István Köteles
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View article: Potent Fluorescent Probe for Target‐Engagement Studies of Allosteric Pyruvate Kinase Modulators
Potent Fluorescent Probe for Target‐Engagement Studies of Allosteric Pyruvate Kinase Modulators Open
Pyruvate kinases (PKs) are highly allosterically regulated enzymes that play a central role in cellular metabolism and are increasingly recognized as valuable therapeutic targets in cancer, metabolic diseases, and diabetes. Despite their b…
View article: Potent Fluorescent Probe for Target‐Engagement Studies of Allosteric Pyruvate Kinase Modulators
Potent Fluorescent Probe for Target‐Engagement Studies of Allosteric Pyruvate Kinase Modulators Open
Pyruvate kinases (PKs) are highly allosterically regulated enzymes that play a central role in cellular metabolism and are increasingly recognized as valuable therapeutic targets in cancer, metabolic diseases, and diabetes. Despite their b…
View article: Fluorescent binding assay for allosteric ligands of liver pyruvate kinase
Fluorescent binding assay for allosteric ligands of liver pyruvate kinase Open
Environment-sensitive fluorescent probes are indispensable tools for studying biological systems and advancing drug discovery. This study reports the development of 4-sulfamoyl-7-aminobenzoxadiazole (SBD)-based fluorescent probes for the a…
View article: Synthesis and physicochemical characterization of new potential haptens and their precursors with morphine skeleton
Synthesis and physicochemical characterization of new potential haptens and their precursors with morphine skeleton Open
Opiate analgetics are widely used therapeutic agents, but their side-effects can cause serious harm to users, and they are often abused for their euphoric effects. Their abuse is a serious healthcare problem worldwide, and in addition, pha…
View article: Opioid-Based Haptens: Development of Immunotherapy
Opioid-Based Haptens: Development of Immunotherapy Open
Over the past decades, extensive preclinical research has been conducted to develop vaccinations to protect against substance use disorder caused by opioids, nicotine, cocaine, and designer drugs. Morphine or fentanyl derivatives are small…
View article: Simultaneous Determination of Enantiomeric Purity and Organic Impurities of Dexketoprofen Using Reversed-Phase Liquid Chromatography—Enhancing Enantioselectivity through Hysteretic Behavior and Temperature-Dependent Enantiomer Elution Order Reversal on Polysaccharide Chiral Stationary Phases
Simultaneous Determination of Enantiomeric Purity and Organic Impurities of Dexketoprofen Using Reversed-Phase Liquid Chromatography—Enhancing Enantioselectivity through Hysteretic Behavior and Temperature-Dependent Enantiomer Elution Order Reversal on Polysaccharide Chiral Stationary Phases Open
A reversed-phase high-performance liquid chromatographic (HPLC) method was developed for the simultaneous determination of the potential impurities of dexketoprofen, including the distomer R-ketoprofen. After screening the separation capab…
View article: The Effect of the Particle Size Reduction on the Biorelevant Solubility and Dissolution of Poorly Soluble Drugs with Different Acid-Base Character
The Effect of the Particle Size Reduction on the Biorelevant Solubility and Dissolution of Poorly Soluble Drugs with Different Acid-Base Character Open
Particle size reduction is a commonly used process to improve the solubility and the dissolution of drug formulations. The solubility of a drug in the gastrointestinal tract is a crucial parameter, because it can greatly influence the bioa…
View article: Species-specific acid-base characterization of carnosine and homocarnosine using nuclear magnetic resonance
Species-specific acid-base characterization of carnosine and homocarnosine using nuclear magnetic resonance Open
Carnosine and homocarnosine have long been known to be important constituents of the human metabolome, performing pH- and redox homeostasis-related roles. These are the most important imidazole-containing 'small' chemical entities in biolo…
View article: Enantioseparation of solriamfetol and its major impurity phenylalaninol by capillary electrophoresis using sulfated gamma cyclodextrin
Enantioseparation of solriamfetol and its major impurity phenylalaninol by capillary electrophoresis using sulfated gamma cyclodextrin Open
R ‐solriamfetol is a recently approved drug used for the treatment of excessive sleepiness associated with narcolepsy and sleep apnea. Herein, a capillary electrophoretic method was developed, enabling the simultaneous analysis of the API …
View article: Synthesis of 3‐<i>O</i>‐Carboxyalkyl Morphine Derivatives and Characterization of Their Acid‐Base Properties
Synthesis of 3‐<i>O</i>‐Carboxyalkyl Morphine Derivatives and Characterization of Their Acid‐Base Properties Open
The C‐3 phenolic hydroxy group containing morphine derivatives (morphine, oxymorphone, naloxone, naltrexone) are excellent candidates for the synthesis of 3‐ O ‐functionalized molecules. Achieving free carboxylic group containing derivativ…
View article: Synthesis of Potential Haptens with Morphine Skeleton and Determination of Protonation Constants
Synthesis of Potential Haptens with Morphine Skeleton and Determination of Protonation Constants Open
Vaccination could be a promising alternative warfare against drug addiction and abuse. For this purpose, so-called haptens can be used. These molecules alone do not induce the activation of the immune system, this occurs only when they are…
View article: Vaccines against Drug Abuse: Morphine-Hapten Design and Synthesis
Vaccines against Drug Abuse: Morphine-Hapten Design and Synthesis Open
Drugs of abuse are small molecules that typically do not induce an antibody response following the administration. To induce antibodies against these kind of molecules, structural changes have to be made to obtain so called “haptens”. The …