Abstract
The Hsp70 molecular chaperones are ATPases that play critical roles in the pathogenesis of many human diseases, including breast cancer. Hsp70 ATP hydrolysis is relatively weak but is stimulated by J domain-containing proteins. We identified pyrimidinone-peptoid hybrid molecules that inhibit cell proliferation with greater potency than previously described Hsp70 modulators. In many cases, anti-proliferative activity correlated with inhibition of J domain stimulation of Hsp70.
Original language | English (US) |
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Pages (from-to) | 3291-3301 |
Number of pages | 11 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 16 |
Issue number | 6 |
DOIs | |
State | Published - Mar 15 2008 |
Externally published | Yes |
Keywords
- ATP
- ATPase
- Apoptosis
- Biginelli
- Chaperone
- Dihydropyrimidinone
- Hsp40
- Hsp70
- J domain
- SK-BR-3
- SV40
- T antigen
- Tetrahydropyrimidinone
- Ugi
ASJC Scopus subject areas
- Drug Discovery
- Molecular Medicine
- Molecular Biology
- Biochemistry
- Clinical Biochemistry
- Pharmaceutical Science
- Organic Chemistry