Biphenyls as potential mimetics of protein alpha-helix.
Based on theoretical arguments, 2,6,3',5'-substituted biphenyl analogues are proposed as protein alpha-helix mimetics superimposing the side chains of the residues i, i+1, i+3 and i+4. Knowing that many protein-protein interactions of therapeutical relevance involve alpha-helix contacts, the communication outlines how this novel category of scaffolds might potentially open access to such targets.
Jacoby
Edgar
E
Novartis Pharma AG, Combinatorial Chemistry Unit, WSJ-507.7.53, CH-4002, Basel, Switzerland. edgar.jacoby@pharma.novartis.com
D000818:Animals; D001713:Biphenyl Compounds / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D018716:Molecular Mimicry; D017433:Protein Structure, Secondary; D011506:Proteins / Q000737:chemistry*
D001713:Biphenyl Compounds; D011506:Proteins