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  1. Article ; Online: Introduction: Transporters, Porins, and Efflux Pumps.

    Zgurskaya, Helen I

    Chemical reviews

    2021  Volume 121, Issue 9, Page(s) 5095–5097

    Abstract: All living cells are surrounded by lipidic membranes that separate metabolic and macromolecular biosynthetic processes from external environments. Biological membranes vary dramatically in their composition and structures and are optimized by mega-annum ... ...

    Abstract All living cells are surrounded by lipidic membranes that separate metabolic and macromolecular biosynthetic processes from external environments. Biological membranes vary dramatically in their composition and structures and are optimized by mega-annum of evolution to effectively carry out diverse biological functions including energy production, biosynthetic reactions, signaling, uptake of nutrients and active efflux, and others. This thematic issue of
    MeSH term(s) Animals ; Bacteria/metabolism ; Biological Transport ; Cell Membrane/metabolism ; Diffusion ; Eukaryotic Cells/metabolism ; Humans ; Membrane Lipids/metabolism ; Porins/metabolism ; Solute Carrier Proteins/metabolism
    Chemical Substances Membrane Lipids ; Porins ; Solute Carrier Proteins
    Language English
    Publishing date 2021-05-11
    Publishing country United States
    Document type Editorial ; Introductory Journal Article
    ZDB-ID 207949-5
    ISSN 1520-6890 ; 0009-2665
    ISSN (online) 1520-6890
    ISSN 0009-2665
    DOI 10.1021/acs.chemrev.1c00010
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: An Old Problem in a New Light: Antibiotic Permeation Barriers.

    Zgurskaya, Helen I

    ACS infectious diseases

    2020  Volume 6, Issue 12, Page(s) 3090–3091

    MeSH term(s) Anti-Bacterial Agents/pharmacokinetics ; Diffusion ; Permeability
    Chemical Substances Anti-Bacterial Agents
    Language English
    Publishing date 2020-12-09
    Publishing country United States
    Document type Editorial
    ISSN 2373-8227
    ISSN (online) 2373-8227
    DOI 10.1021/acsinfecdis.0c00780
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  3. Book ; Online ; E-Book: Efflux-mediated antimicrobial resistance in bacteria

    Li, Xian-Zhi / Elkins, Christopher A. / Zgurskaya, Helen I.

    mechanisms, regulation and clinical implications

    2016  

    Author's details Xian-Zhi Li, Christopher A. Elkins, Helen I. Zgurskaya editors
    Keywords ABC ; Acinetobacter ; Antibiotic ; Antimicrobial ; Chromosome ; Enterobacteriaceae ; Inhibitor ; MATE ; MDR ; MFS ; Microbiology ; Multidrug ; Pharmacology ; Plasmid ; Pseudomonas ; Pump ; RND ; SMR ; Staphylococcus ; Transporter
    Language English
    Size 1 Online-Ressource (xxi, 848 Seiten)
    Publisher Adis
    Publishing place Cham
    Publishing country Germany
    Document type Book ; Online ; E-Book
    Remark Zugriff für angemeldete ZB MED-Nutzerinnen und -Nutzer
    HBZ-ID HT019154065
    ISBN 978-3-319-39658-3 ; 9783319396569 ; 3-319-39658-7 ; 3319396560
    DOI 10.1007/978-3-319-39658-3
    Database ZB MED Catalogue: Medicine, Health, Nutrition, Environment, Agriculture

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  4. Article ; Online: Study of SQ109 analogs binding to mycobacterium MmpL3 transporter using MD simulations and alchemical relative binding free energy calculations.

    Stampolaki, Marianna / Stylianakis, Ioannis / Zgurskaya, Helen I / Kolocouris, Antonios

    Journal of computer-aided molecular design

    2023  Volume 37, Issue 5-6, Page(s) 245–264

    Abstract: N-geranyl-N΄-(2-adamantyl)ethane-1,2-diamine (SQ109) is a tuberculosis drug that has high potency against Mycobacterium tuberculosis (Mtb) and may function by blocking cell wall biosynthesis. After the crystal structure of MmpL3 from Mycobacterium ... ...

