| Structural highlights
2zir is a 2 chain structure with sequence from Rattus norvegicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | , , ,
| | Related: | 2zis |
| Gene: | Fnta (Rattus norvegicus), Fntb (Rattus norvegicus) |
| Activity: | Protein farnesyltransferase, with EC number 2.5.1.58 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice.
Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.,Asoh K, Kohchi M, Hyoudoh I, Ohtsuka T, Masubuchi M, Kawasaki K, Ebiike H, Shiratori Y, Fukami TA, Kondoh O, Tsukaguchi T, Ishii N, Aoki Y, Shimma N, Sakaitani M Bioorg Med Chem Lett. 2009 Mar 15;19(6):1753-7. Epub 2009 Feb 11. PMID:19217288[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Asoh K, Kohchi M, Hyoudoh I, Ohtsuka T, Masubuchi M, Kawasaki K, Ebiike H, Shiratori Y, Fukami TA, Kondoh O, Tsukaguchi T, Ishii N, Aoki Y, Shimma N, Sakaitani M. Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1753-7. Epub 2009 Feb 11. PMID:19217288 doi:10.1016/j.bmcl.2009.01.074
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