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]

Chemical Compound Review:

CHEMBL502330 quinoline-8-carboxamide

Synonyms: SureCN460456, CCRIS 6967, AG-F-95033, CHEBI:573936, CTK5A4047, ...

Marquis, R.W. et al., Papageorgiou, C. et al.

Papageorgiou, von Matt, Joergensen, Andersen, Wagner, Beerli, Than, Borer, Florineth, Rihs, Schreier, Weckbecker, Heusser, Marquis, James, Zeng, Trout, Thompson, Rahman, Yamashita, Xie, Ru, Gress, Blake, Lark, Hwang, Tomaszek, Offen, Head, Cummings, Veber,

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

High impact information on quinoline-8-carboxamide

Structure-activity studies examining the effect of inhibitor selectivity as a function of the P3 and P2 binding elements of the potent cathepsin K inhibitor 1 revealed that incorporation of either a P3 quinoline-8-carboxamide or a naphthylene-1-carboxamide led to increased selectivity for cathepsin L over cathepsin K [1].
By capitalizing on the target enzyme-bound (DHODH) structure 1b of one of these compounds, leflunomide, and modulating part of its multiple mechanisms of action to gain selectivity, the quinoline-8-carboxamide 3 was designed as a potentially weak enzyme inhibitor but effective immunosuppressant [2].

References

Azepanone-based inhibitors of human cathepsin L. Marquis, R.W., James, I., Zeng, J., Trout, R.E., Thompson, S., Rahman, A., Yamashita, D.S., Xie, R., Ru, Y., Gress, C.J., Blake, S., Lark, M.A., Hwang, S.M., Tomaszek, T., Offen, P., Head, M.S., Cummings, M.D., Veber, D.F. J. Med. Chem. (2005) [Pubmed]
Aromatic quinolinecarboxamides as selective, orally active antibody production inhibitors for prevention of acute xenograft rejection. Papageorgiou, C., von Matt, A., Joergensen, J., Andersen, E., Wagner, K., Beerli, C., Than, T., Borer, X., Florineth, A., Rihs, G., Schreier, M.H., Weckbecker, G., Heusser, C. J. Med. Chem. (2001) [Pubmed]

Contributions to this collaborative article are from individual authors of WikiGenes or mined by the WikiGenes Data Mining Engine 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.

Editor

Share