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Proteolytic Activity of Human Osteoclast Cathepsin K
TLDR
Cathepsin K may represent the elusive protease implicated in degradation of protein matrix during bone resorption and represents a novel molecular target in treatment of disease states associated with excessive bone loss such as osteoporosis. Expand
DESIGN, SYNTHESIS, AND KINETIC EVALUATION OF HIGH-AFFINITY FKBP LIGANDS AND THE X-RAY CRYSTAL-STRUCTURES OF THEIR COMPLEXES WITH FKBP12.
The design and synthesis of high-affinity FKBP12 ligands is described. These compounds potently inhibit the cis-trans-peptidylprolyl isomerase (rotamase) activity catalyzed by FKBP12 with inhibitionExpand
Dietary zinc alters early inflammatory responses during cutaneous wound healing in weanling CD-1 mice.
TLDR
It is demonstrated that zinc deficiency and high-dose zinc supplementation delay wound healing as a result of altered inflammatory responses and suggested that adequate zinc supplementation may have beneficial effects on the inflammatory responses to enhance cutaneous wound healing. Expand
Rapamycin sensitivity in Saccharomyces cerevisiae is mediated by a peptidyl-prolyl cis-trans isomerase related to human FK506-binding protein.
TLDR
The resonse to rapamycin in yeast cells is mediated by a gene encoding a 114-amino-acid, approximately 13-kDa protein which has a high degree of sequence homology with human FKBP, indicating a functional equivalence between the yeast and human enzymes. Expand
Protection by dietary zinc in ALS mutant G93A SOD transgenic mice
TLDR
A role for moderate levels of dietary zinc potentially protecting against the toxicity of ALS-associated SOD and the protection does not result from depleting copper. Expand
Preclinical pharmacokinetics of SB-203580, a potent inhibitor of p38 mitogen-activated protein kinase
TLDR
Interspecies differences in bioavailability, and the non-linear pharmacokinetics observed in rat, highlight the importance of monitoring SB-203580 systemic exposure in parallel with the pharmacological endpoint during in vivo pharmacology studies. Expand
Predictors of vitamin D status in subjects that consume a vitamin D supplement
TLDR
Vitamin D supplementation was the most significant positive predictor of vitamin D status and these data point to the practicality of utilizing vitamin D supplements to reduce hypovitaminosis D in adults throughout the United States. Expand
Potent and selective nonpeptide inhibitors of caspases 3 and 7.
5-Dialkylaminosulfonylisatins have been identified as potent, nonpeptide inhibitors of caspases 3 and 7. The most active compound within this series (34) inhibited caspases 3 and 7 in the 2-6 nMExpand
Development of an in vivo preclinical screen model to estimate absorption and bioavailability of xenobiotics.
TLDR
The aim of this study was to develop an in vivo screening method for rapid preclinical characterization of absorption and bioavailability of large numbers of compounds using a single intraduodenal dose in a preclinical model. Expand
Metabolism and Disposition of Eltrombopag, an Oral, Nonpeptide Thrombopoietin Receptor Agonist, in Healthy Human Subjects
The metabolism and disposition of eltrombopag, the first-in-class small molecule human thrombopoietin receptor agonist, were studied in six healthy men after a single oral administration of aExpand
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