Antifungals: mechanism of action and resistance, established and novel drugs

被引：181

作者：

Georgopapadakou, NH ^{[1
]}

机构：

[1] DuPont Co Inc, Pharmaceut Res Labs, Expt Stn, Wilmington, DE 19880 USA

来源：

CURRENT OPINION IN MICROBIOLOGY | 1998年 / 1卷 / 05期

关键词：

D O I：

10.1016/S1369-5274(98)80087-8

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Serious fungal infections, caused mostly by opportunistic species, are increasingly common in immunocompromised and other vulnerable patients. The use of antifungal drugs, primarily azoles and polyenes, has increased in parallel. Yet, established agents do not satisfy the medical need completely: azoles are fungistatic and vulnerable to resistance, whereas polyenes cause serious host toxicity. Drugs in clinical development include echinocandins, pneumocandins, and improved azoles. Promising novel agents in preclinical development include several inhibitors of fungal protein, lipid and cell wall syntheses. Recent advances in fungal genomics, combinatorial chemistry, and high-throughput screening may accelerate the antifungal discovery process.

引用

页码：547 / 557

页数：11

共 154 条

[31] Echinocandins and pneumocandins - a new antifungal class with a novel mode of action [J].

Denning, DW .

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1997, 40 (05) :611-614

[32] Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity [J].

Devadas, B ;

Freeman, SK ;

Zupec, ME ;

Lu, HF ;

Nagarajan, SR ;

Kishore, NS ;

Lodge, JK ;

Kuneman, DW ;

McWherter, CA ;

Vinjamoori, DV ;

Getman, DP ;

Gordon, JI ;

Sikorski, JA .

JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (16) :2609-2625

[33] Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase [J].

Devadas, B ;

Freeman, SK ;

McWherter, CA ;

Kishore, NS ;

Lodge, JK ;

Jackson-Machelski, E ;

Gordon, JI ;

Sikorski, JA .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (06) :996-1000

[34] SYNTHESIS OF INHIBITORS OF 2,3-OXIDOSQUALENE LANOSTEROL CYCLASE .2. CYCLOCONDENSATION OF GAMMA,DELTA-UNSATURATED BETA-KETO-ESTERS WITH IMINES [J].

DODD, DS ;

OEHLSCHLAGER, AC ;

GEORGOPAPADAKOU, NH ;

POLAK, AM ;

HARTMAN, PG .

JOURNAL OF ORGANIC CHEMISTRY, 1992, 57 (26) :7226-7234

[35]

DOMINGUEZ JM, 1997, 37 INT C ANT AG CHEM, P155

[36] A SACCHAROMYCES-CEREVISIAE MUTANT WITH ECHINOCANDIN-RESISTANT 1,3-BETA-D-GLUCAN SYNTHASE [J].

DOUGLAS, CM ;

MARRINAN, JA ;

LI, W ;

KURTZ, MB .

JOURNAL OF BACTERIOLOGY, 1994, 176 (18) :5686-5696

[37] THE SACCHAROMYCES-CEREVISIAE FKS1 (ETG1) GENE ENCODES AN INTEGRAL MEMBRANE-PROTEIN WHICH IS A SUBUNIT OF 1,3-BETA-D-GLUCAN SYNTHASE [J].

DOUGLAS, CM ;

FOOR, F ;

MARRINAN, JA ;

MORIN, N ;

NIELSEN, JB ;

DAHL, AM ;

MAZUR, P ;

BAGINSKY, W ;

LI, WL ;

ELSHERBEINI, M ;

CLEMAS, JA ;

MANDALA, SM ;

FROMMER, BR ;

KURTZ, MB .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1994, 91 (26) :12907-12911

[38] Rho1p, a yeast protein at the interface between cell polarization and morphogenesis [J].

Drgonova, J ;

Drgon, T ;

Tanaka, K ;

Kollar, R ;

Chen, GC ;

Ford, RA ;

Chan, CSM ;

Takai, Y ;

Cabib, E .

SCIENCE, 1996, 272 (5259) :277-279

[39] SELECTIVE-INHIBITION OF TOPOISOMERASES FROM PNEUMOCYSTIS-CARINII COMPARED WITH THAT OF TOPOISOMERASES FROM MAMMALIAN-CELLS [J].

DYKSTRA, CC ;

MCCLERNON, DR ;

ELWELL, LP ;

TIDWELL, RR .

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1994, 38 (09) :1890-1898

[40] A conserved kinase cascade for MAP kinase activation in yeast [J].

Errede, Beverly ;

Levin, David E. .

CURRENT OPINION IN CELL BIOLOGY, 1993, 5 (02) :254-260

← 1 2 3 4 5 6 7 8 9 10 →