Antifungal activity of a Candida albicans GGTase I inhibitor-alanine conjugate. Inhibition of Rho1p prenylation in C. albicans.

作者: Krishna K Murthi , Susan E Smith , Arthur F Kluge , Gustave Bergnes , Patrick Bureau

DOI: 10.1016/S0960-894X(03)00320-2

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摘要: An alanine conjugate of a Candida albicans geranylgeranyl transferase I inhibitor was synthesized to facilitate its uptake into the fungal cell. The antifungal activity CaGGTase-Ala is demonstrated. It also shown that affects prenylation endogenous Rho1p, but has no effect on Ras1p.

参考文章(12)
Brian E. Caplin, Mark S. Marshall, [6] Mutagenesis and biochemical analysis of recombinant yeast prenyltransferases Methods in Enzymology. ,vol. 250, pp. 51- 68 ,(1995) , 10.1016/0076-6879(95)50062-6
O Kondoh, Y Tachibana, Y Ohya, M Arisawa, T Watanabe, Cloning of the RHO1 gene from Candida albicans and its regulation of beta-1,3-glucan synthesis. Journal of Bacteriology. ,vol. 179, pp. 7734- 7741 ,(1997) , 10.1128/JB.179.24.7734-7741.1997
William G. Stirtan, C. Dale Poulter, Yeast Protein Geranylgeranyltransferase Type-I: Steady-State Kinetics and Substrate Binding† Biochemistry. ,vol. 36, pp. 4552- 4557 ,(1997) , 10.1021/BI962579C
Elizabeth A. Stone, Horatio B. Fung, Harold L. Kirschenbaum, Caspofungin: an echinocandin antifungal agent. Clinical Therapeutics. ,vol. 24, pp. 351- 377 ,(2002) , 10.1016/S0149-2918(02)85039-1
William D. Kingsbury, Jeffrey C. Boehm, Rajanikant J. Mehta, Sarah F. Grappel, Transport of antimicrobial agents using peptide carrier systems: anticandidal activity of m-fluorophenylalanine--peptide conjugates. Journal of Medicinal Chemistry. ,vol. 26, pp. 1725- 1729 ,(1983) , 10.1021/JM00366A013
Nafsika H Georgopapadakou, Jan S Tkacz, The fungal cell wall as a drug target Trends in Microbiology. ,vol. 3, pp. 98- 104 ,(1995) , 10.1016/S0966-842X(00)88890-3
C. A. Omer, J. B. Gibbs, Protein prenylation in eukaryotic microorganisms: genetics, biology and biochemistry. Molecular Microbiology. ,vol. 11, pp. 219- 225 ,(1994) , 10.1111/J.1365-2958.1994.TB00302.X
Jana Drgonová, Tomás Drgon, Enrico Cabib, Role of small G proteins in yeast cell polarization and wall biosynthesis Annual Review of Biochemistry. ,vol. 67, pp. 307- 333 ,(1998) , 10.1146/ANNUREV.BIOCHEM.67.1.307
Susan E. Smith, Csilla Csank, Guadalupe Reyes, Mahmoud A. Ghannoum, Vivian Berlin, Candida albicans RHO1 is required for cell viability in vitro and in vivo. Fems Yeast Research. ,vol. 2, pp. 103- 111 ,(2002) , 10.1111/J.1567-1364.2002.TB00075.X
D. W. Denning, Echinocandins: a new class of antifungal Journal of Antimicrobial Chemotherapy. ,vol. 49, pp. 889- 891 ,(2002) , 10.1093/JAC/DKF045