Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: Intelligent design and evolution …

…, T Wang, Y Wei, H Zhang, D Stamos - Journal of Medicinal …, 2008 - ACS Publications
The discovery of new antibacterial agents with novel mechanisms of action is necessary to
overcome the problem of bacterial resistance that affects all currently used classes of …

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

…, M Dabros, C Zhao, RJ Cherney, P Carter, D Stamos… - Nature, 2016 - nature.com
CC chemokine receptor 2 (CCR2) is one of 19 members of the chemokine receptor
subfamily of human class A G-protein-coupled receptors. CCR2 is expressed on monocytes, …

DCAF11 supports targeted protein degradation by electrophilic proteolysis-targeting chimeras

…, LG Bauer, MM Dix, D Stamos… - Journal of the …, 2021 - ACS Publications
Ligand-induced protein degradation has emerged as a compelling approach to promote the
targeted elimination of proteins from cells by directing these proteins to the ubiquitin-…

A mild preparation of vinyliodides from vinylsilanes

DP Stamos, AG Taylor, Y Kishi - Tetrahedron letters, 1996 - Elsevier
OTBS OTBS [..~O NIS, rt ~ O MeON/OIOH2ON " MeO2CI~o ~"~"~OTBS 80% yield OTBS Page 1
Pergamon Tetrahedron Letters, Vol. 37, No. 48, pp. 8647-8650, 1996 Copyright © 1996 Elsevier …

Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase

…, TH Grossman, N Mani, JD Parsons, D Stamos… - Bioorganic & Medicinal …, 2010 - Elsevier
Bacterial DNA gyrase is an attractive target for the investigation of new antibacterial agents.
Inhibitors of the GyrB subunit, which contains the ATP-binding site, are described in this …

Dual targeting of GyrB and ParE by a novel aminobenzimidazole class of antibacterial compounds

…, JD Parsons, Y Liao, AL Grillot, D Stamos… - Antimicrobial agents …, 2007 - Am Soc Microbiol
A structure-guided drug design approach was used to optimize a novel series of
aminobenzimidazoles that inhibit the essential ATPase activities of bacterial DNA gyrase and …

[HTML][HTML] A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy

…, MJ Kröner, DJ van der Berg, D Stamos… - Scientific reports, 2017 - nature.com
CC Chemokine Receptor 2 (CCR2) and its endogenous ligand CCL2 are involved in a number
of diseases, including atherosclerosis. Several CCR2 antagonists have been developed …

Identification of novel HSP90α/β isoform selective inhibitors using structure-based drug design. Demonstration of potential utility in treating CNS disorders such as …

…, J Reynolds, K Alvi, L Goulet, D Stamos - Journal of medicinal …, 2014 - ACS Publications
A structure-based drug design strategy was used to optimize a novel benzolactam series of
HSP90α/β inhibitors to achieve >1000-fold selectivity versus the HSP90 endoplasmic …

In vitro characterization of the antibacterial spectrum of novel bacterial type II topoisomerase inhibitors of the aminobenzimidazole class

…, S Mullin, Y Liao, AL Grillot, D Stamos… - Antimicrobial agents …, 2006 - Am Soc Microbiol
Antibiotics with novel mechanisms of action are becoming increasingly important in the
battle against bacterial resistance to all currently used classes of antibiotics. Bacterial DNA …

Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity—Implications for the structure-based design of HSP90α/β …

…, A Turnbull, A Kallel, B Vought, D Stamos - Bioorganic & medicinal …, 2014 - Elsevier
HSP90 continues to be a target of interest for neurodegeneration indications. Selective
knockdown of the HSP90 cytosolic isoforms α and β is sufficient to reduce mutant huntingtin …