title: Design of libraries targeting protein-protein interfaces.
abstract: TARGETING PPIS: A novel strategy for designing libraries targeting protein-protein interfaces enabled us to identify diverse chemical entry points to interact with therapeutic targets for which conventional screening libraries delivered no or only few hit structures. The concept was experimentally validated by early hit evaluation in biochemical screens and early ADMET profiling.
authors: Discovery Technologies & Discovery Chemistry, F Hoffmann-La Roche Inc. 340 Kingsland St., Nutley, NJ 07110, USA.
authors: David
authors: D
authors: Fry
authors: Kuo-Sen
authors: KS
authors: Huang
authors: Paola
authors: P
authors: Di Lello
authors: Peter
authors: P
authors: Mohr
authors: Klaus
authors: K
authors: Müller
authors: Sung-Sau
authors: SS
authors: So
authors: Takeo
authors: T
authors: Harada
authors: Martin
authors: M
authors: Stahl
authors: Binh
authors: B
authors: Vu
authors: Harald
authors: H
authors: Mauser
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding / Q000187:drug effects; D054730:Protein Interaction Domains and Motifs / Q000187:drug effects*; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D051736:Proto-Oncogene Proteins c-mdm2 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D012015:Reference Standards; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility; D013329:Structure-Activity Relationship; D016159:Tumor Suppressor Protein p53 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
chemical_list: D019253:Proto-Oncogene Proteins c-bcl-2; D054852:Small Molecule Libraries; D016159:Tumor Suppressor Protein p53; C497206:MDM2 protein, human; D051736:Proto-Oncogene Proteins c-mdm2