    Abstract N-geranyl-N΄-(2-adamantyl)ethane-1,2-diamine (SQ109) is a tuberculosis drug that has high potency against Mycobacterium tuberculosis (Mtb) and may function by blocking cell wall biosynthesis. After the crystal structure of MmpL3 from Mycobacterium smegmatis in complex with SQ109 became available, it was suggested that SQ109 inhibits Mmpl3 mycolic acid transporter. Here, we showed using molecular dynamics (MD) simulations that the binding profile of nine SQ109 analogs with inhibitory potency against Mtb and alkyl or aryl adducts at C-2 or C-1 adamantyl carbon to MmpL3 was consistent with the X-ray structure of MmpL3 - SQ109 complex. We showed that rotation of SQ109 around carbon-carbon bond in the monoprotonated ethylenediamine unit favors two gauche conformations as minima in water and lipophilic solvent using DFT calculations as well as inside the transporter's binding area using MD simulations. The binding assays in micelles suggested that the binding affinity of the SQ109 analogs was increased for the larger, more hydrophobic adducts, which was consistent with our results from MD simulations of the SQ109 analogues suggesting that sizeable C-2 adamantyl adducts of SQ109 can fill a lipophilic region between Y257, Y646, F260 and F649 in MmpL3. This was confirmed quantitatively by our calculations of the relative binding free energies using the thermodynamic integration coupled with MD simulations method with a mean assigned error of 0.74 kcal mol
    MeSH term(s) Antitubercular Agents/pharmacology ; Molecular Dynamics Simulation ; Bacterial Proteins/chemistry ; Membrane Transport Proteins/chemistry ; Membrane Transport Proteins/metabolism ; Mycobacterium tuberculosis ; Ethylenediamines/metabolism ; Ethylenediamines/pharmacology
    Chemical Substances Antitubercular Agents ; Bacterial Proteins ; Membrane Transport Proteins ; N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine ; Ethylenediamines
    Language English
    Publishing date 2023-05-02
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 808166-9
    ISSN 1573-4951 ; 0920-654X
    ISSN (online) 1573-4951
    ISSN 0920-654X
    DOI 10.1007/s10822-023-00504-6
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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2625: Show issues Location:
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  5. Article ; Online: Recent advances in mycobacterial membrane protein large 3 inhibitor drug design for mycobacterial infections.

    North, E Jeffrey / Schwartz, Chris P / Zgurskaya, Helen I / Jackson, Mary

    Expert opinion on drug discovery

    2023  Volume 18, Issue 7, Page(s) 707–724

    Abstract: Introduction: Tuberculosis and nontuberculous mycobacterial infections are notoriously difficult to treat, requiring long-courses of intensive multi-drug therapies associated with adverse side effects. To identify better therapeutics, whole cell screens ...

    Abstract Introduction: Tuberculosis and nontuberculous mycobacterial infections are notoriously difficult to treat, requiring long-courses of intensive multi-drug therapies associated with adverse side effects. To identify better therapeutics, whole cell screens have identified novel pharmacophores, a surprisingly high number of which target an essential lipid transporter known as MmpL3.
    Areas covered: This paper summarizes what is known about MmpL3, its mechanism of lipid transport and therapeutic potential, and provides an overview of the different classes of MmpL3 inhibitors currently under development. It further describes the assays available to study MmpL3 inhibition by these compounds.
    Expert opinion: MmpL3 has emerged as a target of high therapeutic value. Accordingly, several classes of MmpL3 inhibitors are currently under development with one drug candidate (SQ109) having undergone a Phase 2b clinical study. The hydrophobic character of most MmpL3 series identified to date seems to drive antimycobacterial potency resulting in poor bioavailability, which is a significant impediment to their development. There is also a need for more high-throughput and informative assays to elucidate the precise mechanism of action of MmpL3 inhibitors and drive the rational optimization of analogues.
    MeSH term(s) Humans ; Membrane Proteins ; Antitubercular Agents/pharmacology ; Mycobacterium tuberculosis ; Drug Design ; Lipids ; Bacterial Proteins
    Chemical Substances Membrane Proteins ; Antitubercular Agents ; Lipids ; Bacterial Proteins
    Language English
    Publishing date 2023-06-04
    Publishing country England
    Document type Journal Article ; Review ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 2259618-5
    ISSN 1746-045X ; 1746-0441
    ISSN (online) 1746-045X
    ISSN 1746-0441
    DOI 10.1080/17460441.2023.2218082
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  6. Article ; Online: Making sense of drug-efflux transporters in the physiological environment.

