Biomedical subjects

Xiaodong Fan

Publications and source records attributed to Xiaodong Fan.

4 recordsLinked to original sources

PubMed2006

Synthesis of poly(ethylene glycol)-metaxalone conjugates and study of its controlled release in vitro.

Metaxalone (Met), a drug for treatment of pain and stiffness due to muscular injuries, was covalently linked to poly(ethylene glycols) (PEG) via a chloroacetyl chloride spacer. The average weight molecular weights used for PEG are 4000, 6000 and 10,000, respectively, and the procedure of chemical modification for PEGs was conducted by a two-step protocol: (1) synthesis of N-chloroacetyl-metaxalone; (2) synthesis of PEG(4000)-Met, PEG(6000)-Met and PEG(10000)-Met. The controlled drug release studies were performed in buffer solutions with pH values equal to 1.1, 7.4 and 10.0. The results demonstrate that, in the same condition, the rate of hydrolysis for PEG(10000)-Met is the slowest among three prodrugs, and more amount of metaxalone can be detected releasing from prodrug matrices at the presence of alpha-chymotrypsin in a buffer solution with pH 8.0. It was also found that these novel prodrugs can effectively improve the metaxalone's pharmacokinetics, and furthermore can markedly increase its half-life period.

Acetates↗

PubMed2006

Inhibitors of unactivated p38 MAP kinase.

Inhibition of the p38 map kinase pathway has been shown to be beneficial in the treatment of inflammatory diseases. The first class of potent p38 kinase inhibitors was the pyridinylimidazole compounds from SKB. Since then several pyridinylimidazole-based compounds have been shown to inhibit activated p38 kinase in vitro and in vivo. We have developed a novel series of pyridinylimidazole-based compounds, which potently inhibit the p38 pathway by binding to unactivated p38 kinase and only weakly inhibiting activated p38 kinase activity in vitro.

Animals↗

PubMed2006

Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors.

A series of novel carboxylic acid-based alpha-sulfone MMP inhibitors have been synthesized and the in vitro enzyme SAR is discussed. A potential binding mode in the active site of the MMP-9 homology model was highlighted. These compounds are potent MMP-9 inhibitors and are selective over MMP-1.

Animals↗

PubMed2004

A coarse-to-fine strategy for multiclass shape detection.

Multiclass shape detection, in the sense of recognizing and localizing instances from multiple shape classes, is formulated as a two-step process in which local indexing primes global interpretation. During indexing a list of instantiations (shape identities and poses) is compiled, constrained only by no missed detections at the expense of false positives. Global information, such as expected relationships among poses, is incorporated afterward to remove ambiguities. This division is motivated by computational efficiency. In addition, indexing itself is organized as a coarse-to-fine search simultaneously in class and pose. This search can be interpreted as successive approximations to likelihood ratio tests arising from a simple ("naive Bayes") statistical model for the edge maps extracted from the original images. The key to constructing efficient "hypothesis tests" for multiple classes and poses is local ORing; in particular, spread edges provide imprecise but common and locally invariant features. Natural tradeoffs then emerge between discrimination and the pattern of spreading. These are analyzed mathematically within the model-based framework and the whole procedure is illustrated by experiments in reading license plates.

Journal Article↗