901210-84-2Relevant academic research and scientific papers
2-arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase
Trotter,Quigley, Amy G.,Lumma, William C.,Sisko, John T.,Walsh, Eileen S.,Hamann, Christian S.,Robinson, Ronald G.,Bhimnathwala, Hema,Kolodin,Zheng, Wei,Buser, Carolyn A.,Huber, Hans E.,Lobell, Robert B.,Kohl, Nancy E.,Williams, Theresa M.,Graham, Samuel L.,Dinsmore, Christopher J.
, p. 865 - 869 (2001)
A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylation is suppressed.
