1N95

Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives

Summary for 1N95

• Entry DOI: 10.2210/pdb1n95/pdb
• Related: 1N94 1N9A
• Descriptor: Protein farnesyltransferase alpha subunit, Protein farnesyltransferase beta subunit, ZINC ION, ... (5 entities in total)
• Functional Keywords: farnesyltransferase, histidine tetrahydropyridine, prenyltransferase, transferase
• Biological source: Rattus norvegicus (Norway rat); More
• Total number of polymer chains: 2
• Total formula weight: 83867.52

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: glycine, phenylalanine and histidine derivatives.
Bioorg.Med.Chem.Lett., 13:1359-1362, 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 a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.

PubMed: 12657282
DOI: 10.1016/S0960-894X(03)00095-7

Experimental method

X-RAY DIFFRACTION (2.3 Å)