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Natural-based biomolecules continuously play an important role in novel drug discovery for the treatment of chronic diseases. The development of natural peptide/protein-based, toxin-based, and antibody-based drugs can significantly improve the biomedical efficiency of disease-specific therapy. The focus of this Special Issue of Biomolecules will be on the most recent advances related to novel peptides/proteins, antibodies, and toxins as forms of medicinal therapy. Recent advances in the discovery and development of these natural biomolecules for use in targeted therapy and immunotherapy against chronic diseases (e.g., cancer, diabetes, cardiovascular diseases, and rheumatoid arthritis) will be addressed. The discussion on using novel disease-specific proteins/peptides/toxins/antibodies along with currently available FDA-approved drugs as combinatorial treatments will also be encouraged in this context. Finally, an overview of some of the selected promising natural biomolecules that are potentially able to address the forthcoming challenges in this field will be included. Both research (in particular) and review articles proposing novelties or overviews, respectively, are welcome.

Humanities --- Social interaction --- DAPK1 --- SUMO --- SENP --- protein degradation --- post-translational modification --- amphibian Bowman-Birk inhibitor --- Tat peptide --- molecular cloning --- antifungal --- drug design --- protease inhibitor --- natural-based compound --- anticancer therapy --- lung cancer --- survivin --- apoptosis --- STAT3 --- colorectal cancer --- orientin --- cell cycle arrest --- Bcl-2 family proteins --- Astragalus membranaceus --- insulin --- PI3K --- AKT --- PPARγ --- PDX-1 --- Petasites japonicus --- Asteraceae --- lignan --- anti-inflammation --- NO --- PGE2 --- iNOS --- COX-2 --- molecular docking --- peptides --- kynurenines --- binding affinity --- μ-opioid receptor --- pharmacophore --- G-protein activation --- fucoidan --- PLGA --- docetaxel --- drug delivery system --- anticancer therapy/cancer treatment --- hIAPP --- amyloidogenesis --- insulin granules --- endoplasmic reticulum --- anionic lipids --- F23R variant --- β-sheet transitions --- β-cell cytotoxicity --- unfolded protein response --- pomegranate --- punicalagin --- tannins --- gingiva --- fibroblasts --- antioxidant --- wound healing --- branched-chain fatty acids --- Conidiobolus heterosporus --- peroxisome proliferator-activated receptor α --- lipid metabolism --- fatty acid oxidation --- hepatocyte --- n/a

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Natural-based biomolecules continuously play an important role in novel drug discovery for the treatment of chronic diseases. The development of natural peptide/protein-based, toxin-based, and antibody-based drugs can significantly improve the biomedical efficiency of disease-specific therapy. The focus of this Special Issue of Biomolecules will be on the most recent advances related to novel peptides/proteins, antibodies, and toxins as forms of medicinal therapy. Recent advances in the discovery and development of these natural biomolecules for use in targeted therapy and immunotherapy against chronic diseases (e.g., cancer, diabetes, cardiovascular diseases, and rheumatoid arthritis) will be addressed. The discussion on using novel disease-specific proteins/peptides/toxins/antibodies along with currently available FDA-approved drugs as combinatorial treatments will also be encouraged in this context. Finally, an overview of some of the selected promising natural biomolecules that are potentially able to address the forthcoming challenges in this field will be included. Both research (in particular) and review articles proposing novelties or overviews, respectively, are welcome.

Humanities --- Social interaction --- DAPK1 --- SUMO --- SENP --- protein degradation --- post-translational modification --- amphibian Bowman-Birk inhibitor --- Tat peptide --- molecular cloning --- antifungal --- drug design --- protease inhibitor --- natural-based compound --- anticancer therapy --- lung cancer --- survivin --- apoptosis --- STAT3 --- colorectal cancer --- orientin --- cell cycle arrest --- Bcl-2 family proteins --- Astragalus membranaceus --- insulin --- PI3K --- AKT --- PPARγ --- PDX-1 --- Petasites japonicus --- Asteraceae --- lignan --- anti-inflammation --- NO --- PGE2 --- iNOS --- COX-2 --- molecular docking --- peptides --- kynurenines --- binding affinity --- μ-opioid receptor --- pharmacophore --- G-protein activation --- fucoidan --- PLGA --- docetaxel --- drug delivery system --- anticancer therapy/cancer treatment --- hIAPP --- amyloidogenesis --- insulin granules --- endoplasmic reticulum --- anionic lipids --- F23R variant --- β-sheet transitions --- β-cell cytotoxicity --- unfolded protein response --- pomegranate --- punicalagin --- tannins --- gingiva --- fibroblasts --- antioxidant --- wound healing --- branched-chain fatty acids --- Conidiobolus heterosporus --- peroxisome proliferator-activated receptor α --- lipid metabolism --- fatty acid oxidation --- hepatocyte --- DAPK1 --- SUMO --- SENP --- protein degradation --- post-translational modification --- amphibian Bowman-Birk inhibitor --- Tat peptide --- molecular cloning --- antifungal --- drug design --- protease inhibitor --- natural-based compound --- anticancer therapy --- lung cancer --- survivin --- apoptosis --- STAT3 --- colorectal cancer --- orientin --- cell cycle arrest --- Bcl-2 family proteins --- Astragalus membranaceus --- insulin --- PI3K --- AKT --- PPARγ --- PDX-1 --- Petasites japonicus --- Asteraceae --- lignan --- anti-inflammation --- NO --- PGE2 --- iNOS --- COX-2 --- molecular docking --- peptides --- kynurenines --- binding affinity --- μ-opioid receptor --- pharmacophore --- G-protein activation --- fucoidan --- PLGA --- docetaxel --- drug delivery system --- anticancer therapy/cancer treatment --- hIAPP --- amyloidogenesis --- insulin granules --- endoplasmic reticulum --- anionic lipids --- F23R variant --- β-sheet transitions --- β-cell cytotoxicity --- unfolded protein response --- pomegranate --- punicalagin --- tannins --- gingiva --- fibroblasts --- antioxidant --- wound healing --- branched-chain fatty acids --- Conidiobolus heterosporus --- peroxisome proliferator-activated receptor α --- lipid metabolism --- fatty acid oxidation --- hepatocyte

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The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general.

