1mzc

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{{STRUCTURE_1mzc| PDB=1mzc | SCENE= }}
{{STRUCTURE_1mzc| PDB=1mzc | SCENE= }}
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'''Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a'''
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===Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 12825937 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12825937}}
==About this Structure==
==About this Structure==
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[[Category: Pftase]]
[[Category: Pftase]]
[[Category: Ra]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 01:53:39 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 17:47:08 2008''

Revision as of 14:47, 28 July 2008

Image:1mzc.png

Template:STRUCTURE 1mzc

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

Template:ABSTRACT PUBMED 12825937

About this Structure

1MZC is a Protein complex structure of sequences from Homo sapiens. 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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