Haifeng Cui
GlaxoSmithKline
7 Papers
Haifeng Cui is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: DNA gyrase & Biology. The author has an hindex of 6, co-authored 6 publications.
Chat about Author
Papers
Tunneling Nanotubes and Gap Junctions-Their Role in Long-Range Intercellular Communication during Development, Health, and Disease Conditions.
Jennifer L. Ariazi,Andrew B. Benowitz,Vern de Biasi,Monique L. den Boer,Stephanie Cherqui,Haifeng Cui,Nathalie Douillet,Eliseo A. Eugenin,Eliseo A. Eugenin,David Favre,Spencer Goodman,Karine Gousset,Dorit Hanein,David I. Israel,Shunsuke Kimura,Robert B. Kirkpatrick,Nastaran Z. Kuhn,Claire G. Jeong,Emil Lou,Robbie B. Mailliard,Stephen Maio,George Okafo,Matthias Osswald,Matthias Osswald,Jennifer Pasquier,Roel Polak,Gabriele Pradel,Bob de Rooij,Peter Schaeffer,Vytenis Arvydas Skeberdis,Ian F. Smith,Ahmad Tanveer,Niels Volkmann,Zhenhua Wu,Chiara Zurzolo +34 more
TL;DR: The combined data from numerous laboratories indicate that some TNT mediate a long-range gap junctional communication to coordinate metabolism and signaling, in relation to infectious, genetic, metabolic, cancer, and age-related diseases.
Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors.
Krista B. Goodman,Haifeng Cui,Sarah E. Dowdell,Dimitri E. Gaitanopoulos,Robert L. Ivy,Clark A. Sehon,Robert A. Stavenger,Gren Z. Wang,Andrew Q. Viet,Weiwei Xu,Guosen Ye,Simon Semus,Christopher P. Evans,Harvey E. Fries,Larry J. Jolivette,Robert B. Kirkpatrick,Edward Dul,Sanjay S. Khandekar,Tracey Yi,David Kendallc Jung,Lois L Wright,Gary K Smith,David J. Behm,Ross Bentley,Christopher P. Doe,Erding Hu,Dennis Lee +26 more
TL;DR: Indazole substitution played a critical role in decreasing clearance and improving oral bioavailability and a series of dihydropyridones were discovered, exemplified by 13, with improved pharmacokinetic parameters relative to the initial lead.
158
Structural basis of DNA gyrase inhibition by antibacterial QPT-1, anticancer drug etoposide and moxifloxacin.
Pan F. Chan,Velupillai Srikannathasan,Jianzhong Huang,Haifeng Cui,Andrew P. Fosberry,Minghua Gu,Michael M. Hann,Martin Hibbs,Paul Homes,Karen A. Ingraham,Jason Pizzollo,Carol Shen,Anthony Shillings,Claus Spitzfaden,Robert Tanner,Andrew J. Theobald,Robert A. Stavenger,Benjamin D. Bax,Michael N. Gwynn +18 more
TL;DR: The first co-crystal structures of the antibacterial QPT-1 and the anticancer drug etoposide with Staphylococcus aureus DNA gyrase are reported, showing binding at the same sites in the cleaved DNA as the fluoroquinolone moxifloxacin.
129
Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase
Pan F. Chan,Thomas Germe,Benjamin D. Bax,Jianzhong Huang,Reema K. Thalji,Eric Bacqué,Anna Checchia,Dongzhao Chen,Haifeng Cui,Xiao Ding,Karen A. Ingraham,Lynn McCloskey,Kaushik Raha,Velupillai Srikannathasan,Anthony Maxwell,Robert A. Stavenger +15 more
TL;DR: A class of antibacterial thiophenes that target DNA gyrase with a unique mechanism of action and have activity against a range of bacterial pathogens, including strains resistant to fluoroquinolones are identified.
75
Fragment-Based Discovery of 6-Azaindazoles As Inhibitors of Bacterial DNA Ligase
Steven Howard,Nader Amin,Andrew B. Benowitz,Elisabetta Chiarparin,Haifeng Cui,Xiaodong Deng,Tom D. Heightman,David J. Holmes,Anna Hopkins,Jianzhong Huang,Qi Jin,Constantine Kreatsoulas,Agnes C. L. Martin,Frances Massey,Lynn McCloskey,Paul N. Mortenson,Puja Pathuri,Dominic Tisi,Pamela A. Williams +18 more
TL;DR: X-ray crystallography was used to guide structure-based optimization of a fragment-screening hit to give novel, nanomolar, AMP-competitive inhibitors to bacterial DNA ligase, showing antibacterial activity across a range of pathogens.
23