1,363 results found
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Coupling of remote alternating-access transport mechanisms for protons and substrates in the multidrug efflux pump AcrB

    Thomas Eicher et al.
    A transport mechanism is uncovered in the major drug-efflux system in E. coli involving two remote alternating-access conformational cycles, which could provide the basis for the development of allosteric inhibitors against multidrug resistance.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Structural basis of nucleoside and nucleoside drug selectivity by concentrative nucleoside transporters

    Zachary Lee Johnson et al.
    Studies of the substrate selectivity of concentrative nucleoside transporters provide proof of principle for structure-based improvement of drug delivery by these transporters.
    1. Structural Biology and Molecular Biophysics

    An allosteric transport mechanism for the AcrAB-TolC multidrug efflux pump

    Zhao Wang et al.
    The tripartite drug efflux pump AcrA-AcrB-TolC, representative of a wide group of pumps from Gram-negative bacteria, enters a transport-competent state through long-distance conformational changes that switch the channel from a closed to an open state.
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Energetics and conformational pathways of functional rotation in the multidrug transporter AcrB

    Yasuhiro Matsunaga et al.
    High-performance computing simulations reveal how two remote sites in the multidrug transporter AcrB work together for drug extrusion using the proton-motive force.
    1. Cell Biology

    Mucosal absorption of therapeutic peptides by harnessing the endogenous sorting of glycosphingolipids

    Maria Daniela Garcia-Castillo et al.
    Non-native synthetic short-chain glycosphingolipids fused to GLP-1 enable intestinal absorption with high bioavailability in vivo.
    1. Cell Biology

    Duodenum Intestine-Chip for preclinical drug assessment in a human relevant model

    Magdalena Kasendra et al.
    Combining Organs-on-Chips technology with adult intestinal organoids provides an improved model of human duodenum and a new platform for preclinical drug assessment.
    1. Biochemistry and Chemical Biology
    2. Microbiology and Infectious Disease

    Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei

    Ali H Alghamdi et al.
    Study of TbAQP2 adaptations and substrate interactions shows how this aquaglyceroporin enables cellular entry of large antimicrobial agents in Trypanosoma brucei.
    1. Epidemiology and Global Health
    2. Microbiology and Infectious Disease

    Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent

    Hideo Imamura et al.
    Genome sequencing reveals the evolution and epidemiology of Leishmania donovani in the Indian subcontinent, where epidemics have caused up to 30,000 deaths per year.
    1. Structural Biology and Molecular Biophysics

    Inducing conformational preference of the membrane protein transporter EmrE through conservative mutations

    Maureen Leninger et al.
    Conservative mutations within a secondary active transport protein influenced the conformational equilibrium probed using NMR spectroscopy which correlated to the functional output in vivo.
    1. Biochemistry and Chemical Biology

    Thermodynamic evidence for a dual transport mechanism in a POT peptide transporter

    Joanne L Parker et al.
    Two thermodynamically distinct transport mechanisms operating within the same binding site explains the remarkable promiscuity of POT family transporters towards peptide and drug ligands.

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