• Publications
  • Influence
Molecular basis for inhibition of AcrB multidrug efflux pump by novel and powerful pyranopyridine derivatives
TLDR
The molecular basis for pyranopyridine-based inhibition of AcrB is described using a combination of cellular, X-ray crystallographic, and molecular dynamics simulations studies and provides a molecular platform for the development of novel combinational therapies using efflux pump inhibitors for combating multidrug resistant Gram-negative pathogens.
Mutations in the Pseudomonas aeruginosa Needle Protein Gene pscF Confer Resistance to Phenoxyacetamide Inhibitors of the Type III Secretion System
TLDR
The results implicate the PscF needle protein as an apparent new molecular target for T3 SS inhibitor discovery and suggest that three other chemically distinct T3SS inhibitors interact with one or more different targets or a different region of Pscf.
Respiratory syncytial virus-induced chemokine production: linking viral replication to chemokine production in vitro and in vivo.
TLDR
It is suggested that viral replication is necessary for optimal chemokine production in RSV-infected airway epithelial cells and alveolar macrophages.
Characterization of a Novel Pyranopyridine Inhibitor of the AcrAB Efflux Pump of Escherichia coli
TLDR
MBX2319 is a potent EPI with possible utility as an adjunctive therapeutic agent for the treatment of infections caused by Gram-negative pathogens and was broadly active against Enterobacteriaceae species and Pseudomonas aeruginosa.
Identification of a Small-Molecule Entry Inhibitor for Filoviruses
TLDR
It is hypothesized that compound 7 binds to this hydrophobic pocket at or near the GP1 and GP2 interface and as a consequence inhibits EBOV infection of cells, but the details of the mechanism remain to be determined.
A new cytokine-receptor binding mode revealed by the crystal structure of the IL-1 receptor with an antagonist
TLDR
The crystal structure at 2.7 Å resolution of the soluble extracellular part of type-I IL1R complexed with IL1RA is described, which consists of three immunoglobulin-like domains and a region that is important for biological function in IL-1β, the 'receptor trigger site', is not in direct contact with the receptor in theIL1RA complex.
Patterns of expression of tumor necrosis factor alpha, tumor necrosis factor beta, and their receptors in synovia of patients with juvenile rheumatoid arthritis and juvenile spondylarthropathy.
TLDR
JRA and JSpA synovia are characterized by the presence of TNF alpha, TNF beta, and cells expressing TNFR, providing further evidence that TNF, through autocrine/paracrine mechanisms, may amplify local inflammation, leading to joint destruction.
Discovery and Characterization of Inhibitors of Pseudomonas aeruginosa Type III Secretion
TLDR
Five inhibitors in three chemical classes were demonstrated to inhibit type III secretion selectively with minimal cytotoxicity and with no effects on bacterial growth or on the type II-mediated secretion of elastase.
Selective inhibition of T cell activation by an inhibitor of S-adenosyl-L-homocysteine hydrolase.
TLDR
It is demonstrated that MDL 28,842 is a potent nontoxic immunosuppressive agent, which has selectivity for T cells and therefore may be useful in the treatment of T cell-mediated disorders, such as autoimmune disease and tissue transplantation.
Immunomodulation by an inhibitor of S-adenosyl-L-homocysteine hydrolase: inhibition of in vitro and in vivo allogeneic responses.
TLDR
It is suggested that MDL 28,842 is useful in the prevention of allograft rejection and in vitro and in vivo models of transplant rejection.
...
1
2
3
4
5
...