    Zgurskaya, Helen I / Adamiak, Justyna W / Leus, Inga V

    Current opinion in microbiology

    2022  Volume 69, Page(s) 102179

    Abstract: Bacterial drug-efflux transporters act synergistically with diffusion barriers of cellular membranes and other resistance mechanisms to protect cells from antibiotics and toxic metabolites. Their critical roles in clinical antibiotic and multidrug ... ...

    Abstract Bacterial drug-efflux transporters act synergistically with diffusion barriers of cellular membranes and other resistance mechanisms to protect cells from antibiotics and toxic metabolites. Their critical roles in clinical antibiotic and multidrug resistance are well established. In addition, a large body of evidence has been accumulated in support of their important contributions to bacterial growth and proliferation during infections. However, how these diverse functions of drug transporters are integrated at the level of bacterial cell physiology remains unclear. This opinion briefly summarizes the current understanding of substrate specificities and physiological roles of drug-efflux pumps from Resistance-Nodulation-Division (RND) superfamily of proteins in two ESKAPE pathogens Pseudomonas aeruginosa and Acinetobacter baumannii. Based on the analysis of phenotypic and transcriptomic studies in vitro and in vivo, we propose that RND pumps of Gram-negative bacteria fall into three categories: constitutively expressed, regulated, and silent. These three categories of efflux pumps participate in different physiological programs, which are not involved in the central metabolism and bacterial growth.
    MeSH term(s) Acinetobacter baumannii/genetics ; Anti-Bacterial Agents/metabolism ; Anti-Bacterial Agents/pharmacology ; Bacterial Proteins/genetics ; Bacterial Proteins/metabolism ; Drug Resistance, Multiple, Bacterial ; Gram-Negative Bacteria/genetics ; Gram-Negative Bacteria/metabolism ; Membrane Transport Proteins/genetics ; Membrane Transport Proteins/metabolism ; Pseudomonas aeruginosa/genetics ; Pseudomonas aeruginosa/metabolism
    Chemical Substances Anti-Bacterial Agents ; Bacterial Proteins ; Membrane Transport Proteins
    Language English
    Publishing date 2022-07-23
    Publishing country England
    Document type Journal Article ; Review ; Research Support, N.I.H., Extramural
    ZDB-ID 1418474-6
    ISSN 1879-0364 ; 1369-5274
    ISSN (online) 1879-0364
    ISSN 1369-5274
    DOI 10.1016/j.mib.2022.102179
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    Zs.A 5514: Show issues Location:
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    Zs.MG 51: Show issues

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  7. Article: Acinetobacter baumannii

    Leus, Inga V / Olvera, Marcela / Adamiak, Justyna W / Nguyen, Lauren L / Zgurskaya, Helen I

    Antibiotics (Basel, Switzerland)

    2023  Volume 13, Issue 1

    Abstract: Multidrug efflux transporters are major contributors to the antibiotic resistance ... ...

    Abstract Multidrug efflux transporters are major contributors to the antibiotic resistance of
    Language English
    Publishing date 2023-12-20
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2681345-2
    ISSN 2079-6382
    ISSN 2079-6382
    DOI 10.3390/antibiotics13010007
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  8. Article: Penetration through Outer Membrane and Efflux Potential in

    Kim, Choon / Tomoshige, Shusuke / Lee, Mijoon / Zgurskaya, Helen I / Mobashery, Shahriar

    Antibiotics (Basel, Switzerland)

    2023  Volume 12, Issue 2

    Abstract: The treatment of infections by Gram-negative bacteria remains a difficult clinical challenge. In the light of the dearth of discovery of novel antibiotics, one strategy that is being explored is the use of adjuvants to enhance antibacterial activities of ...

