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Acenocoumarol --- Mixed Function Oxygenases --- Ligases --- Warfarin --- Carboxy-Lyases --- Vitamin K --- pharmacology --- metabolism --- metabolism --- pharmacology --- metabolism --- metabolism

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Pharmacogenomics is one of the emerging approaches to precision medicine, tailoring drug selection and dosing to the patient’s genetic features. In recent years, several pharmacogenetic guidelines have been published by international scientific consortia, but the uptake in clinical practice is still poor. Many coordinated international efforts are ongoing in order to overcome the existing barriers to pharmacogenomic implementation. On the other hand, existing validated pharmacogenomic markers can explain only a minor part of the observed clinical variability in the therapeutic outcome. New investigational approaches are warranted, including a study of the pharmacogenomic role of the immune system genetics and of previously neglected rare genetic variants, reported to account for a large part of inter-individual variability in drug metabolism. In this book, we have collected a series of articles covering many aspects of pharmacogenomics. These include clinical implementation of pharmacogenomics in clinical practice, development of tools or infrastructures to support this process, research of new pharmacogenomics markers to increase drug efficacy and safety, and the impact of rare genetic variants in pharmacogenomics.

Medicine --- CYP2C9 --- VKORC1 --- warfarin --- warfarin initiation phase of therapy --- INR --- pharmacogenetics study --- pharmacogenomics --- pharmacogenetics --- genotype --- phenotype --- alleles --- precision medicine --- pharmacotranscriptomics --- high-throughput analysis --- childhood acute lymphoblastic leukemia --- clopidogrel --- acenocoumarol --- CDSS --- implementation --- azathioprine --- inflammatory bowel disease --- glutathione-S transferase --- pharmacokinetics --- nucleoside analogs --- microRNAs --- gene expression --- drug resistance --- AML --- cisplatin --- nephrotoxicity --- kidney injury --- genetic polymorphisms --- pre-emptive --- panel --- breast cancer subtype --- miRNA --- pathway --- crosstalk network --- precision drugs --- ovarian cancer --- platinum resistance --- focal copy number alterations --- whole exome sequencing --- personalized medicine --- human genetics --- pharmacology --- CYP2C9 --- VKORC1 --- warfarin --- warfarin initiation phase of therapy --- INR --- pharmacogenetics study --- pharmacogenomics --- pharmacogenetics --- genotype --- phenotype --- alleles --- precision medicine --- pharmacotranscriptomics --- high-throughput analysis --- childhood acute lymphoblastic leukemia --- clopidogrel --- acenocoumarol --- CDSS --- implementation --- azathioprine --- inflammatory bowel disease --- glutathione-S transferase --- pharmacokinetics --- nucleoside analogs --- microRNAs --- gene expression --- drug resistance --- AML --- cisplatin --- nephrotoxicity --- kidney injury --- genetic polymorphisms --- pre-emptive --- panel --- breast cancer subtype --- miRNA --- pathway --- crosstalk network --- precision drugs --- ovarian cancer --- platinum resistance --- focal copy number alterations --- whole exome sequencing --- personalized medicine --- human genetics --- pharmacology

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Coumarins are widely distributed in nature and can be found in a large number of naturally occurring and synthetic bioactive molecules. The unique and versatile oxygen-containing heterocyclic structure makes them a privileged scaffold in Medicinal Chemistry. Many coumarin derivatives have been extracted from natural sources, designed, synthetized, and evaluated on different pharmacological targets. In addition, coumarin-based ion receptors, fluorescent probes, and biological stains are growing quickly and have extensive applications to monitor timely enzyme activity, complex biological events, as well as accurate pharmacological and pharmacokinetic properties in living cells. The extraction, synthesis, and biological evaluation of coumarins have become extremely attractive and rapidly developing topics. A large number of research and review papers have compiled information on this important family of compounds in 2020. Research articles, reviews, communications, and concept papers focused on the multidisciplinary profile of coumarins, highlighting natural sources, most recent synthetic pathways, along with the main biological applications and theoretical studies, were the main focus of this book. The huge and growing range of applications of coumarins described in this book is a demonstration of the potential of this family of compounds in Organic Chemistry, Medicinal Chemistry, and different sciences related to the study of natural products. This book includes 23 articles: 17 original papers and six review papers.

