest
رقم الانضمام: edsbas.FE48C25A
قاعدة البيانات: BASE