RGD Reference Report - Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. - Rat Genome Database

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Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.

Authors: Gwaltney SL, 2ND  O'Connor, SJ  Nelson, LT  Sullivan, GM  Imade, H  Wang, W  Hasvold, L  Li, Q  Cohen, J  Gu, WZ  Tahir, SK  Bauch, J  Marsh, K  Ng, SC  Frost, DJ  Zhang, H  Muchmore, S  Jakob, CG  Stoll, V  Hutchins, C  Rosenberg, SH  Sham, HL 
Citation: Gwaltney SL 2nd, etal., Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62.
RGD ID: 8554767
Pubmed: PMID:12657282   (View Abstract at PubMed)

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.




Molecular Function

  
Object Symbol
Species
Term
Qualifier
Evidence
With
Notes
Source
Original Reference(s)
FntaRatprotein binding enablesIPIUniProtKB:Q02293PMID:12657282IntAct 
FntbRatprotein binding enablesIPIUniProtKB:Q04631PMID:12657282IntAct 


Genes (Rattus norvegicus)
Fnta  (farnesyltransferase, CAAX box, subunit alpha) Fntb  (farnesyltransferase, CAAX box, subunit beta)