Research & information: general --- Biology, life sciences --- coumarin --- hydroxyl-modified coumarin --- photophysical --- thermal and structural characterization --- Glycyrrhiza uralensis --- glycyrol --- liquiritigenin --- cholinesterases --- human monoamine oxidases --- kinetics --- docking simulation --- chalcone --- neurodegenerative diseases --- adenosine receptors --- binding affinity --- docking --- 4-hydroxy-7-methoxycoumarin --- macrophage --- inflammation --- NF-κB --- MAPK --- calanolides --- pseudocalanolides --- calanolide A --- Calophyllum --- Calophyllaceae --- anti-HIV --- reverse transcriptase --- non-nucleoside reverse transcriptase inhibitors (NNRTIs) --- osthole --- umbelliferone --- esculin --- 4-hydroxycoumarin --- sorafenib --- apoptosis --- autophagy --- Yin Chen Hao --- constitutive androstane receptor --- scoparone --- coumarins --- quorum sensing --- QS inhibitors --- plant-derived molecules --- Chromobacterium violaceum --- immunoproteasome --- psoralen core --- non-peptidic --- electrophilic compounds --- warhead scan --- inflammatory bowel disease --- isocoumarin --- Crohn’s disease --- ulcerative colitis --- glutathione --- oxidative stress --- complementary therapies --- intestinal inflammation --- benzopyrones --- five-membered aromatic heterocycles --- furan --- pyrrole --- thiophene --- selenophen --- dihydrocoumarin-fused dihydropyranones --- 3-aroylcoumarines --- benzyl 2,3-butadienoate --- 6’-(4-biphenyl)-β-iso-cinchonine --- biological applications --- drug discovery --- fluorescent probes --- warfarin --- acenocoumarol --- mechanical valve --- time in therapeutic range --- anticoagulation --- Ruta chalepensis --- Rutaceae --- chalepin --- chalepensin --- bioactivity --- biosynthesis --- coumarin3-carboxamides --- pyranocoumarins --- anticancer activity --- antibacterial activity --- free radical polymerization --- LED --- photocomposites --- direct laser write --- analytical methods --- model plant --- natural genetic variation --- natural products --- simple coumarins --- chalcocoumarin --- MAO-B --- molecular dynamics --- in silico studies --- dye-sensitized solar cells --- coumarin dyes --- thieno [3,2-b] thiophene --- charge transfer --- ethynylaryl --- esculetin --- antiplatelet activity --- impedance aggregometry --- COX --- polyphenols --- pyrazole --- imidazole --- thiazole --- oxazole --- triazole --- thiadiazole --- curcumin --- curcumin–coumarin hybrids --- neuroprotection --- monoamine oxidase inhibition --- cholinesterase inhibition --- scavenging activity --- Escherichia coli --- biotransformation --- ferulenol --- structural annotation --- in silico tools --- n/a --- Crohn's disease --- 6'-(4-biphenyl)-β-iso-cinchonine --- curcumin-coumarin hybrids

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Coumarins are widely distributed in nature and can be found in a large number of naturally occurring and synthetic bioactive molecules. The unique and versatile oxygen-containing heterocyclic structure makes them a privileged scaffold in Medicinal Chemistry. Many coumarin derivatives have been extracted from natural sources, designed, synthetized, and evaluated on different pharmacological targets. In addition, coumarin-based ion receptors, fluorescent probes, and biological stains are growing quickly and have extensive applications to monitor timely enzyme activity, complex biological events, as well as accurate pharmacological and pharmacokinetic properties in living cells. The extraction, synthesis, and biological evaluation of coumarins have become extremely attractive and rapidly developing topics. A large number of research and review papers have compiled information on this important family of compounds in 2020. Research articles, reviews, communications, and concept papers focused on the multidisciplinary profile of coumarins, highlighting natural sources, most recent synthetic pathways, along with the main biological applications and theoretical studies, were the main focus of this book. The huge and growing range of applications of coumarins described in this book is a demonstration of the potential of this family of compounds in Organic Chemistry, Medicinal Chemistry, and different sciences related to the study of natural products. This book includes 23 articles: 17 original papers and six review papers.

