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Publications (27)
CB2 cannabinoid receptors (CB2) are a promising therapeutic target that lacks unwanted side effects of CB1 activation. However, the cell types expressing CB2 that mediate these effects remain poorly understood. We used transgenic mice with CB2 promoter-driven expression of enhanced green fluorescent protein (EGFP) to study cell types that express C...
Cannabinoid 1 receptor (CB1R) allosteric ligands hold far-reaching therapeutic promise. We report application of fluoro- and nitrogen-walk approaches to enhance the drug-like properties of GAT211, a prototype CB1R allosteric agonist-positive allosteric modulator (ago-PAM). Several analogs exhibited improved functional potency (cAMP, arrestin2), me...
AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced neuropathic pain in rodents without producing tolerance or unwanted side effects associated with CB1 receptors; however, the signaling profile of AM1710 remains incompletely characterize...
The CB2 cannabinoid agonist LY2828360 lacked both toxicity and efficacy in a clinical trial for osteoarthritis. Whether LY2828360 suppresses neuropathic pain has not been reported and its signaling profile is unknown. In vitro, LY2828360 was a slowly acting but efficacious G protein-biased CB2 agonist, inhibiting cAMP accumulation and activating ER...
The world is at the precipice of a postantibiotic era in which medical procedures and minor injuries can result in bacterial infections that are no longer effectively treated by antibiotics. Cathelicidins are peptides produced by animals to combat bacterial infections and to regulate innate immune responses. However, cathelicidins are potent activa...
The peptides that are unable to enhance TLR3 and TLR9 signaling are also decreased for association of the FRPL-1 receptor that promotes nucleic acid-peptide endocytosis. (A) Quantification of the reduction in the mRNA levels of three known receptors that interact with LL-37 after siRNA knockdown. BEAS-2B cells were transfected with siRNA at 30 nM f...
Time-lapse flow cell visualization of displacement of V. vulnificus cellular contents into the SMAP-29D-generated lesions. The SMAP-29D peptide covalently labeled with fluorescein is shown in green, and DNA stained with 4′,6-diamidino-2-phenyllindole (DAPI) is shown in blue. Download
Effects of cathelicidins on Toll-like receptor signaling. (A) Nonhuman cathelicidins and their derivatives have reduced enhancement of TLR3 signaling. TLR3 signaling was assessed by quantifying IL-6 levels secreted by BEAS-2B cells using ELISAs. The cells were treated with poly(I⋅C) at 0.13 µg/ml. (B) Nonhuman cathelicidins and their derivatives re...
Effects of cathelicidins on cell proliferation. (A) Effects of a panel of cathelicidins on the proliferation of human lung epithelial BEAS-2B cells. Cell proliferation was assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays (top) and the Wst-1 assays (bottom). All cathelicidins were added to the cells at a fina...
Time-lapse flow cell visualization of bacterial killing of V. vulnificus cells cultured in LB. The SMAP-29D peptide covalently labeled with fluorescein is shown in green, and DNA stained with 4′,6-diamidino-2-phenyllindole (DAPI) is shown in blue. Download
Bactericidal activity of 1 mM SMAP-29D and BMAP-27B on colony formation by several species of bacteria.
Time-lapse flow cell visualization of V. vulnificus cell following influx of ampicillin to a final concentration of 100 µM. The SMAP-29D peptide covalently labeled with fluorescein is shown in green, and DNA stained with 4′,6-diamidino-2-phenyllindole (DAPI) is shown in blue. Download
Time-lapse flow cell visualization of V. vulnificus cell following influx of SMAP-29D to a final concentration of 2 µM. The SMAP-29D peptide covalently labeled with fluorescein is shown in green, and DNA stained with 4′,6-diamidino-2-phenyllindole (DAPI) is shown in blue. Download
Eravacycline is a novel, fully synthetic fluorocycline antibiotic of the tetracycline class being developed for the treatment of complicated urinary tract infections and complicated intra-abdominal infections. Eravacycline has activity against many key Gram-negative pathogens, including Enterobacteriaceae resistant to carbapenems, cephalosporins, f...
