期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 6, 期 2, 页码 140-145出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml5003629
关键词
Replication protein A; fragment-based discovery; medicinal chemistry
资金
- NIH [5DP1OD006933/8DP1CA174419, R01CA174887, R01GM065484, P01CA092584, S10 RR025677-01]
- ARRA [5RC2CA148375, F32ES021690, F32CA174315, 5T21CA9582-24]
- Deutscher Akademischer Austausch Dienst (DAAD)
- National Council for Scientific and Technological Development-CNPq
- Federal University of Minas Gerais/Brazil
- NSF [DBI-0922862]
- U.S. DOE [DE-AC02-06CH11357]
- Cancer Research UK [11566] Funding Source: researchfish
Replication Protein A is the primary eukaryotic ssDNA binding protein that has a central role in initiating the cellular response to DNA damage. RPA recruits multiple proteins to sites of DNA damage via the N-terminal domain of the 70 kDa subunit (RPA70N). Here we describe the optimization of a diphenylpyrazole carboxylic acid series of inhibitors of these RPA protein interactions. We evaluated substituents on the aromatic rings as well as the type and geometry of the linkers used to combine fragments, ultimately leading to submicromolar inhibitors of RPA70N protein protein interactions.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据