title: Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors.
abstract: The STAT3 oncogene is a promising molecular target for the design of a new class of anticancer drugs. In this letter, we describe the design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as novel STAT3 inhibitors. Compound 3 binds to STAT3 with a K(i) value of 190nM and is a promising lead compound for further design and optimization.
authors.affiliation: Cancer Center, University of Michigan, Ann Arbor, MI 48109, USA.
authors.forename: Cindy
authors.initials: C
authors.lastname: Gomez
authors.forename: Longchuan
authors.initials: L
authors.lastname: Bai
authors.forename: Jian
authors.initials: J
authors.lastname: Zhang
authors.forename: Zaneta
authors.initials: Z
authors.lastname: Nikolovska-Coleska
authors.forename: Jianyong
authors.initials: J
authors.lastname: Chen
authors.forename: Han
authors.initials: H
authors.lastname: Yi
authors.forename: Shaomeng
authors.initials: S
authors.lastname: Wang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D032701:Biomimetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007700:Kinetics; D007769:Lactams / Q000138:chemical synthesis* / Q000494:pharmacology; D008956:Models, Chemical; D015394:Molecular Structure; D010748:Phosphopeptides / Q000737:chemistry; D010766:Phosphorylation; D011487:Protein Conformation; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007769:Lactams; D010748:Phosphopeptides; D050796:STAT3 Transcription Factor