Explanipedia

Antibiotic–Polycationic Peptide Conjugation as an Effective Strategy to Overcome Daptomycin Resistance (Adv. Therap. 5/2025) Open

Sari Rasheed, Florian Umstätter, Eric Mühlberg, Barbro Beijer, Tobias Hertlein , et al. · 2025

Antibiotic–Polycationic Peptide Conjugation as an Effective Strategy to Overcome Daptomycin Resistance Open

Sari Rasheed, Florian Umstätter, Eric Mühlberg, Barbro Beijer, Tobias Hertlein , et al. · 2025

The benefit that antibiotics confer to the welfare of mankind is threatened by bacterial resistance. Resistance to daptomycin, a cyclic lipopeptide frequently used for the treatment of complicated bacteremia, is a prime example of this ala…

Conjugation of Polycationic Peptides Extends the Efficacy Spectrum of β‐Lactam Antibiotics Open

Julia Werner, Florian Umstätter, Manuel Ben Böhmann, Katharina Müller, Barbro Beijer , et al. · 2024

Antibiotic‐resistant enterococci represent a significant global health challenge. Unfortunately, most β‐lactam antibiotics are not applicable for enterococcal infections due to intrinsic resistance. To extend their antimicrobial spectrum, …

Oral Delivery of the Vancomycin Derivative FU002 by a Surface‐Modified Liposomal Nanocarrier Open

Julia Werner, Florian Umstätter, Tobias Hertlein, Eric Mühlberg, Barbro Beijer , et al. · 2024

Oral delivery of peptide therapeutics faces multiple challenges due to their instability in the gastrointestinal tract and low permeation capability. In this study, the aim is to develop a liposomal nanocarrier formulation to enable the or…

Improved pharmacokinetics and enhanced efficacy of the vancomycin derivative FU002 using a liposomal nanocarrier Open

Julia Werner, Florian Umstätter, Tobias Hertlein, Barbro Beijer, Christian Kleist , et al. · 2023

Antibiotic resistance still represents a global health concern which diminishes the pool of effective antibiotics. With the vancomycin derivative FU002, we recently reported a highly potent substance active against Gram-positive bacteria w…

Next-generation humanized NSG-SGM3 mice are highly susceptible to Staphylococcus aureus infection Open

Sophia Hung, Amelie Kasperkowitz, Florian Kurz, Liane Dreher, Joachim Diessner , et al. · 2023

Humanized hemato-lymphoid system mice, or humanized mice, emerged in recent years as a promising model to study the course of infection of human-adapted or human-specific pathogens. Though Staphylococcus aureus infects and colonizes a vari…

Novel Effective Fluorinated Benzothiophene-Indole Hybrid Antibacterials against S. aureus and MRSA Strains Open

Marius Seethaler, Tobias Hertlein, Elisa Hopke, Paul Köhling, Knut Ohlsen , et al. · 2022

Increasing antibacterial drug resistance threatens global health, unfortunately, however, efforts to find novel antibacterial agents have been scaled back by the pharmaceutical industry due to concerns about a poor return on investment. Ne…

MRSA Infection in the Thigh Muscle Leads to Systemic Disease, Strong Inflammation, and Loss of Human Monocytes in Humanized Mice Open

Sophia Hung, Liane Dreher, Joachim Diessner, Štefan Schwarz, Knut Ohlsen , et al. · 2022

MRSA (Methicillin-resistant Staphylococcus aureus ) is the second-leading cause of deaths by antibiotic-resistant bacteria globally, with more than 100,000 attributable deaths annually. Despite the high urgency to develop a vaccine to cont…

Impact of Linker Modification and PEGylation of Vancomycin Conjugates on Structure-Activity Relationships and Pharmacokinetics Open

Florian Umstätter, Julia Werner, Leah Zerlin, Eric Mühlberg, Christian Kleist , et al. · 2022

As multidrug-resistant bacteria represent a concerning burden, experts insist on the need for a dramatic rethinking on antibiotic use and development in order to avoid a post-antibiotic era. New and rapidly developable strategies for antim…

Novel Small-Molecule Hybrid-Antibacterial Agents against S. aureus and MRSA Strains Open

Robin Gehrmann, Tobias Hertlein, Elisa Hopke, Knut Ohlsen, Michael Lalk , et al. · 2021

Ongoing resistance developments against antibiotics that also affect last-resort antibiotics require novel antibacterial compounds. Strategies to discover such novel structures have been dimerization or hybridization of known antibacterial…

Intracellular Staphylococcus aureus employs the cysteine protease staphopain A to induce host cell death in epithelial cells Open

