Search Results - "Kuder, Kamil J"
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Perry Disease: Current Outlook and Advances in Drug Discovery Approach to Symptomatic Treatment
Published in International journal of molecular sciences (01-10-2024)“…Perry disease (PeD) is a rare, neurodegenerative, genetic disorder inherited in an autosomal dominant manner. The disease manifests as parkinsonism, with…”
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Structure Prediction, Evaluation, and Validation of GPR18 Lipid Receptor Using Free Programs
Published in International journal of molecular sciences (18-07-2022)“…The GPR18 receptor, often referred to as the N-arachidonylglycine receptor, although assigned (along with GPR55 and GPR119) to the new class A GPCR…”
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The Potent and Selective Histamine H3 Receptor Antagonist E169 Counteracts Cognitive Deficits and Mitigates Disturbances in the PI3K/AKT/GSK-3β Signaling Pathway in MK801-Induced Amnesia in Mice
Published in International journal of molecular sciences (01-08-2023)“…The role of histamine H3 receptors (H3Rs) in memory and the prospective of H3R antagonists in pharmacological control of neurodegenerative disorders, e.g.,…”
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Discovery of Potential, Dual-Active Histamine H3 Receptor Ligands with Combined Antioxidant Properties
Published in Molecules (Basel, Switzerland) (15-04-2021)“…In an attempt to find new dual acting histamine H3 receptor (H3R) ligands, we designed a series of compounds, structurally based on previously described in our…”
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AR71, Histamine H3 Receptor Ligand—In Vitro and In Vivo Evaluation (Anti-Inflammatory Activity, Metabolic Stability, Toxicity, and Analgesic Action)
Published in International journal of molecular sciences (01-08-2024)“…The future of therapy for neurodegenerative diseases (NDs) relies on new strategies targeting multiple pharmacological pathways. Our research led to obtaining…”
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Anti-Inflammatory Activities of 8-Benzylaminoxanthines Showing High Adenosine A2A and Dual A1/A2A Receptor Affinity
Published in International journal of molecular sciences (05-09-2023)“…Chronic inflammation plays an important role in the development of neurodegenerative diseases, such as Parkinson’s disease (PD). In the present study, we…”
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Benzophenone Derivatives with Histamine H3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer’s Disease
Published in Molecules (Basel, Switzerland) (28-12-2022)“…The multitarget-directed ligands demonstrating affinity to histamine H3 receptor and additional cholinesterase inhibitory potency represent a promising…”
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Fluorescent GPCR ligands as new tools in pharmacology-update, years 2008-early 2014
Published in Current medicinal chemistry (01-01-2014)“…The robust of fluorescent techniques to study the ligand-receptor interaction followed by rapidly developing fluorescence imaging techniques resulted in a…”
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Histamine H3 Receptor Ligands—KSK-59 and KSK-73—Reduce Body Weight Gain in a Rat Model of Excessive Eating
Published in Pharmaceuticals (Basel, Switzerland) (25-10-2021)“…Noting the worldwide rapid increase in the prevalence of overweight and obesity new effective drugs are now being sought to combat these diseases. Histamine H3…”
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Docking Foundations: From Rigid to Flexible Docking
Published in Methods in molecular biology (Clifton, N.J.) (2024)“…Despite the development of methods for the experimental determination of protein structures, the dissonance between the number of known sequences and their…”
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Dual-targeting Approach on Histamine H 3 and Sigma-1 Receptor Ligands as Promising Pharmacological Tools in the Treatment of CNS-linked Disorders
Published in Current medicinal chemistry (2021)“…With the recent market approval of Pitolisant (Wakix®), the interest in clinical application for novel multifunctional histamine H receptor antagonists has…”
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12
Machine Learning Methods in Protein-Protein Docking
Published in Methods in molecular biology (Clifton, N.J.) (2024)“…An exponential increase in the number of publications that address artificial intelligence (AI) usage in life sciences has been noticed in recent years, while…”
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The histamine H3 receptor inverse agonist pitolisant reduces body weight in obese mice
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-08-2018)“…The pharmacological profile of pitolisant, a histamine H 3 receptor antagonist/inverse agonist, indicates that this compound might reduce body weight and…”
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N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H 3 receptor and cancer resistance proteins
Published in Bioorganic & medicinal chemistry letters (15-11-2020)“…Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment, the ability of novel histamine H…”
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N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H3 receptor and cancer resistance proteins
Published in Bioorganic & medicinal chemistry letters (15-11-2020)“…[Display omitted] •ABCB1 efflux pump modulating assays in mouse T-lymphoma cells for compounds 1–18.•Cytotoxicity and proliferation assays in PAR and MDR…”
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Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands
Published in European journal of medicinal chemistry (25-05-2018)“…As a continuation of our search for novel histamine H3 receptor ligands, a series of twenty four new tert-butyl and tert-pentyl phenoxyalkylamine derivatives…”
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Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent
Published in European journal of medicinal chemistry (05-03-2021)“…A series of 4-pyridylpiperazine derivatives with varying regulatory region substituents proved to be potent histamine H3 receptor (H3R) ligands in the…”
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Structural modifications in the distal, regulatory region of histamine H 3 receptor antagonists leading to the identification of a potent anti-obesity agent
Published in European journal of medicinal chemistry (05-03-2021)“…A series of 4-pyridylpiperazine derivatives with varying regulatory region substituents proved to be potent histamine H receptor (H R) ligands in the nanomolar…”
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The histamine H 3 receptor inverse agonist pitolisant reduces body weight in obese mice
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-08-2018)“…The pharmacological profile of pitolisant, a histamine H receptor antagonist/inverse agonist, indicates that this compound might reduce body weight and…”
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Optimization and preclinical evaluation of novel histamine H 3 receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives
Published in Bioorganic & medicinal chemistry (15-12-2018)“…As a continuation of our search for novel histamine H receptor ligands, a series of new acetyl and propionyl phenoxyalkylamine derivatives (2-25) was…”
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