Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Editor

Personal info

View

About

Terms

Javascript disabled

Please enable Javascript support in your browser to use this application.

Instructions on how to enable JavaScript on different browsers can be found here: http://www.google.com/support/bin/answer.py?answer=23852.

[edit this page]

Shin, B.S. et al.

In vitro investigation of the hepatic intrinsic clearance of apicidin, a histone deacetylase inhibitor, in mouse, rat, and human, with correction by nonspecific protein binding.

Apicidin is a potent histone deacetylase inhibitor exhibiting broad-spectrum antiprotozoal, antiproliferative, and antiangiogenic activities. This study was conducted to calculate the intrinsic hepatic clearance of apicidin in mouse, rat, and human. The microsomal stability was determined in pooled microsomes of mouse, rat, and human. The V(max) and K(m) were 680.4 ng/min/ mg protein and 10,544.1 ng/ml for mouse, 745.0 ng/min/ mg protein and 24,306.0 ng/ml for rat, and 927.0 ng/min/ mg protein and 62,906.0 ng/ml for human, respectively. The f(u,plasma) was extremely low, 0.369 +/- 0.034% for mouse, 0.376 +/- 0.059% rat, and 1.042 +/- 0.114% human. The unbound fraction of apicidin in microsomes (f(u,mic)) was also low, 1.731 +/- 0.237% for mouse, 0.767 +/- 0.048% for rat, and 5.751 +/- 1.575% for human. The hepatic intrinsic clearance calculated by Michaelis kinetics was further corrected by nonspecific binding to microsomal proteins. The corrected intrinsic clearance of apicidin was 1.9, 8.6, and 284.2 ml/min for mouse, rat, and human, respectively. The allometric correlation was improved when the hepatic intrinsic clearance was corrected by the nonspecific protein binding.[1]

References

In vitro investigation of the hepatic intrinsic clearance of apicidin, a histone deacetylase inhibitor, in mouse, rat, and human, with correction by nonspecific protein binding. Shin, B.S., Park, E.H., Yoon, C.H., Kim, J., Zee, O., Yoo, S.D. J. Toxicol. Environ. Health Part A (2005) [Pubmed]

Annotations and hyperlinks in this abstract are from individual authors of WikiGenes or automatically generated by the WikiGenes Data Mining Engine. The abstract is from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.About WikiGenes Open Access Licence Privacy Policy Terms of Use apsburg

The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.