Kathrin Stelzner, Aziza Boyny, Tobias Hertlein, Aneta Sroka, Adriana Moldovan , et al. · 2021

Staphylococcus aureus is a major human pathogen, which can invade and survive in non-professional and professional phagocytes. Uptake by host cells is thought to contribute to pathogenicity and persistence of the bacterium. Upon internaliz…

Overcoming the Mucosal Barrier: Tetraether Lipid‐Stabilized Liposomal Nanocarriers Decorated with Cell‐Penetrating Peptides Enable Oral Delivery of Vancomycin Open

Philipp Uhl, Max Sauter, Tobias Hertlein, Dominik Witzigmann, Flavia Laffleur , et al. · 2021

Despite the high medical need for oral peptide delivery, instability in the gastrointestinal tract and low mucosal permeation still impede this preferred route of administration. Herein, a liposomal nanocarrier combining two self‐reliant s…

Corrigendum: Vancomycin Resistance is Overcome by Conjugation of Polycationic Peptides Open

Florian Umstätter, Cornelius Domhan, Tobias Hertlein, Knut Ohlsen, Eric Mühlberg , et al. · 2020

A vancomycin-arginine conjugate that is effective against Gram-negative bacteria, [1] and a D-octaarginine conjugate of vancomycin that eliminates biofilm-associated MRSA in a murine wound infection model, MRSA persister cells, and vancomy…

Berichtigung: Überwindung von Vancomycinresistenzen durch Modifikation mit polykationischen Peptiden Open

Florian Umstätter, Cornelius Domhan, Tobias Hertlein, Knut Ohlsen, Eric Mühlberg , et al. · 2020

Vancomycin-Lipopeptide Conjugates with High Antimicrobial Activity on Vancomycin-Resistant Enterococci Open

Eric Mühlberg, Florian Umstätter, Cornelius Domhan, Tobias Hertlein, Knut Ohlsen , et al. · 2020

Multidrug-resistant bacteria represent one of the most important health care problems worldwide. While there are numerous drugs available for standard therapy, there are only a few compounds capable of serving as a last resort for severe i…

Graphisches Inhaltsverzeichnis: Angew. Chem. 23/2020 Open

Lena Scherthan, Alan Powell, Volker Schünemann, Carmen Leitner, Marion Schulz , et al. · 2020

The interpretation of the chemical bond in NaBH 3À as a dative bond Na À !BH 3 proposed by Liu et al. is questioned.The dissociation products are Na À and BH 3 but the nature of the bond changes during the bond formation from dative intera…

Innenrücktitelbild: Überwindung von Vancomycinresistenzen durch Modifikation mit polykationischen Peptiden (Angew. Chem. 23/2020) Open

Florian Umstätter, Cornelius Domhan, Tobias Hertlein, Knut Ohlsen, Eric Mühlberg , et al. · 2020

Bakterielle Resistenzen drohen, die Errungenschaften der Antibiotikatherapie zunichte zu machen. Wie P. Uhl et al. in ihrer Zuschrift auf S. 8908 erläutern, konnte am Klinikum Heidelberg mit Peptid-Konjugaten eine tausendfache Aktivitätsst…

Inside Back Cover: Vancomycin Resistance Is Overcome by Conjugation of Polycationic Peptides (Angew. Chem. Int. Ed. 23/2020) Open

Florian Umstätter, Cornelius Domhan, Tobias Hertlein, Knut Ohlsen, Eric Mühlberg , et al. · 2020

Bacterial resistance threatens to destroy the achievements of antibiotic therapy. As P. Uhl and co-workers report in their Communication on page 8823, a 1000-fold increase in the activity of the reserve antibiotic vancomycin was achieved b…

Überwindung von Vancomycinresistenzen durch Modifikation mit polykationischen Peptiden Open

Florian Umstätter, Cornelius Domhan, Tobias Hertlein, Knut Ohlsen, Eric Mühlberg , et al. · 2020

Die zunehmende Prävalenz von Resistenzen bei Bakterien gegen Glykopeptid‐Antibiotika macht auch vor Vancomycin nicht halt. Um die ursprünglich hohe Effektivität gegen diese resistenten Bakterien wieder zu erzielen, wurden hier polykationis…

Vancomycin Resistance Is Overcome by Conjugation of Polycationic Peptides Open

Florian Umstätter, Cornelius Domhan, Tobias Hertlein, Knut Ohlsen, Eric Mühlberg , et al. · 2020

Multidrug‐resistant bacteria represent one of the biggest challenges facing modern medicine. The increasing prevalence of glycopeptide resistance compromises the efficacy of vancomycin, for a long time considered as the last resort for the…

