1NI1

Imidazole and cyanophenyl farnesyl transferase inhibitors

Summary for 1NI1

• Entry DOI: 10.2210/pdb1ni1/pdb
• Related: 1N95 1N9A
• Descriptor: Protein farnesyltransferase alpha subunit, Protein farnesyltransferase beta subunit, ZINC ION, ... (5 entities in total)
• Functional Keywords: transferase, prenyltransferase, ftase, cyanophenyl
• Biological source: Rattus norvegicus (Norway rat); More
• Total number of polymer chains: 2
• Total formula weight: 83841.27

Authors

Tong, Y.,Lin, N.H.,Wang, L.,Hasvold, L.,Wang, W.,Leonard, N.,Li, T.,Li, Q.,Cohen, J.,Gu, W.Z.,Zhang, H.,Stoll, V.,Bauch, J.,Marsh, K.,Rosenberg, S.H.,Sham, H.L. (deposition date: 2002-12-20, release date: 2004-04-06, Last modification date: 2024-02-14)

Primary citation

Tong, Y.,Lin, N.H.,Wang, L.,Hasvold, L.,Wang, W.,Leonard, N.,Li, T.,Li, Q.,Cohen, J.,Gu, W.Z.,Zhang, H.,Stoll, V.,Bauch, J.,Marsh, K.,Rosenberg, S.H.,Sham, H.L.
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.
Bioorg.Med.Chem.Lett., 13:1571-1574, 2003

PubMed Abstract: A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.

PubMed: 12699757
DOI: 10.1016/S0960-894X(03)00195-1

Experimental method

X-RAY DIFFRACTION (2.3 Å)