Novobiocin: redesigning a DNA gyrase inhibitor for selective inhibition of hsp90
JA Burlison, L Neckers, AB Smith… - Journal of the …, 2006 - ACS Publications
Novobiocin is a member of the coumermycin family of antibiotics and is a well-established
inhibitor of DNA gyrase. Recent studies have shown that novobiocin binds to a previously …
inhibitor of DNA gyrase. Recent studies have shown that novobiocin binds to a previously …
Development of novobiocin analogues that manifest anti-proliferative activity against several cancer cell lines
JA Burlison, C Avila, G Vielhauer… - The Journal of …, 2008 - ACS Publications
Recent studies have shown that the DNA gyrase inhibitor, novobiocin, binds to a previously
unrecognized ATP-binding site located at the C-terminus of Hsp90 and induces degradation …
unrecognized ATP-binding site located at the C-terminus of Hsp90 and induces degradation …
The design, synthesis, and evaluation of coumarin ring derivatives of the novobiocin scaffold that exhibit antiproliferative activity
AC Donnelly, JR Mays, JA Burlison… - The Journal of …, 2008 - ACS Publications
Novobiocin, a known DNA gyrase inhibitor, binds to a nucleotide-binding site located on the
Hsp90 C-terminus and induces degradation of Hsp90-dependent client proteins at∼ 700 …
Hsp90 C-terminus and induces degradation of Hsp90-dependent client proteins at∼ 700 …
Novobiocin and additional inhibitors of the Hsp90 C-terminal nucleotide-binding pocket
A Donnelly, BSJ Blagg - Current medicinal chemistry, 2008 - ingentaconnect.com
The 90 kDa heat shock proteins (Hsp90), which are integrally involved in cell signaling,
proliferation, and survival, are ubiquitously expressed in cells. Many proteins in tumor cells …
proliferation, and survival, are ubiquitously expressed in cells. Many proteins in tumor cells …
Synthesis and evaluation of coumermycin A1 analogues that inhibit the Hsp90 protein folding machinery
JA Burlison, BSJ Blagg - Organic letters, 2006 - ACS Publications
The coumarin antibiotics are not only potent inhibitors of DNA gyrase but also represent the
most effective C-terminal inhibitors of 90 kDa heat shock proteins (Hsp90) reported thus far …
most effective C-terminal inhibitors of 90 kDa heat shock proteins (Hsp90) reported thus far …
Engineering an antibiotic to fight cancer: optimization of the novobiocin scaffold to produce anti-proliferative agents
H Zhao, AC Donnelly, BR Kusuma… - Journal of medicinal …, 2011 - ACS Publications
Development of the DNA gyrase inhibitor, novobiocin, into a selective Hsp90 inhibitor was
accomplished through structural modifications to the amide side chain, coumarin ring, and …
accomplished through structural modifications to the amide side chain, coumarin ring, and …
Targeting the heat shock protein 90 dimer with dimeric inhibitors
BR Kusuma, LB Peterson, H Zhao… - Journal of medicinal …, 2011 - ACS Publications
The design, synthesis, and biological evaluation of conformationally constrained
coumermycin A1 analogues are reported. Compounds were evaluated against both breast …
coumermycin A1 analogues are reported. Compounds were evaluated against both breast …
Posttranslational modifications in microcin B17 define an additional class of DNA gyrase inhibitor.
P Yorgey, J Lee, J Kördel, E Vivas… - Proceedings of the …, 1994 - National Acad Sciences
Drugs that inhibit the activity of DNA gyrase fall almost exclusively into two structural classes,
the quinolones and the coumarins. A third class of DNA gyrase inhibitor is defined by the …
the quinolones and the coumarins. A third class of DNA gyrase inhibitor is defined by the …
Hsp90 inhibitors identified from a library of novobiocin analogues
XM Yu, G Shen, L Neckers, H Blake… - Journal of the …, 2005 - ACS Publications
Novobiocin is a C-terminal inhibitor of the Hsp90 protein folding machinery, which is
responsible for the conformational maturation of numerous proteins involved in cancer …
responsible for the conformational maturation of numerous proteins involved in cancer …
Simocyclinone D8, an inhibitor of DNA gyrase with a novel mode of action
RH Flatman, AJ Howells, L Heide… - Antimicrobial agents …, 2005 - Am Soc Microbiol
We have characterized the interaction of a new class of antibiotics, simocyclinones, with
bacterial DNA gyrase. Even though their structures include an aminocoumarin moiety, a key …
bacterial DNA gyrase. Even though their structures include an aminocoumarin moiety, a key …