Open Access. Powered by Scholars. Published by Universities.®

Medicinal-Pharmaceutical Chemistry Commons

Open Access. Powered by Scholars. Published by Universities.®

Physics and Astronomy Publications

Other Chemistry

Articles 1 - 5 of 5

Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Crystal Structure Of The Alcanivorax Borkumensis Ydah Transporter Reveals An Unusual Topology, Jani Reddy Bolla, Chih-Chia Su, Jared A. Delmar, Pattathil Radhakrishnan, Nitin Kumar, Tsung-Han Chou, Feng Long, Kanagalaghatta R. Rajashankar, Edward Yu Jan 2015

Crystal Structure Of The Alcanivorax Borkumensis Ydah Transporter Reveals An Unusual Topology, Jani Reddy Bolla, Chih-Chia Su, Jared A. Delmar, Pattathil Radhakrishnan, Nitin Kumar, Tsung-Han Chou, Feng Long, Kanagalaghatta R. Rajashankar, Edward Yu

Physics and Astronomy Publications

The potential of the folic acid biosynthesis pathway as a target for the development of antibiotics has been clinically validated. However, many pathogens have developed resistance to these antibiotics, prompting a re-evaluation of potential drug targets within the pathway. The ydaH gene of Alcanivorax borkumensis encodes an integral membrane protein of the AbgT family of transporters for which no structural information was available. Here we report the crystal structure of A. borkumensis YdaH, revealing a dimeric molecule with an architecture distinct from other families of transporters. YdaH is a bowl-shaped dimer with a solvent-filled basin extending from the cytoplasm to ...


Structure And Function Of Neisseria Gonorrhoeae Mtrf Illuminates A Class Of Antimetabolite Efflux Pumps, Chih-Chia Su, Jani Reddy Bolla, Nitin Kumar, Pattathil Radhakrishnan, Feng Long, Jared A. Delmar, Tsung-Han Chou, Kanagalaghatta R. Rajashankar, William M. Shafer, Edward Yu Jan 2015

Structure And Function Of Neisseria Gonorrhoeae Mtrf Illuminates A Class Of Antimetabolite Efflux Pumps, Chih-Chia Su, Jani Reddy Bolla, Nitin Kumar, Pattathil Radhakrishnan, Feng Long, Jared A. Delmar, Tsung-Han Chou, Kanagalaghatta R. Rajashankar, William M. Shafer, Edward Yu

Physics and Astronomy Publications

Neisseria gonorrhoeae is an obligate human pathogen and the causative agent of the sexually transmitted disease gonorrhea. The control of this disease has been compromised by the increasing proportion of infections due to antibiotic-resistant strains, which are growing at an alarming rate. N. gonorrhoeae MtrF is an integral membrane protein that belongs to the AbgT family of transporters for which no structural information is available. Here, we describe the crystal structure of MtrF, revealing a dimeric molecule with architecture distinct from all other families of transporters. MtrF is a bowl-shaped dimer with a solvent-filled basin extending from the cytoplasm to ...


Functional Cloning And Characterization Of The Multidrug Efflux Pumps Norm From Neisseria Gonorrhoeae And Ydhe From Escherichia Coli, Feng Long, Corrinne Rouquette-Loughlin, William M. Shafer, Edward Yu Jan 2008

Functional Cloning And Characterization Of The Multidrug Efflux Pumps Norm From Neisseria Gonorrhoeae And Ydhe From Escherichia Coli, Feng Long, Corrinne Rouquette-Loughlin, William M. Shafer, Edward Yu

Physics and Astronomy Publications

Active efflux of antimicrobial agents is one of the most important adapted strategies that bacteria use to defend against antimicrobial factors that are present in their environment. The NorM protein of Neisseria gonorrhoeae and the YdhE protein of Escherichia coli have been proposed to be multidrug efflux pumps that belong to the multidrug and toxic compound extrusion (MATE) family. In order to determine their antimicrobial export capabilities, we cloned, expressed, and purified these two efflux proteins and characterized their functions both in vivo and in vitro. E. coli strains expressing norM or ydhE showed elevated (twofold or greater) resistance to ...


Cloning, Expression, Purification, Crystallization And Preliminary X-Ray Diffraction Analysis Of The Regulator Acrr From Escherichia Coli, Ming Li, Xi Qiu, Chih-Chia Su, Feng Long, Ruoyu Gu, Gerry Mcdermott, Edward Yu Jan 2006

Cloning, Expression, Purification, Crystallization And Preliminary X-Ray Diffraction Analysis Of The Regulator Acrr From Escherichia Coli, Ming Li, Xi Qiu, Chih-Chia Su, Feng Long, Ruoyu Gu, Gerry Mcdermott, Edward Yu

Physics and Astronomy Publications

This paper describes the cloning, expression, purification and preliminary X-ray data analysis of the AcrR regulatory protein. The Escherichia coli AcrR is a member of the TetR family of transcriptional regulators. It regulates the expression of the AcrAB multidrug transporter. Recombinant AcrR with a 6×His tag at the C-terminus was expressed in E. coli and purified by metal-affinity chromatography. The protein was crystallized using hanging-drop vapor diffusion. X-ray diffraction data were collected from cryocooled crystals at a synchrotron light source. The best crystal diffracted to 2.5 Å. The space group was determined to be P32, with ...


A Periplasmic Drug-Binding Site Of The Acrb Multidrug Efflux Pump: A Crystallographic And Site-Directed Mutagenesis Study, Edward Yu, Juilo R. Aires, Gerry Mcdermott, Hiroshi Nikaido Jan 2005

A Periplasmic Drug-Binding Site Of The Acrb Multidrug Efflux Pump: A Crystallographic And Site-Directed Mutagenesis Study, Edward Yu, Juilo R. Aires, Gerry Mcdermott, Hiroshi Nikaido

Physics and Astronomy Publications

The Escherichia coli AcrB multidrug efflux pump is a membrane protein that recognizes many structurally dissimilar toxic compounds. We previously reported the X-ray structures of four AcrB-ligand complexes in which the ligands were bound to the wall of the extremely large central cavity in the transmembrane domain of the pump. Genetic studies, however, suggested that discrimination between the substrates occurs mainly in the periplasmic domain rather than the transmembrane domain of the pump. We here describe the crystal structures of the AcrB mutant in which Asn109 was replaced by Ala, with five structurally diverse ligands, ethidium, rhodamine 6G, ciprofloxacin, nafcillin ...