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Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors
- Source :
- Journal of medicinal chemistry. 58(14)
- Publication Year :
- 2015
-
Abstract
- Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of these effects upon the ATAD2 bromodomain, which has been categorized as among the least tractable of its class. The absence of any potent, selective inhibitors limits clear understanding of the therapeutic potential of the bromodomain. Here, we describe the discovery of a hit from a fragment-based targeted array. Optimization of this produced the first known micromolar inhibitors of the ATAD2 bromodomain.
- Subjects :
- Adenosine Triphosphatases
Models, Molecular
biology
Chemistry
Drug discovery
ATPase
Molecular Sequence Data
Cancer
Antineoplastic Agents
Quinolones
medicine.disease
Bromodomain
Protein Structure, Tertiary
Protein structure
Biochemistry
Disease severity
Drug Discovery
medicine
biology.protein
Cancer research
Molecular Medicine
Humans
Amino Acid Sequence
Enzyme Inhibitors
Peptide sequence
Subjects
Details
- ISSN :
- 15204804
- Volume :
- 58
- Issue :
- 14
- Database :
- OpenAIRE
- Journal :
- Journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....ddb3845b766f600c6cb136aa5e1eb88a