Research & information: general --- Biology, life sciences --- coumarin --- hydroxyl-modified coumarin --- photophysical --- thermal and structural characterization --- Glycyrrhiza uralensis --- glycyrol --- liquiritigenin --- cholinesterases --- human monoamine oxidases --- kinetics --- docking simulation --- chalcone --- neurodegenerative diseases --- adenosine receptors --- binding affinity --- docking --- 4-hydroxy-7-methoxycoumarin --- macrophage --- inflammation --- NF-κB --- MAPK --- calanolides --- pseudocalanolides --- calanolide A --- Calophyllum --- Calophyllaceae --- anti-HIV --- reverse transcriptase --- non-nucleoside reverse transcriptase inhibitors (NNRTIs) --- osthole --- umbelliferone --- esculin --- 4-hydroxycoumarin --- sorafenib --- apoptosis --- autophagy --- Yin Chen Hao --- constitutive androstane receptor --- scoparone --- coumarins --- quorum sensing --- QS inhibitors --- plant-derived molecules --- Chromobacterium violaceum --- immunoproteasome --- psoralen core --- non-peptidic --- electrophilic compounds --- warhead scan --- inflammatory bowel disease --- isocoumarin --- Crohn's disease --- ulcerative colitis --- glutathione --- oxidative stress --- complementary therapies --- intestinal inflammation --- benzopyrones --- five-membered aromatic heterocycles --- furan --- pyrrole --- thiophene --- selenophen --- dihydrocoumarin-fused dihydropyranones --- 3-aroylcoumarines --- benzyl 2,3-butadienoate --- 6'-(4-biphenyl)-β-iso-cinchonine --- biological applications --- drug discovery --- fluorescent probes --- warfarin --- acenocoumarol --- mechanical valve --- time in therapeutic range --- anticoagulation --- Ruta chalepensis --- Rutaceae --- chalepin --- chalepensin --- bioactivity --- biosynthesis --- coumarin3-carboxamides --- pyranocoumarins --- anticancer activity --- antibacterial activity --- free radical polymerization --- LED --- photocomposites --- direct laser write --- analytical methods --- model plant --- natural genetic variation --- natural products --- simple coumarins --- chalcocoumarin --- MAO-B --- molecular dynamics --- in silico studies --- dye-sensitized solar cells --- coumarin dyes --- thieno [3,2-b] thiophene --- charge transfer --- ethynylaryl --- esculetin --- antiplatelet activity --- impedance aggregometry --- COX --- polyphenols --- pyrazole --- imidazole --- thiazole --- oxazole --- triazole --- thiadiazole --- curcumin --- curcumin-coumarin hybrids --- neuroprotection --- monoamine oxidase inhibition --- cholinesterase inhibition --- scavenging activity --- Escherichia coli --- biotransformation --- ferulenol --- structural annotation --- in silico tools --- coumarin --- hydroxyl-modified coumarin --- photophysical --- thermal and structural characterization --- Glycyrrhiza uralensis --- glycyrol --- liquiritigenin --- cholinesterases --- human monoamine oxidases --- kinetics --- docking simulation --- chalcone --- neurodegenerative diseases --- adenosine receptors --- binding affinity --- docking --- 4-hydroxy-7-methoxycoumarin --- macrophage --- inflammation --- NF-κB --- MAPK --- calanolides --- pseudocalanolides --- calanolide A --- Calophyllum --- Calophyllaceae --- anti-HIV --- reverse transcriptase --- non-nucleoside reverse transcriptase inhibitors (NNRTIs) --- osthole --- umbelliferone --- esculin --- 4-hydroxycoumarin --- sorafenib --- apoptosis --- autophagy --- Yin Chen Hao --- constitutive androstane receptor --- scoparone --- coumarins --- quorum sensing --- QS inhibitors --- plant-derived molecules --- Chromobacterium violaceum --- immunoproteasome --- psoralen core --- non-peptidic --- electrophilic compounds --- warhead scan --- inflammatory bowel disease --- isocoumarin --- Crohn's disease --- ulcerative colitis --- glutathione --- oxidative stress --- complementary therapies --- intestinal inflammation --- benzopyrones --- five-membered aromatic heterocycles --- furan --- pyrrole --- thiophene --- selenophen --- dihydrocoumarin-fused dihydropyranones --- 3-aroylcoumarines --- benzyl 2,3-butadienoate --- 6'-(4-biphenyl)-β-iso-cinchonine --- biological applications --- drug discovery --- fluorescent probes --- warfarin --- acenocoumarol --- mechanical valve --- time in therapeutic range --- anticoagulation --- Ruta chalepensis --- Rutaceae --- chalepin --- chalepensin --- bioactivity --- biosynthesis --- coumarin3-carboxamides --- pyranocoumarins --- anticancer activity --- antibacterial activity --- free radical polymerization --- LED --- photocomposites --- direct laser write --- analytical methods --- model plant --- natural genetic variation --- natural products --- simple coumarins --- chalcocoumarin --- MAO-B --- molecular dynamics --- in silico studies --- dye-sensitized solar cells --- coumarin dyes --- thieno [3,2-b] thiophene --- charge transfer --- ethynylaryl --- esculetin --- antiplatelet activity --- impedance aggregometry --- COX --- polyphenols --- pyrazole --- imidazole --- thiazole --- oxazole --- triazole --- thiadiazole --- curcumin --- curcumin-coumarin hybrids --- neuroprotection --- monoamine oxidase inhibition --- cholinesterase inhibition --- scavenging activity --- Escherichia coli --- biotransformation --- ferulenol --- structural annotation --- in silico tools