Medicine --- opioid receptors --- neurokinin-1 receptor --- peptide synthesis --- receptor binding studies --- functional assay --- writhing test --- tolerance --- Leu-enkephalin --- beta-arrestin --- mu opioid receptor --- delta opioid receptor --- biased signaling --- DADLE --- ischemia --- plasma stability --- morphinan --- BNTX --- δ opioid receptor antagonist --- 1H-NMR experiments --- mechanism elucidation --- peripheral antinociception --- 14-methoxycodeine-6-O-sulfate --- codeine-6-O-sulfate --- opioid peptides and peptidomimetics --- DAMGO --- DALDA --- [Dmt1]DALDA --- KGOP01 --- binding --- molecular docking --- structure-activity relationships --- β2-amino acids --- β2-Homo-amino acids --- µ-opioid receptor --- opioid peptides --- TAPP --- racemic synthesis of β2-amino acids --- peripheral µ-opioid receptors --- analgesia --- peripheral analgesic tolerance --- dysbiosis --- opioid --- bifunctional ligands --- (−)-N-phenethylnorhydromorphone analogs --- [35S]GTPgammaS assay --- forskolin-induced cAMP accumulation assays --- β-arrestin recruitment assays --- MOR and DOR agonists --- respiratory depression --- bias factor --- molecular modeling &amp --- simulation --- δ opioid receptor --- NTI derivative --- sulfonamide --- inverse agonist --- neutral antagonist --- agonist --- opioids --- mu receptor --- opioid side effects --- biased agonism --- partial agonism --- zerumbone --- chronic constriction injury (CCI) --- allodynia --- hyperalgesia --- potassium channels --- over-the-counter drugs --- misuse --- abuse --- opioid drugs --- pharmacology --- codeine --- dihydrocodeine --- loperamide --- opioid peptide --- macrocyclic tetrapeptide --- multifunctional ligands --- kappa opioid receptor --- analgesics --- opioid liabilities --- μ opioid receptor --- receptor model --- biased ligands --- dependence --- pain therapy --- neonatal opioid withdrawal syndrome --- naltrexone --- 6β-naltrexol --- buprenorphine --- G-protein bias --- arrestin recruitment --- respiration --- mitragynine --- heteromer --- internalization --- primary hippocampal culture --- lysosomes --- µ opioid receptor --- molecular dynamics --- docking --- interaction fingerprints --- biased agonists --- SR-17018 --- PZM21 --- morphine --- fentanyl --- diphenethylamines --- design and synthesis --- structure-activity relationships --- partial agonist --- biased agonist --- antagonist --- binding affinity --- selectivity --- opioid receptors --- neurokinin-1 receptor --- peptide synthesis --- receptor binding studies --- functional assay --- writhing test --- tolerance --- Leu-enkephalin --- beta-arrestin --- mu opioid receptor --- delta opioid receptor --- biased signaling --- DADLE --- ischemia --- plasma stability --- morphinan --- BNTX --- δ opioid receptor antagonist --- 1H-NMR experiments --- mechanism elucidation --- peripheral antinociception --- 14-methoxycodeine-6-O-sulfate --- codeine-6-O-sulfate --- opioid peptides and peptidomimetics --- DAMGO --- DALDA --- [Dmt1]DALDA --- KGOP01 --- binding --- molecular docking --- structure-activity relationships --- β2-amino acids --- β2-Homo-amino acids --- µ-opioid receptor --- opioid peptides --- TAPP --- racemic synthesis of β2-amino acids --- peripheral µ-opioid receptors --- analgesia --- peripheral analgesic tolerance --- dysbiosis --- opioid --- bifunctional ligands --- (−)-N-phenethylnorhydromorphone analogs --- [35S]GTPgammaS assay --- forskolin-induced cAMP accumulation assays --- β-arrestin recruitment assays --- MOR and DOR agonists --- respiratory depression --- bias factor --- molecular modeling &amp --- simulation --- δ opioid receptor --- NTI derivative --- sulfonamide --- inverse agonist --- neutral antagonist --- agonist --- opioids --- mu receptor --- opioid side effects --- biased agonism --- partial agonism --- zerumbone --- chronic constriction injury (CCI) --- allodynia --- hyperalgesia --- potassium channels --- over-the-counter drugs --- misuse --- abuse --- opioid drugs --- pharmacology --- codeine --- dihydrocodeine --- loperamide --- opioid peptide --- macrocyclic tetrapeptide --- multifunctional ligands --- kappa opioid receptor --- analgesics --- opioid liabilities --- μ opioid receptor --- receptor model --- biased ligands --- dependence --- pain therapy --- neonatal opioid withdrawal syndrome --- naltrexone --- 6β-naltrexol --- buprenorphine --- G-protein bias --- arrestin recruitment --- respiration --- mitragynine --- heteromer --- internalization --- primary hippocampal culture --- lysosomes --- µ opioid receptor --- molecular dynamics --- docking --- interaction fingerprints --- biased agonists --- SR-17018 --- PZM21 --- morphine --- fentanyl --- diphenethylamines --- design and synthesis --- structure-activity relationships --- partial agonist --- biased agonist --- antagonist --- binding affinity --- selectivity