2ZIR

Crystal Structure of rat protein farnesyltransferase complexed with a benzofuran inhibitor and FPP

Summary for 2ZIR

• Entry DOI: 10.2210/pdb2zir/pdb
• Related: 2ZIS
• Descriptor: Protein farnesyltransferase subunit alpha, Protein farnesyltransferase subunit beta, GLYCEROL, ... (7 entities in total)
• Functional Keywords: prenyltransferase, transferase, metal-binding, phosphoprotein
• Biological source: Rattus norvegicus (Rat); More
• Total number of polymer chains: 2
• Total formula weight: 94541.87

Authors

Fukami, T.A.,Sogabe, S.,Nagata, Y.,Kondoh, O.,Ishii, N. (deposition date: 2008-02-22, release date: 2009-02-24, Last modification date: 2023-11-01)

Primary citation

Asoh, K.,Kohchi, M.,Hyoudoh, I.,Ohtsuka, T.,Masubuchi, M.,Kawasaki, K.,Ebiike, H.,Shiratori, Y.,Fukami, T.A.,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., 19:1753-1757, 2009

PubMed Abstract: 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.

PubMed: 19217288
DOI: 10.1016/j.bmcl.2009.01.074

Experimental method

X-RAY DIFFRACTION (2.4 Å)