Lukas Schulig
YOU?
Author Swipe
View article: Genomic and functional characterization of the L‑sorbose phosphotransferase system in high-risk <i>Escherichia coli</i> lineages
Genomic and functional characterization of the L‑sorbose phosphotransferase system in high-risk <i>Escherichia coli</i> lineages Open
Certain Escherichia coli strains belong to international high-risk clonal lineages exhibiting a combination of multidrug resistance, enhanced fitness, and increased virulence, posing major public health challenges. Investigation of charact…
View article: The divergent roles of tryptophans W354 and W217 in OCT1 transport: similar localization, distinct functions
The divergent roles of tryptophans W354 and W217 in OCT1 transport: similar localization, distinct functions Open
View article: Combined chiral–achiral supercritical fluid chromatography method for the impurity analysis of dapoxetine reveals insights in entropy-driven retention and acid-modulated selectivity
Combined chiral–achiral supercritical fluid chromatography method for the impurity analysis of dapoxetine reveals insights in entropy-driven retention and acid-modulated selectivity Open
Chiral analysis is an essential part of the development and quality control of enantiopure pharmaceuticals. Supercritical fluid chromatography (SFC) emerged as a powerful tool for the chiral separation of drugs, however, its implementation…
View article: Crystal structure of chloromethyl 2-[2-(2,6-dichlorophenylamino)phenyl]acetate
Crystal structure of chloromethyl 2-[2-(2,6-dichlorophenylamino)phenyl]acetate Open
The title compound, C 15 H 15 Cl 3 NO 2 , was synthesized from diclofenac and chloromethyl chlorosulfate under phase-transfer conditions, and crystallizes in the monoclinic space group P 2 1 / c . As a result of steric strain, the two adja…
View article: Drosera rotundifolia L. as E. coli biofilm inhibitor: Insights into the mechanism of action using proteomics/metabolomics and toxicity studies
Drosera rotundifolia L. as E. coli biofilm inhibitor: Insights into the mechanism of action using proteomics/metabolomics and toxicity studies Open
View article: Double the Double: Revisiting <scp>BCL11B</scp>'s Multimerization
Double the Double: Revisiting <span>BCL11B</span>'s Multimerization Open
The transcription factor B Cell Lymphoma/Leukemia 11B (BCL11B) exerts a bi‐directional function in cancer, with its role as an emerging therapeutic target in cancer treatment being particularly intriguing. BCL11B knockouts in cultured T ce…
View article: Targeting PARP-1 and DNA Damage Response Defects in Colorectal Cancer Chemotherapy with Established and Novel PARP Inhibitors
Targeting PARP-1 and DNA Damage Response Defects in Colorectal Cancer Chemotherapy with Established and Novel PARP Inhibitors Open
The DNA repair protein PARP-1 emerged as a valuable target in the treatment of tumor entities with deficiencies of BRCA1/2, such as breast cancer. More recently, the application of PARP inhibitors (PARPi) such as olaparib has been expanded…
View article: Structure-based mapping of the histone-binding pocket of KDM4D using functionalized tetrazole and pyridine core compounds
Structure-based mapping of the histone-binding pocket of KDM4D using functionalized tetrazole and pyridine core compounds Open
View article: Fexinidazole optimization: enhancing anti-leishmanial profile, metabolic stability and hERG safety
Fexinidazole optimization: enhancing anti-leishmanial profile, metabolic stability and hERG safety Open
Structure-guided optimization of fexinidazole led to analog ( S )-51, a promising lead compound with superior activity, improved metabolic stability, and enhanced hERG safety
View article: Structure‐Activity Relationships of Flupirtine Analogues for Liver Esterase‐Mediated Cleavage of the 4‐Fluorobenzylamine Moiety and Its Possible Relevance to Liver Toxicity
Structure‐Activity Relationships of Flupirtine Analogues for Liver Esterase‐Mediated Cleavage of the 4‐Fluorobenzylamine Moiety and Its Possible Relevance to Liver Toxicity Open
Flupirtine and retigabine were essential drugs to combat pain and epilepsy. However, the K v 7 potassium channel openers are fraught with hepatotoxicity and tissue discoloration, respectively, limiting their therapeutic value. Both adverse…
View article: Replacing the oxidation‐sensitive triaminoaryl chemotype of problematic K<sub>V</sub>7 channel openers: Exploration of a nicotinamide scaffold
Replacing the oxidation‐sensitive triaminoaryl chemotype of problematic K<sub>V</sub>7 channel openers: Exploration of a nicotinamide scaffold Open
K V 7 channel openers have proven their therapeutic value in the treatment of pain as well as epilepsy and, moreover, they hold the potential to expand into additional indications with unmet medical needs. However, the clinically validated…
View article: Carba Analogues of Flupirtine and Retigabine with Improved Oxidation Resistance and Reduced Risk of Quinoid Metabolite Formation
Carba Analogues of Flupirtine and Retigabine with Improved Oxidation Resistance and Reduced Risk of Quinoid Metabolite Formation Open
The K V 7 potassium channel openers flupirtine and retigabine have been valuable options in the therapy of pain and epilepsy. However, as a result of adverse reactions, both drugs are currently no longer in therapeutic use. The flupirtine‐…
View article: Extensively Drug-Resistant Klebsiella pneumoniae Counteracts Fitness and Virulence Costs That Accompanied Ceftazidime-Avibactam Resistance Acquisition
Extensively Drug-Resistant Klebsiella pneumoniae Counteracts Fitness and Virulence Costs That Accompanied Ceftazidime-Avibactam Resistance Acquisition Open
Extensively drug-resistant Klebsiella pneumoniae causing major outbreaks and severe infections has become a significant challenge for health care systems worldwide. Rapid resistance development against last-resort therapeutics like ceftazi…
