Melissa Hill-Drzewi
Boehringer Ingelheim
14 Papers
251 Citations
Melissa Hill-Drzewi is an academic researcher from Boehringer Ingelheim. The author has contributed to research in topics: Allosteric regulation & Receptor. The author has an hindex of 9, co-authored 14 publications. Previous affiliations of Melissa Hill-Drzewi include Bristol-Myers Squibb.
Chat about Author
Papers
Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.
Alexander Heim-Riether,Steven John Taylor,Shuang Liang,Donghong Amy Gao,Zhaoming Xiong,E. Michael August,Brandon Collins,Bennett T. Farmer,Kathleen Haverty,Melissa Hill-Drzewi,Hans-Dieter Junker,S. Mariana Margarit,Neil Moss,Thomas Neumann,John R. Proudfoot,Lana Louise Smith Keenan,Renate Sekul,Qiang Zhang,Jun Li,Neil A. Farrow +19 more
TL;DR: Discovery and optimization of potency and selectivity of a non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information is reported.
50
Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13
Steven John Taylor,Asitha Abeywardane,Shuang Liang,Ingo Muegge,Anil Kumar Padyana,Zhaoming Xiong,Melissa Hill-Drzewi,Bennett T. Farmer,Xiang Li,Brandon Collins,John Xiang Li,Alexander Heim-Riether,John R. Proudfoot,Qiang Zhang,Daniel E. Goldberg,Ljiljana Zuvela-Jelaska,Hani Zaher,Jun Li,Neil A. Farrow +18 more
TL;DR: The identification of a potent, selective MMP-13 inhibitor is described, developed using fragment-based structure-guided lead identification and optimization techniques, that was >100-fold selective over nine other MMP isoforms tested.
39
SAR studies of non-zinc-chelating MMP-13 inhibitors: Improving selectivity and metabolic stability
Donghong Amy Gao,Zhaoming Xiong,Alexander Heim-Riether,Laura Amodeo,E. Michael August,Xianhua Cao,Leonard Ciccarelli,Brandon Collins,Kyle E. Harrington,Kathleen Haverty,Melissa Hill-Drzewi,Xiang Li,Shuang Liang,Steluta Mariana Margarit,Neil Moss,Nelamangala V. Nagaraja,John R. Proudfoot,Rene Roman,Sabine Schlyer,Lana Louise Smith Keenan,Steven John Taylor,Bernd Wellenzohn,Dieter Wiedenmayer,Jun Li,Neil A. Farrow +24 more
TL;DR: Improved selectivity was achieved by modifying interactions with the S1' pocket and metabolic stability was improved through reduction of inhibitor lipophilicity, which translated into lower in vivo clearance for the preferred compound.
33
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.
Scott A. Mitchell,Mihaela Diana Danca,Peter Blomgren,James W. Darrow,Kevin S. Currie,Kropf Jeffrey E,Seung H. Lee,Steven L. Gallion,Jin-Ming Xiong,Douglas A. Pippin,Robert Desimone,David R. Brittelli,David C. Eustice,Aaron Bourret,Melissa Hill-Drzewi,Patricia Maciejewski,Lisa Elkin +16 more
TL;DR: A novel series of imidazo[1,2-a]pyrazine diarylureas that show nanomolar potency for the EphB4 receptor, in addition to potent activity against several other RTKs are reported.
32
Discovery of Potent, Selective Chymase Inhibitors via Fragment Linking Strategies
Steven John Taylor,Anil Kumar Padyana,Asitha Abeywardane,Shuang Liang,Ming-Hong Hao,Stéphane De Lombaert,John R. Proudfoot,Bennett Sandy Farmer,Xiang Li,Brandon Collins,Leslie Martin,Daniel R. Albaugh,Melissa Hill-Drzewi,Steven S. Pullen,Hidenori Takahashi +14 more
TL;DR: This work describes the identification of potent, selective chymase inhibitors, developed using fragment-based, structure-guided linking and optimization techniques, and mitigated a number of liabilities associated with poor physicochemical properties of the series it was derived from.
31