Probing the hydrophobic pocket of farnesyltransferase: Aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors

Bioorganic and Medicinal Chemistry

Volumn 7, Issue 12, 1999, Pages 3011-3024

  Qian, Yimin ^a   Marugan, Juan Jose ^c   Fossum, Renae D ^c   Vogt, Andreas ^d   Sebti, Said M ^b   Hamilton, Andrew D ^a  

^a YALE UNIVERSITY   (United States)

^b H LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE   (United States)

^c UNIVERSITY OF PITTSBURGH   (United States)

^d UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

Author keywords

Anticancer targets; Farnesyltransferase inhibitors; Hydrophobic pocket; Peptidomimetics

Indexed keywords

AROMATIC COMPOUND; CYSTEINE; FARNESYL TRANS TRANSFERASE; FUNCTIONAL GROUP; GERANYLGERANYLTRANSFERASE 1; PEPTIDOMIMETIC AGENT; PROTEIN FARNESYLTRANSFERASE INHIBITOR; RAS PROTEIN; UNCLASSIFIED DRUG;

ARTICLE; CANCER; CARBON NUCLEAR MAGNETIC RESONANCE; CARBOXY TERMINAL SEQUENCE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME INHIBITION; HYDROPHOBICITY; MUTATION; ONCOGENE; PROTEIN MODIFICATION; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION;

ALKYL AND ARYL TRANSFERASES; BINDING SITES; CELL LINE; DRUG DESIGN; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; MOLECULAR PROBES; OLIGOPEPTIDES; RAS PROTEINS;

EID: 0033367998     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0968-0896(99)00252-7     Document Type: Article

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