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Volumn 6, Issue 12, 1996, Pages 1291-1296

Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; METHYLPHOSPHONIC ACID; PHENYLALANINE DERIVATIVE; PHENYLALANINE METHYL ESTER; PHOSPHONIC ACID DERIVATIVE; PROTEIN FARNESYLTRANSFERASE; PROTEIN FARNESYLTRANSFERASE INHIBITOR; RAS PROTEIN; SQUALENE SYNTHASE; SQUALENE SYNTHASE INHIBITOR;

EID: 0030011713     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00238-7     Document Type: Article
Times cited : (11)

References (36)
  • 1
    • 0025078512 scopus 로고
    • a) Hall, A. Science 1990, 249, 635.
    • (1990) Science , vol.249 , pp. 635
    • Hall, A.1
  • 10
    • 0027213688 scopus 로고
    • a) Tamanoï, F. TIBS 1993, 18, 349.
    • (1993) TIBS , vol.18 , pp. 349
    • Tamanoï, F.1
  • 26
    • 85030205293 scopus 로고    scopus 로고
    • note
    • All new compounds have been fully characterised by CHN analysis, IR, MS and NMR spectra. Compounds 3a-3g have been isolated as mixtures of epimers at the carbon center next to the phosphoryl and/or carboxyl groups. In the case of compound 3a, the epimers at the diethylester precursor level have been separated but spontaneous epimerization was observed upon deprotection.
  • 29
    • 0025194466 scopus 로고
    • FPT was partially purified by ion exchange chromatography on a Hi-Trap Q sepharose column from bovine brain according to a) Reiss, Y.; Goldstein, J.L.; Seabra, M.C.; Casey, P.J.; Brown, M.S. Cell 1990, 62, 81.
    • (1990) Cell , vol.62 , pp. 81
    • Reiss, Y.1    Goldstein, J.L.2    Seabra, M.C.3    Casey, P.J.4    Brown, M.S.5
  • 31
    • 0001437041 scopus 로고
    • b) Moores, S.L.; Schaber, M.D.; Mosser S.D.; Rands, E.; O'Hara, M.B.; Garsky, V.M.; Marshall, M.S.; Pompliano, D.L.; Gibbs, J.B. J. Biol. Chem. 1991, 268, 14603. FPT activity was measured by fluorimetry using 2μM dansyl-GCVLS and 2μM FPP as described by Pompliano, D.L.; Gomez, R.P.; Anthony, N.J. J. Amer. Chem. Soc. 1992, 114, 7945.
    • (1992) J. Amer. Chem. Soc. , vol.114 , pp. 7945
    • Pompliano, D.L.1    Gomez, R.P.2    Anthony, N.J.3
  • 36
    • 0343350731 scopus 로고
    • Houston, TX, Nov.
    • For example, BMS-188494 which is the bis(pivaloyloxy-methyl) ester prodrug of the phosphonic acid BMS-187745 (a potent SS inhibitor) is an orally active hypocholesterolemic agent which has now entered phase II clinical trials (Gregg, R. E. XII International Symposium on Drugs Affecting Lipid Metabolism Houston, TX, Nov. 1995).
    • (1995) XII International Symposium on Drugs Affecting Lipid Metabolism
    • Gregg, R.E.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.