Search Results - "Lang, Pauline A."
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High-throughput screen with the l,d-transpeptidase LdtMt2 of Mycobacterium tuberculosis reveals novel classes of covalently reacting inhibitors
Published in Chemical science (Cambridge) (05-07-2023)“…Disruption of bacterial cell wall biosynthesis in Mycobacterium tuberculosis is a promising target for treating tuberculosis. The l,d-transpeptidase LdtMt2,…”
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Biochemical and crystallographic studies of l,d-transpeptidase 2 from Mycobacterium tuberculosis with its natural monomer substrate
Published in Communications biology (18-09-2024)“…The essential l,d -transpeptidase of Mycobacterium tuberculosis (Ldt Mt2 ) catalyses the formation of 3 → 3 cross-links in cell wall peptidoglycan and is a…”
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3
Bicyclic Boronates as Potent Inhibitors of AmpC, the Class C β-Lactamase from Escherichia coli
Published in Biomolecules (Basel, Switzerland) (12-06-2020)“…Resistance to β-lactam antibacterials, importantly via production of β-lactamases, threatens their widespread use. Bicyclic boronates show promise as…”
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4
Anaerobic fixed-target serial crystallography
Published in IUCrJ (01-09-2020)“…Cryogenic X-ray diffraction is a powerful tool for crystallographic studies on enzymes including oxygenases and oxidases. Amongst the benefits that…”
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5
Will morphing boron-based inhibitors beat the β-lactamases?
Published in Current opinion in chemical biology (01-06-2019)“…The β-lactams remain the most important antibacterials, but their use is increasingly compromised by resistance, importantly by β-lactamases. Although β-lactam…”
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Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases
Published in Journal of medicinal chemistry (26-09-2019)“…The bicyclic boronate VNRX-5133 (taniborbactam) is a new type of β-lactamase inhibitor in clinical development. We report that VNRX-5133 inhibits…”
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Molecular Basis of Class A β-Lactamase Inhibition by Relebactam
Published in Antimicrobial agents and chemotherapy (01-10-2019)“…β-Lactamase production is the major β-lactam resistance mechanism in Gram-negative bacteria. β-Lactamase inhibitors (BLIs) efficacious against serine…”
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Studies on enmetazobactam clarify mechanisms of widely used β-lactamase inhibitors
Published in Proceedings of the National Academy of Sciences - PNAS (03-05-2022)“…β-Lactams are the most important class of antibacterials, but their use is increasingly compromised by resistance, most importantly via serine β-lactamase…”
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Structural Investigations of the Inhibition of Escherichia coli AmpC β-Lactamase by Diazabicyclooctanes
Published in Antimicrobial agents and chemotherapy (20-01-2021)“…β-Lactam antibiotics are presently the most important treatments for infections by pathogenic , but their use is increasingly compromised by β-lactamases,…”
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High-throughput screen with the l,d-transpeptidase Ldt Mt2 of Mycobacterium tuberculosis reveals novel classes of covalently reacting inhibitors
Published in Chemical science (Cambridge) (05-07-2023)“…Disruption of bacterial cell wall biosynthesis in is a promising target for treating tuberculosis. The l,d-transpeptidase Ldt , which is responsible for the…”
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Journal Article -
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How Clavulanic Acid Inhibits Serine β‐Lactamases
Published in Chembiochem : a European journal of chemical biology (18-11-2024)“…Clavulanic acid is a medicinally important inhibitor of serine β‐lactamases (SBLs). We report studies on the mechanisms by which clavulanic acid inhibits…”
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Pretargeted PET Imaging with a TCO-Conjugated Anti-CD44v6 Chimeric mAb U36 and [ 89 Zr]Zr-DFO-PEG 5 -Tz
Published in Bioconjugate chemistry (18-05-2022)“…The recent advances in the production of engineered antibodies have facilitated the development and application of tailored, target-specific antibodies…”
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An on-demand, drop-on-drop method for studying enzyme catalysis by serial crystallography
Published in Nature communications (22-07-2021)“…Serial femtosecond crystallography has opened up many new opportunities in structural biology. In recent years, several approaches employing light-inducible…”
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Pretargeted PET Imaging with a TCO-Conjugated Anti-CD44v6 Chimeric mAb U36 and [89Zr]Zr-DFO-PEG5‑Tz
Published in Bioconjugate chemistry (18-05-2022)“…The recent advances in the production of engineered antibodies have facilitated the development and application of tailored, target-specific antibodies…”
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15
Mapping the Hydrophobic Substrate Binding Site of Phenylalanine Ammonia-Lyase from Petroselinum crispum
Published in ACS catalysis (06-09-2019)“…Modification of the hydrophobic binding pocket of phenylalanine ammonia-lyase from Petroselinum crispum (PcPAL) enables increased activity and selectivity…”
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Targeting the Mycobacterium tuberculosis transpeptidase Ldt Mt2 with cysteine-reactive inhibitors including ebselen
Published in Chemical communications (Cambridge, England) (22-08-2019)“…The l,d-transpeptidases (Ldts) are promising antibiotic targets for treating tuberculosis. We report screening of cysteine-reactive inhibitors against LdtMt2…”
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X-ray free-electron laser studies reveal correlated motion during isopenicillin N synthase catalysis
Published in Science advances (01-08-2021)“…Isopenicillin synthase (IPNS) catalyzes the unique reaction of l-δ-(α-aminoadipoyl)-l-cysteinyl-d-valine (ACV) with dioxygen giving isopenicillin (IPN), the…”
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Cover Feature: How Clavulanic Acid Inhibits Serine β‐Lactamases (ChemBioChem 22/2024)
Published in Chembiochem : a European journal of chemical biology (18-11-2024)“…Clavulanic acid is a densely functionalized low mass (C8H9NO5) drug, which is used to protect penicillins and other β‐lactam antibiotics from hydrolysis by…”
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Journal Article -
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High-throughput screen with the -transpeptidase Ldt of reveals novel classes of covalently reacting inhibitors
Published in Chemical science (Cambridge) (05-07-2023)“…Disruption of bacterial cell wall biosynthesis in Mycobacterium tuberculosis is a promising target for treating tuberculosis. The l,d -transpeptidase Ldt Mt2 ,…”
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Journal Article -
20
Bicyclic Boronates as Potent Inhibitors of AmpC, the Class C [beta]-Lactamase from Escherichia coli
Published in Biomolecules (Basel, Switzerland) (01-06-2020)“…Resistance to [beta]-lactam antibacterials, importantly via production of [beta]-lactamases, threatens their widespread use. Bicyclic boronates show promise as…”
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Journal Article