PMID- 16413022
OWN - NLM
STAT- MEDLINE
DCOM- 20060321
LR  - 20151119
IS  - 0014-5793 (Print)
IS  - 0014-5793 (Linking)
VI  - 580
IP  - 2
DP  - 2006 Jan 23
TI  - Characterization and inhibitor discovery of one novel malonyl-CoA: acyl carrier 
      protein transacylase (MCAT) from Helicobacter pylori.
PG  - 697-702
AB  - Type II fatty acid synthesis (FAS II) is an essential process for bacteria 
      survival, and malonyl-CoA:acyl carrier protein transacylase (MCAT) is a key 
      enzyme in FAS II pathway, which is responsible for transferring the malonyl group 
      from malonyl-CoA to the holo-ACP by forming malonyl-ACP. In this work, we 
      described the cloning, characterization and enzymatic inhibition of a new MCAT 
      from Helicobacter pylori strain SS1 (HpMCAT), and the gene sequence of HpfabD was 
      deposited in the GenBank database (Accession No. AY738332 ). Enzymatic 
      characterization of HpMCAT showed that the K(m) value for malonyl-CoA was 
      21.01+/-2.3 microM, and the thermal- and guanidinium hydrochloride-induced 
      unfolding processes for HpMCAT were quantitatively investigated by circular 
      dichroism spectral analyses. Moreover, a natural product, corytuberine, was 
      discovered to demonstrate inhibitory activity against HpMCAT with IC(50) value at 
      33.1+/-3.29 microM. Further enzymatic assay results indicated that corytuberine 
      inhibits HpMCAT in an uncompetitive manner. To our knowledge, this is the firstly 
      reported MCAT inhibitor to date. This current work is hoped to supply useful 
      information for better understanding the MCAT features of H. pylori strain, and 
      corytuberine might be used as a potential lead compound in the discovery of the 
      antibacterial agents using HpMCAT as target.
FAU - Liu, Weizhi
AU  - Liu W
AD  - Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai 
      Institute of Materia Medica, Shanghai Institutes for Biological Sciences, 
      Graduate School of the Chinese Academy of Sciences, Shanghai 201203, China.
FAU - Han, Cong
AU  - Han C
FAU - Hu, Lihong
AU  - Hu L
FAU - Chen, Kaixian
AU  - Chen K
FAU - Shen, Xu
AU  - Shen X
FAU - Jiang, Hualiang
AU  - Jiang H
LA  - eng
SI  - GENBANK/AY738332
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20060106
PL  - England
TA  - FEBS Lett
JT  - FEBS letters
JID - 0155157
RN  - 0 (Aporphines)
RN  - 0 (Bacterial Proteins)
RN  - 0 (Fatty Acids)
RN  - 4YJ94A3D8W (corytuberine)
RN  - EC 2.3.1.39 (Acyl-Carrier Protein S-Malonyltransferase)
SB  - IM
MH  - Acyl-Carrier Protein S-Malonyltransferase/*antagonists & 
      inhibitors/chemistry/genetics/*metabolism
MH  - Amino Acid Sequence
MH  - Aporphines/metabolism
MH  - Bacterial Proteins/*antagonists & inhibitors/chemistry/genetics/*metabolism
MH  - Enzyme Stability
MH  - Fatty Acids/biosynthesis
MH  - Helicobacter pylori/*enzymology
MH  - Molecular Sequence Data
MH  - Molecular Structure
MH  - Protein Denaturation
MH  - Sequence Alignment
EDAT- 2006/01/18 09:00
MHDA- 2006/03/22 09:00
CRDT- 2006/01/18 09:00
PHST- 2005/12/09 00:00 [received]
PHST- 2005/12/27 00:00 [revised]
PHST- 2005/12/27 00:00 [accepted]
PHST- 2006/01/18 09:00 [pubmed]
PHST- 2006/03/22 09:00 [medline]
PHST- 2006/01/18 09:00 [entrez]
AID - S0014-5793(05)01570-X [pii]
AID - 10.1016/j.febslet.2005.12.085 [doi]
PST - ppublish
SO  - FEBS Lett. 2006 Jan 23;580(2):697-702. doi: 10.1016/j.febslet.2005.12.085. Epub 
      2006 Jan 6.