Fragment‐Based Design of Ligands Targeting a Novel Site on the Integrase Enzyme of Human Immunodeficiency Virus 1

Abstract

Every little bit counts! Fragment-based screening has been used to identify a novel ligand binding site on HIV-1 integrase. Crystal structures of fragments bound at this site (shown) have been used to design elaborated second- generation compounds that bind with higher affinity and good ligand efficiency. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.