Norovirus (NoV) is a positive-sense single-stranded RNA virus that causes acute gastroenteritis and is responsible for 200,000 deaths per year worldwide. No effective vaccines or treatments are available. Recent studies have shown that the nucleoside analogs favipiravir (T-705) and 2’ -
C
-methyl-cytidine (2CM-C) inhibit NoV replication
in vitro
an...
The Hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp), nonstructural protein 5B (NS5B), is anchored in the membrane through a C-terminal helix. A sequence of ca. 12 residues that connects the catalytically competent portion of the RdRp and the C-terminal helix, the juxtamembrane sequence (JMS), has a poorly defined role in RdRp function i...
The replication enzyme of RNA viruses must preferentially recognize their RNAs in an environment that contains an abundance of cellular RNAs. The factors responsible for specific RNA recognition are not well understood, in part because viral RNA synthesis takes place within enzyme complexes associated with modified cellular membrane compartments. R...
Unlabelled:
All members of the Caliciviridae family of viruses produce a subgenomic RNA during infection. The subgenomic RNA typically encodes only the major and minor capsid proteins, but in murine norovirus (MNV), the subgenomic RNA also encodes the VF1 protein, which functions to suppress host innate immune responses. To date, the mechanism of...
A multi-copy and small plasmid pBMB2062 from Bacillus thuringiensis kurstaki YBT-1520 strain was cloned and characterized and its distribution was analyzed using dot-blot analysis with the ORF1 fragment as a probe. Bacillus species of 84 serotypes were evaluated. The pBMB2062 plasmid was found to be present in commercial B. thuringiensis kurstaki (...
Clathrin is a trimeric protein involved in receptor-mediated-endocytosis, but can function as a non-trimer outside of endocytosis. We have discovered that the subcellular distribution of a clathrin cysteine mutant we previously studied is altered and a proportion is also localized to nuclear spaces. MALS shows C1573A hub is a mixture of trimer-like...
HIP1 crystal structures solved in our laboratory revealed abnormalities in the coiled-coil region, suggesting intrinsic plasticity. To test this, specific amino acids in the coiled-coil were mutated. The apparent thermal stability of HIP1 was altered when Thr528 and Glu531 were replaced by leucine, and was enhanced when Lys510 was also mutated. In...
Human telomerase reverse transcriptase (hTERT) represents an attractive target for cancer immunotherapy because hTERT is reactivated in most human tumors. In an attempt to develop an effective vaccine against most human cancers, we constructed chemotactic-hTERT vaccine. Two hTERT fragments encoding multiple cytotoxic T lymphocyte and T helper cell...
Xiaoyan Lin Liu Yi L Peng- [...]
yu Ziniu
A microcalorimetric technique was used to investigate the influence of plasmid copy number and various promoters on the green fluorescent protein expression in Bacillus thuringiensis. The power-time curves of the growth metabolism of B. thuringiensis have been determined by using an LKB-2277 bioactivity monitor at 28 degrees C. For evaluation of th...
A microcalorimetric technique based on the bacterial heat output was applied to evaluate the influence of plasmid copy number and various promoters on the green fluorescent protein expression in Bacillus thuringiensis. The thermogenic curves of the aerobic metabolism of B. thuringiensis strains were determined by using an LKB-2277 bioactivity monit...
A novel microcalorimetric technique based on the bacterial heat output was applied to evaluate the special growth model, the protein expression and the generation time of Bacillus thuringiensis for the first time. The thermogenic curves of the aerobic metabolism of B. thuringiensis strains YBT-833, YBT-1520 and YBT-833-2-1 were determined by using...
A novel microcalorimetric technique based on the bacterial heat output was applied to evaluate the special growth model, the protein expression and the generation time of Bacillus thuringiensis for the first time. The thermogenic curves of the aerobic metabolism of B. thuringiensis strains YBT-833, YBT-1520 and YBT-833-2-1 were determined by using...
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