The first low μM SecA inhibitors
نویسندگان
چکیده
منابع مشابه
Inhibitors of SecA as Potential Antimicrobial Agents
Protein translocation is essential for bacterial survival and the most important translocation mechanism in bacteria is the secretion (Sec) pathway. Thus targeting Sec pathway is a promising strategy for developing novel antibacterial therapeutics. We report the design, syntheses, mechanistic studies and structure-activity relationship analyses using HQSAR and 3-D QSAR Topomer CoMFA analyses of...
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In our previous study, we have identified five antimicrobial small molecules via structure based design, which inhibit SecA of Candidatus Liberibacter asiaticus (Las). SecA is a critical protein translocase ATPase subunit and is involved in pre-protein translocation across and integration into the cellular membrane in bacteria. In this study, eleven compounds were identified using similarity se...
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Abstract This paper presents a design of a switched-capacitor discrete time 1st order Delta-Sigma modulator used for a resolution of 8 bits Sigma-Delta analog to digital converter. For lower power consumption, the use of operational transconductance amplifier is necessary in order to provide wide output voltage swing and moderate DC gain. Simulation results showed that with 0.35um CMOS technolo...
متن کاملDevelopment of a high-throughput screening assay for the discovery of small-molecule SecA inhibitors.
A major pathway for bacterial preprotein translocation is provided by the Sec-dependent preprotein translocation pathway. Proteins destined for Sec-dependent translocation are synthesized as preproteins with an N-terminal signal peptide, which targets them to the SecYEG translocase channel. The driving force for the translocation reaction is provided by the peripheral membrane ATPase SecA, whic...
متن کاملBinding of SecA to the SecYEG complex accelerates the rate of nucleotide exchange on SecA.
SecYEG translocase mediates the transport of preproteins across the inner membrane of Escherichia coli. SecA binds the membrane-embedded SecYEG protein-conducting channel with high affinity and then drives the stepwise translocation of preproteins across the membrane through multiple cycles of ATP binding and hydrolysis. We have investigated the kinetics of nucleotide binding to SecA while asso...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2010
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2009.12.074