View article: Modifications of the Triaminoaryl Metabophore of Flupirtine and Retigabine Aimed at Avoiding Quinone Diimine Formation
Modifications of the Triaminoaryl Metabophore of Flupirtine and Retigabine Aimed at Avoiding Quinone Diimine Formation Open
The potassium channel opening drugs flupirtine and retigabine have been withdrawn from the market due to occasional drug-induced liver injury (DILI) and tissue discoloration, respectively. While the mechanism underlying DILI after prolonge…
View article: Correlation Analysis of Protein Expression of 10 HDAC/Sirtuin Isoenzymes with Sensitivities of 23 Anticancer Drugs in 17 Cancer Cell Lines and Potentiation of Drug Activity by Co-Treatment with HDAC Inhibitors
Correlation Analysis of Protein Expression of 10 HDAC/Sirtuin Isoenzymes with Sensitivities of 23 Anticancer Drugs in 17 Cancer Cell Lines and Potentiation of Drug Activity by Co-Treatment with HDAC Inhibitors Open
Inhibiting the activity of histone deacetylase (HDAC) is an ongoing strategy in anticancer therapy. However, to our knowledge, the relationships between the expression of HDAC proteins and the antitumor drug sensitivity of cancer cells hav…
View article: Pneumococcal Extracellular Serine Proteases: Molecular Analysis and Impact on Colonization and Disease
Pneumococcal Extracellular Serine Proteases: Molecular Analysis and Impact on Colonization and Disease Open
The pathobiont Streptococcus pneumoniae causes life-threatening diseases, including pneumonia, sepsis, meningitis, or non-invasive infections such as otitis media. Serine proteases are enzymes that have been emerged during evolution as one…
View article: Nuclear import of BCL11B is mediated by a classical nuclear localization signal and not the Krüppel-like zinc fingers
Nuclear import of BCL11B is mediated by a classical nuclear localization signal and not the Krüppel-like zinc fingers Open
The Krüppel-like transcription factor (KLF) BCL11B is characterized by a wide tissue distribution and crucial functions in key developmental and cellular processes, as well as in various pathologies including cancer and HIV infection. Alth…
View article: The EyeFlowCell: Development of a 3D-Printed Dissolution Test Setup for Intravitreal Dosage Forms
The EyeFlowCell: Development of a 3D-Printed Dissolution Test Setup for Intravitreal Dosage Forms Open
An in vitro dissolution model, the so-called EyeFlowCell (EFC), was developed to test intravitreal dosage forms, simulating parameters such as the gel-like consistency of the vitreous body. The developed model consists of a stereolithograp…
View article: Supercritical fluid extraction–supercritical fluid chromatography of saliva: Single‐quadrupole mass spectrometry monitoring of caffeine for gastric emptying studies<sup>†</sup>
Supercritical fluid extraction–supercritical fluid chromatography of saliva: Single‐quadrupole mass spectrometry monitoring of caffeine for gastric emptying studies<sup>†</sup> Open
Saliva is an attractive sampling matrix for measuring various endogenous and exogeneous substances but requires sample treatment prior to chromatographic analysis. Exploiting supercritical CO 2 for both extraction and chromatography simpli…
View article: A Hypothesized Mechanism for Chronic Pancreatitis Caused by the N34S Mutation of Serine Protease Inhibitor Kazal-Type 1 Based on Conformational Studies
A Hypothesized Mechanism for Chronic Pancreatitis Caused by the N34S Mutation of Serine Protease Inhibitor Kazal-Type 1 Based on Conformational Studies Open
Based on our result, a hypothesis is formulated that explains the development of chronic pancreatitis through accelerated digestion of the mutant by trypsin.
View article: Unveiling the N-Terminal Homodimerization of BCL11B by Hybrid Solvent Replica-Exchange Simulations
Unveiling the N-Terminal Homodimerization of BCL11B by Hybrid Solvent Replica-Exchange Simulations Open
Transcription factors play a crucial role in regulating biological processes such as cell growth, differentiation, organ development and cellular signaling. Within this group, proteins equipped with zinc finger motifs (ZFs) represent the l…
View article: Activation of Sirtuin 2 Inhibitors Employing Photoswitchable Geometry and Aqueous Solubility
Activation of Sirtuin 2 Inhibitors Employing Photoswitchable Geometry and Aqueous Solubility Open
Because isoenzymes of the experimentally and therapeutically extremely relevant sirtuin family show high similarity, addressing the unique selectivity pocket of sirtuin 2 is a promising strategy towards selective inhibitors. An unrelated a…
View article: Subcritical Fluid Chromatography at Sub-Ambient Temperatures for the Chiral Resolution of Ketamine Metabolites with Rapid-Onset Antidepressant Effects
Subcritical Fluid Chromatography at Sub-Ambient Temperatures for the Chiral Resolution of Ketamine Metabolites with Rapid-Onset Antidepressant Effects Open
Chiral metabolites of ketamine exerting rapid-onset yet sustained antidepressant effects may be marketed directly in the future, but require chemo- and enantio-selective chromatographic methods for quality assurance and control. The chroma…
View article: Flupirtine Analogues: Explorative Synthesis and Influence of Chemical Structure on K<sub>V</sub>7.2/K<sub>V</sub>7.3 Channel Opening Activity
Flupirtine Analogues: Explorative Synthesis and Influence of Chemical Structure on K<sub>V</sub>7.2/K<sub>V</sub>7.3 Channel Opening Activity Open
Neuronal voltage‐gated potassium channels K V 7.2/K V 7.3 are sensitive to small‐molecule drugs such as flupirtine, even though physiological response occurs in the absence of ligands. Clinically, prolonged use of flupirtine as a pain medi…