Cover Picture: Conjugation to Albumin‐Binding Molecule Tags as a Strategy to Improve Both Efficacy and Pharmacokinetic Properties of the Complement Inhibitor Compstatin (ChemMedChem 10/2014). Issue 10 (October 2014)

• Record Type: Journal Article
• Authors: Huang, Yijun; Reis, Edimara S.; Knerr, Patrick J.; van der Donk, Wilfred A.; Ricklin, Daniel; Lambris, John D.
• Is Part Of: ChemMedChem. Volume 9:Issue 10(2014:Oct.)
• Page Start: 2209
• Page End: 2209
• Publication Date: 2014-10
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201490037
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>The front cover picture shows</bold> the chimeric peptide ABM2‐Cp20, a derivative of the complement inhibitor compstatin, simultaneously binding to albumin (pink) and complement C3 (teal). Compstatin has shown promise in the treatment of immuno‐inflammatory disorders; however, optimization of its pharmacokinetic properties would extend long‐term systemic applications. The addition of a small albumin‐binding molecule tag to the compstatin peptide improves plasma protein binding yet also largely enhances target affinity, thereby preventing convertase (teal/green)‐mediated C3 activation, opsonization and cell damage (flash arrow) more efficiently. For more details, see the Communication by Daniel Ricklin, John D. Lambris et al. on <ext-link ext-link-type="doi" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">p. 2223 ff.</ext-link><boxed-text content-type="graphic" position="anchor" orientation="portrait"><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgh1f8xwpvp" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></boxed-text></p> </abstract>