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Gentamicin. --- Ponies.

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In the two last decades, proteases have constituted one of the primary and important targets in drug discovery. The U.S. FDA has approved more than 12 protease therapies in the last 10 years, and a number of next-generation or completely new proteases are under clinical development. Protease inhibition strategies are one of the fastest expanding areas in the field of of drugs that show considerable promise. This Special Issue will focus on the recent advances in the discovery and development of protease inhibitors, covering the synthesis of protease inhibitors, the design of new chemical entities acting as inhibitors of special/particular types of proteases, and their mode of actions (Frolova et al. 2020; Slapak et al. 2020; Künnapuu et al. 2021). In addition, the new applications of these interesting compounds/biomolecules and their limitations have been discussed and described (Wang et al. 2020; Bartošová-Sojková et al. 2021).

Research & information: general --- MMP --- MMP2 --- MMP9 --- MMP7 --- MMP14 --- matrix metalloproteases --- PDAC --- pancreatic cancer --- Bowman–Birk inhibitor --- ranacyclin --- trypsin inhibitor --- structure–activity relationship --- synergistic effect --- Gentamicin --- matrix metalloproteinase --- extracellular matrix --- nuclei --- cancer --- apoptosis --- immune response --- cysteine protease inhibitor --- stefin --- signal peptide --- parasite --- phylogenetic analysis --- diversification --- protein structure --- vascular endothelial growth factors (VEGFs) --- VEGF-A --- PlGF --- VEGF-B --- VEGF-C --- VEGF-D --- angiogenesis --- lymphangiogenesis --- CCBE1 --- proteases --- ADAMTS3 --- plasmin --- cathepsin D --- KLK3 --- prostate-specific antigen (PSA) --- thrombin --- wound healing --- metastasis --- proteolytic activation --- vascular biology --- lymphedema --- MMP --- MMP2 --- MMP9 --- MMP7 --- MMP14 --- matrix metalloproteases --- PDAC --- pancreatic cancer --- Bowman–Birk inhibitor --- ranacyclin --- trypsin inhibitor --- structure–activity relationship --- synergistic effect --- Gentamicin --- matrix metalloproteinase --- extracellular matrix --- nuclei --- cancer --- apoptosis --- immune response --- cysteine protease inhibitor --- stefin --- signal peptide --- parasite --- phylogenetic analysis --- diversification --- protein structure --- vascular endothelial growth factors (VEGFs) --- VEGF-A --- PlGF --- VEGF-B --- VEGF-C --- VEGF-D --- angiogenesis --- lymphangiogenesis --- CCBE1 --- proteases --- ADAMTS3 --- plasmin --- cathepsin D --- KLK3 --- prostate-specific antigen (PSA) --- thrombin --- wound healing --- metastasis --- proteolytic activation --- vascular biology --- lymphedema

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In the two last decades, proteases have constituted one of the primary and important targets in drug discovery. The U.S. FDA has approved more than 12 protease therapies in the last 10 years, and a number of next-generation or completely new proteases are under clinical development. Protease inhibition strategies are one of the fastest expanding areas in the field of of drugs that show considerable promise. This Special Issue will focus on the recent advances in the discovery and development of protease inhibitors, covering the synthesis of protease inhibitors, the design of new chemical entities acting as inhibitors of special/particular types of proteases, and their mode of actions (Frolova et al. 2020; Slapak et al. 2020; Künnapuu et al. 2021). In addition, the new applications of these interesting compounds/biomolecules and their limitations have been discussed and described (Wang et al. 2020; Bartošová-Sojková et al. 2021).

MMP --- MMP2 --- MMP9 --- MMP7 --- MMP14 --- matrix metalloproteases --- PDAC --- pancreatic cancer --- Bowman–Birk inhibitor --- ranacyclin --- trypsin inhibitor --- structure–activity relationship --- synergistic effect --- Gentamicin --- matrix metalloproteinase --- extracellular matrix --- nuclei --- cancer --- apoptosis --- immune response --- cysteine protease inhibitor --- stefin --- signal peptide --- parasite --- phylogenetic analysis --- diversification --- protein structure --- vascular endothelial growth factors (VEGFs) --- VEGF-A --- PlGF --- VEGF-B --- VEGF-C --- VEGF-D --- angiogenesis --- lymphangiogenesis --- CCBE1 --- proteases --- ADAMTS3 --- plasmin --- cathepsin D --- KLK3 --- prostate-specific antigen (PSA) --- thrombin --- wound healing --- metastasis --- proteolytic activation --- vascular biology --- lymphedema

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Marine natural products are characterized by high chemical diversity, biochemical specificity, and other molecular properties that make them favorable as lead structures for drug discovery. In this field, one of the main problems is often the reduced natural availability of isolated substances, which can complicate both the structural characterization and possible future developments. For these reasons, the study of bioactive marine metabolites should rely on the development of chemical synthesis and synthetic strategies aimed at the preparation of pure compounds and analogs both for structural confirmation and/or for the large-scale preparation necessary for future applications. Moreover, natural products can be a crucial starting point for the preparation of molecules structurally inspired by the latter, opening the path to new classes of biologically active compounds with pharmacological potential. This book collects original research articles regarding synthetic strategies for secondary marine metabolites and/or analogs that favor applications of these molecules and/or solve structural challenges common in the field of natural substances.