    Abstract The treatment of infections by Gram-negative bacteria remains a difficult clinical challenge. In the light of the dearth of discovery of novel antibiotics, one strategy that is being explored is the use of adjuvants to enhance antibacterial activities of existing antibiotics. One such adjuvant is bulgecin A, which allows for the lowering of minimal-inhibitory concentrations for β-lactam antibiotics. We have shown that bulgecin A inhibits three of the pseudomonal lytic transglycosylases in its mode of action, yet high concentrations are needed for potentiation activity. Herein, we document that bulgecin A is not a substrate for pseudomonal efflux pumps, whose functions could have been a culprit in the need for high concentrations. We present evidence that the penetration barrier into the periplasm is at the root of the need for high concentrations of bulgecin A in its potentiation of β-lactam antibiotics.
    Language English
    Publishing date 2023-02-09
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2681345-2
    ISSN 2079-6382
    ISSN 2079-6382
    DOI 10.3390/antibiotics12020358
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  9. Article ; Online: Nonadditive functional interactions between ligand-binding sites of the multidrug efflux pump AdeB from

    Leus, Inga V / Roberts, Sean R / Trinh, Anhthu / W Yu, Edward / Zgurskaya, Helen I

    Journal of bacteriology

    2023  Volume 206, Issue 1, Page(s) e0021723

    Abstract: Multidrug efflux is one of the major mechanisms of antibiotic resistance identified in clinical isolates of the human ... ...

    Abstract Multidrug efflux is one of the major mechanisms of antibiotic resistance identified in clinical isolates of the human pathogen
    MeSH term(s) Humans ; Acinetobacter baumannii/genetics ; Acinetobacter baumannii/metabolism ; Bacterial Proteins/metabolism ; Ligands ; Anti-Bacterial Agents/metabolism ; Membrane Transport Proteins/genetics ; Membrane Transport Proteins/metabolism ; Binding Sites ; Escherichia coli/metabolism ; Drug Resistance, Multiple, Bacterial/genetics ; Microbial Sensitivity Tests ; Multidrug Resistance-Associated Proteins/metabolism ; Escherichia coli Proteins/metabolism
    Chemical Substances Bacterial Proteins ; Ligands ; Anti-Bacterial Agents ; Membrane Transport Proteins ; AcrB protein, E coli ; Multidrug Resistance-Associated Proteins ; Escherichia coli Proteins
    Language English
    Publishing date 2023-10-18
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 2968-3
    ISSN 1098-5530 ; 0021-9193
    ISSN (online) 1098-5530
    ISSN 0021-9193
    DOI 10.1128/jb.00217-23
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  10. Article ; Online: Permeability barriers of Gram-negative pathogens.

    Zgurskaya, Helen I / Rybenkov, Valentin V

    Annals of the New York Academy of Sciences

    2019  Volume 1459, Issue 1, Page(s) 5–18

    Abstract: Most clinical antibiotics do not have efficacy against Gram-negative pathogens, mainly because these cells are protected by the permeability barrier comprising the two membranes with active efflux. The emergence of multidrug-resistant Gram-negative ... ...

    Abstract Most clinical antibiotics do not have efficacy against Gram-negative pathogens, mainly because these cells are protected by the permeability barrier comprising the two membranes with active efflux. The emergence of multidrug-resistant Gram-negative strains threatens the utility even of last resort therapeutic treatments. Significant efforts at different levels of resolution are currently focused on finding a solution to this nonpermeation problem and developing new approaches to the optimization of drug activities against multidrug-resistant pathogens. The exceptional efficiency of the Gram-negative permeability barrier is the result of a complex interplay between the two opposing fluxes of drugs across the two membranes. In this review, we describe the current state of understanding of the problem and the recent advances in theoretical and empirical approaches to characterization of drug permeation and active efflux in Gram-negative bacteria.
    MeSH term(s) Animals ; Anti-Bacterial Agents/metabolism ; Anti-Bacterial Agents/pharmacology ; Biological Transport/drug effects ; Biological Transport/physiology ; Drug Resistance, Multiple, Bacterial/drug effects ; Drug Resistance, Multiple, Bacterial/physiology ; Gram-Negative Bacteria/drug effects ; Gram-Negative Bacteria/metabolism ; Humans ; Permeability/drug effects
    Chemical Substances Anti-Bacterial Agents
    Language English
    Publishing date 2019-06-04
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, Non-P.H.S. ; Review
    ZDB-ID 211003-9
    ISSN 1749-6632 ; 0077-8923
    ISSN (online) 1749-6632
    ISSN 0077-8923
    DOI 10.1111/nyas.14134
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