1N9A

Farnesyltransferase complex with tetrahydropyridine inhibitors

Summary for 1N9A

• Entry DOI: 10.2210/pdb1n9a/pdb
• Related: 1N94 1N95
• Descriptor: Protein farnesyltransferase alpha subunit, Protein farnesyltransferase beta subunit, ZINC ION, ... (5 entities in total)
• Functional Keywords: farnesyltransferase, tetrahydropyridine, prenyltransferase, transferase
• Biological source: Rattus norvegicus (Norway rat); More
• Total number of polymer chains: 2
• Total formula weight: 83824.45

Authors

Gwaltney II, S.L.,O'Conner, S.J.,Nelson, L.T.,Sullivan, G.M.,Imade, H.,Wang, W.,Hasvold, L.,Li, Q.,Cohen, J.,Gu, W.Z. (deposition date: 2002-11-22, release date: 2003-01-07, Last modification date: 2024-02-14)

Primary citation

Gwaltney II, S.L.,O'Connor, S.J.,Nelson, L.T.,Sullivan, G.M.,Imade, H.,Wang, W.,Hasvold, L.,Li, Q.,Cohen, J.,Gu, W.Z.,Tahir, S.K.,Bauch, J.,Marsh, K.,Ng, S.C.,Frost, D.J.,Zhang, H.,Muchmore, S.,Jakob, C.G.,Stoll, V.,Hutchins, C.,Rosenberg, S.H.,Sham, H.L.
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Bioorg.Med.Chem.Lett., 13:1363-1366, 2003

PubMed Abstract: Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.

PubMed: 12657283
DOI: 10.1016/S0960-894X(03)00094-5

Experimental method

X-RAY DIFFRACTION (3.2 Å)