organic synthesis --- meroterpenoids --- thiazinoquinones --- antiproliferative activity --- G0/G1 cell-cycle arrest --- cytostatic --- solid tumor cell lines --- alkylglycerol (AKG) --- ricinoleic acid (RA) --- antimicrobial activity --- structure–activity relationship (SAR) studies --- antibiotics (gentamicin --- tetracycline --- ciprofloxacin and ampicillin) --- marine-inspired --- breast cancer --- bis-indoles --- synthesis --- apoptosis --- carbohydrates --- polysaccharides --- semi-synthesis --- sulfation --- glycosylation --- fucose --- fucosylated chondroitin sulfate --- marine natural product --- largazole --- HDAC inhibitors --- modification --- fluoro olefin --- total synthesis --- natural product --- 7-deazapurine nucleoside --- disaccharide nucleoside --- tubercidin --- aureol --- tetracyclic meroterpenoids --- natural products synthesis --- labdane scaffold --- bioactive diterpenes --- sclareolide --- structure-activity relationships --- TRPV4 channel --- amides/esters --- COVID-19 --- SARS-CoV-2 --- lipophilic iminosugars --- polymer-supported triphenyl phosphine --- cholesterol --- antibacterial iminosugars --- n/a --- structure-activity relationship (SAR) studies

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Marine natural products are characterized by high chemical diversity, biochemical specificity, and other molecular properties that make them favorable as lead structures for drug discovery. In this field, one of the main problems is often the reduced natural availability of isolated substances, which can complicate both the structural characterization and possible future developments. For these reasons, the study of bioactive marine metabolites should rely on the development of chemical synthesis and synthetic strategies aimed at the preparation of pure compounds and analogs both for structural confirmation and/or for the large-scale preparation necessary for future applications. Moreover, natural products can be a crucial starting point for the preparation of molecules structurally inspired by the latter, opening the path to new classes of biologically active compounds with pharmacological potential. This book collects original research articles regarding synthetic strategies for secondary marine metabolites and/or analogs that favor applications of these molecules and/or solve structural challenges common in the field of natural substances.

Language --- organic synthesis --- meroterpenoids --- thiazinoquinones --- antiproliferative activity --- G0/G1 cell-cycle arrest --- cytostatic --- solid tumor cell lines --- alkylglycerol (AKG) --- ricinoleic acid (RA) --- antimicrobial activity --- structure-activity relationship (SAR) studies --- antibiotics (gentamicin --- tetracycline --- ciprofloxacin and ampicillin) --- marine-inspired --- breast cancer --- bis-indoles --- synthesis --- apoptosis --- carbohydrates --- polysaccharides --- semi-synthesis --- sulfation --- glycosylation --- fucose --- fucosylated chondroitin sulfate --- marine natural product --- largazole --- HDAC inhibitors --- modification --- fluoro olefin --- total synthesis --- natural product --- 7-deazapurine nucleoside --- disaccharide nucleoside --- tubercidin --- aureol --- tetracyclic meroterpenoids --- natural products synthesis --- labdane scaffold --- bioactive diterpenes --- sclareolide --- structure-activity relationships --- TRPV4 channel --- amides/esters --- COVID-19 --- SARS-CoV-2 --- lipophilic iminosugars --- polymer-supported triphenyl phosphine --- cholesterol --- antibacterial iminosugars --- organic synthesis --- meroterpenoids --- thiazinoquinones --- antiproliferative activity --- G0/G1 cell-cycle arrest --- cytostatic --- solid tumor cell lines --- alkylglycerol (AKG) --- ricinoleic acid (RA) --- antimicrobial activity --- structure-activity relationship (SAR) studies --- antibiotics (gentamicin --- tetracycline --- ciprofloxacin and ampicillin) --- marine-inspired --- breast cancer --- bis-indoles --- synthesis --- apoptosis --- carbohydrates --- polysaccharides --- semi-synthesis --- sulfation --- glycosylation --- fucose --- fucosylated chondroitin sulfate --- marine natural product --- largazole --- HDAC inhibitors --- modification --- fluoro olefin --- total synthesis --- natural product --- 7-deazapurine nucleoside --- disaccharide nucleoside --- tubercidin --- aureol --- tetracyclic meroterpenoids --- natural products synthesis --- labdane scaffold --- bioactive diterpenes --- sclareolide --- structure-activity relationships --- TRPV4 channel --- amides/esters --- COVID-19 --- SARS-CoV-2 --- lipophilic iminosugars --- polymer-supported triphenyl phosphine --- cholesterol --- antibacterial iminosugars