2ZIS

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

Summary for 2ZIS

Entry DOI	10.2210/pdb2zis/pdb
Related	2ZIR
Descriptor	Protein farnesyltransferase subunit alpha, Protein farnesyltransferase subunit beta, ACETIC ACID, ... (8 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	94410.23
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 Cited by 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 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.6 Å)

Structure validation