H-phosphonate derivatives as novel peptide deformylase inhibitors

被引:27
作者
Hu, YJ [1 ]
Rajagopalan, PTR [1 ]
Pei, DH [1 ]
机构
[1] Ohio State Univ, Dept Chem, Columbus, OH 43210 USA
关键词
D O I
10.1016/S0960-894X(98)00443-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Peptide deformylase catalyzes the removal of the N-terminal formyl group from nascent polypeptides during prokaryotic protein maturation and is essential for bacterial survival. Its absence from eukaryotic organisms makes it an attractive target for designing novel antibacterial agents. Peptidyl H-phosphonates were synthesized and shown to be competitive inhibitors of the deformylase. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2479 / 2482
页数:4
相关论文
共 17 条
[1]   ON RELEASE OF FORMYL GROUP FROM NASCENT PROTEIN [J].
ADAMS, JM .
JOURNAL OF MOLECULAR BIOLOGY, 1968, 33 (03) :571-&
[2]   Communication - Structure of peptide deformylase and identification of the substrate binding site [J].
Becker, A ;
Schlichting, I ;
Kabsch, W ;
Schultz, S ;
Wagner, AFV .
JOURNAL OF BIOLOGICAL CHEMISTRY, 1998, 273 (19) :11413-11416
[3]  
BRIAN C, 1986, NUCLEIC ACIDS RES, V14, P5399
[4]   Crystal structure of the Escherichia coli peptide deformylase [J].
Chan, MK ;
Gong, WM ;
Rajagopalan, PTR ;
Hao, B ;
Tsai, CM ;
Pei, DH .
BIOCHEMISTRY, 1997, 36 (45) :13904-13909
[5]   PHOSPHORUS AMINO-ACID-ANALOGS AS INHIBITORS OF LEUCINE AMINOPEPTIDASE [J].
GIANNOUSIS, PP ;
BARTLETT, PA .
JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (09) :1603-1609
[6]   A PHOSPHONAMIDATE DIPEPTIDE ANALOG AS AN INHIBITOR OF CARBOXYPEPTIDASE-A [J].
JACOBSEN, NE ;
BARTLETT, PA .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1981, 103 (03) :654-657
[7]  
Kock P., 1983, B SOC CHIM FR, V11, P189
[8]  
KOZAK M, 1983, MICROBIOL REV, V47, P1
[9]   TOTAL SYNTHESIS AND STRUCTURAL INVESTIGATIONS OF DIDEMNIN-A, DIDEMNIN-B, AND DIDEMNIN-C [J].
LI, WR ;
EWING, WR ;
HARRIS, BD ;
JOULLIE, MM .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1990, 112 (21) :7659-7672
[10]   DEFORMYLATION AND PROTEIN BIOSYNTHESIS [J].
LIVINGSTON, DM ;
LEDER, P .
BIOCHEMISTRY, 1969, 8 (01) :435-+