3KSQ

Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors

Summary for 3KSQ

• Entry DOI: 10.2210/pdb3ksq/pdb
• Descriptor: Farnesyltransferase, CAAX box, alpha, Protein farnesyltransferase subunit beta, MAGNESIUM ION, ... (7 entities in total)
• Functional Keywords: prenyltransferase, metal-binding, phosphoprotein, transferase
• Biological source: Rattus norvegicus (rat); More
• Total number of polymer chains: 2
• Total formula weight: 93802.45

Authors

Zhu, H.Y.,Cooper, A.B.,Njoroge, G.,Kirschmeier, P.,Strickland, C.,Hruza, A.,Girijavallabhan, V.M. (deposition date: 2009-11-23, release date: 2010-01-26, Last modification date: 2023-09-06)

Primary citation

Zhu, H.Y.,Cooper, A.B.,Desai, J.,Njoroge, G.,Kirschmeier, P.,Bishop, W.R.,Strickland, C.,Hruza, A.,Doll, R.J.,Girijavallabhan, V.M.
Discovery of C-imidazole azaheptapyridine FPT inhibitors.
Bioorg.Med.Chem.Lett., 20:1134-1136, 2010

PubMed Abstract: The discovery of C-linked imidazole azaheptapyridine bridgehead FPT inhibitors is described. This novel class of compounds are sub nM FPT enzyme inhibitors with potent cellular inhibitory activities. This series also has reduced hERG activity versus previous N-linked imidazole series. X-ray of compound 10a bound to FTase revealed strong interaction between bridgehead imidazole 3N with catalytic zinc atom.

PubMed: 20056542
DOI: 10.1016/j.bmcl.2009.12.013

Experimental method

X-RAY DIFFRACTION (2.1 Å)