1mzc

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spinqualitylabelsall models 1mzc, resolution 2.00Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a

Overview

A series of novel diaryl ether lactams have been identified as very potent, dual inhibitors of protein farnesyltransferase (FTase) and protein, geranylgeranyltransferase I (GGTase-I), enzymes involved in the, prenylation of Ras. The structure of the complex formed between one of, these compounds and FTase has been determined by X-ray crystallography., These compounds are the first reported to inhibit the prenylation of the, important oncogene Ki-Ras4B in vivo. Unfortunately, doses sufficient to, achieve this endpoint were rapidly lethal.

About this Structure

1MZC is a Protein complex structure of sequences from Homo sapiens with , , and as ligands. Full crystallographic information is available from OCA.

Reference

Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents., deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, Fernandes C, Hamilton KA, Huber HE, Kohl NE, Lobell RB, Robinson RG, Tsou NN, Walsh ES, Graham SL, Beese LS, Taylor JS, J Med Chem. 2003 Jul 3;46(14):2973-84. PMID:12825937

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