Intracellular<i>Staphylococcus aureus</i>employs the cysteine protease staphopain A to induce host cell death in epithelial cells Open

Kathrin Stelzner, Tobias Hertlein, Aneta Sroka, Adriana Moldovan, Kerstin Paprotka , et al. · 2020

Staphylococcus aureus is a major human pathogen, which can invade and survive in non-professional and professional phagocytes. Intracellularity is thought to contribute to pathogenicity and persistence of the bacterium. Upon internalizatio…

Novel Small-molecule Antibacterials against Gram-positive Pathogens of Staphylococcus and Enterococcus Species Open

Marius Seethaler, Tobias Hertlein, Björn Wecklein, Alba Ymeraj, Knut Ohlsen , et al. · 2019

Defeat of the antibiotic resistance of pathogenic bacteria is one great challenge today and for the future. In the last century many classes of effective antibacterials have been developed, so that upcoming resistances could be met with no…

MpsAB is important for Staphylococcus aureus virulence and growth at atmospheric CO2 levels Open

Sook‐Ha Fan, Patrick Ebner, Sebastian Reichert, Tobias Hertlein, Susanne Zabel , et al. · 2019

Induced Pluripotent Stem Cell-Derived Brain Endothelial Cells as a Cellular Model to Study Neisseria meningitidis Infection Open

Sara F. Martins Gomes, Alexander J. Westermann, Till Sauerwein, Tobias Hertlein, Konrad U. Förstner , et al. · 2019

Meningococcal meningitis is a severe central nervous system infection that occurs when Neisseria meningitidis (Nm) penetrates brain endothelial cells (BECs) of the meningeal blood-cerebrospinal fluid barrier. As a human-speci…

Inactivation of farR Causes High Rhodomyrtone Resistance and Increased Pathogenicity in Staphylococcus aureus Open

Minh‐Thu Nguyen, Jongkon Saising, Paula M. Tribelli, Mulugeta Nega, Seydina M. Diene , et al. · 2019

Rhodomyrtone (Rom) is an acylphloroglucinol antibiotic originally isolated from leaves of Rhodomyrtus tomentosa. Rom targets the bacterial membrane and is active against a wide range of Gram-positive bacteria but the exact mode of a…

Antistaphylococcal evaluation of indole–naphthalene hybrid analogs Open

Kerolos Ashraf, Kaveh Yasrebi, Emmanuel T. Adeniyi, Tobias Hertlein, Knut Ohlsen , et al. · 2019

Resistance developments against established antibiotics are an emerging problem for antibacterial therapies. Infections with Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) have become more difficult to treat…

Antistaphylococcal evaluation of indole–naphthalene hybrid analogs Open

Kerolos Ashraf, Kaveh Yasrebi, Adeniyi ET, Tobias Hertlein, Knut Ohlsen , et al. · 2019

Kerolos Ashraf,1 Kaveh Yasrebi,1 Emmanuel Tola Adeniyi,2 Tobias Hertlein,2 Knut Ohlsen,2 Michael Lalk,3 Frank Erdmann,1 Andreas Hilgeroth1 1Institute of Pharmacy, Martin Luther University Halle-Wittenberg, Halle, Germany; 2Institute of Mol…

Bringing together what belongs together: Optimizing murine infection models by using mouse-adapted Staphylococcus aureus strains Open

Patricia Trübe, Tobias Hertlein, Daniel M. Mrochen, Daniel Schulz, Ilka Jorde , et al. · 2018

Inhibition of Rho Activity Increases Expression of SaeRS-Dependent Virulence Factor Genes in Staphylococcus aureus, Showing a Link between Transcription Termination, Antibiotic Action, and Virulence Open

Anna Nagel, Stephan Michalik, Michel Débarbouillé, Tobias Hertlein, Manuela Gesell Salazar , et al. · 2018

The major human pathogen Staphylococcus aureus is a widespread commensal bacterium but also the most common cause of nosocomial infections. It adapts to the different host niches through a complex gene regulatory network. We show here that…

Metabolic conversion of CI-1040 turns a cellular MEK-inhibitor into an antibacterial compound Open

Christin Bruchhagen, Marcel Jarick, Carolin Mewis, Tobias Hertlein, Silke Niemann , et al. · 2018

Influenza virus (IV) infections cause severe respiratory illnesses that can be complicated by bacterial super-infections. Previously, we identified the cellular Raf-MEK-ERK cascade as a promising antiviral target. Inhibitors of MEK, such a…

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