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SRC HOMOLOGY DOMAINS --- PEPTIDOMIMETICS --- SRC HOMOLOGY DOMAINS --- PEPTIDOMIMETICS

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Peptide and Peptidomimetic Therapeutics: From Bench to Beside offers applied, evidence-based instruction on developing and applying peptide therapeutics in disease treatment, driving drug discovery, and improving patient care. Here, researchers, clinicians and students will find tools to harness the full power of peptides and peptidomimetics and improve bioavailability, stability, efficiency and selectivity of new therapeutics and their application in treatment plans. More than 20 leaders in the field share their approaches for identifying and advancing peptide and peptidomimetic therapeutics. Topics examined run from "bench to bedside," beginning with fundamental peptide science, protein-protein interactions and peptide synthesis. Later chapters examine modes for peptide drug delivery, including cell penetration peptide and peptidomimetic delivery, as well as the targeting of specific disease types, peptide therapeutics as applied to infectious disease, cancer, metabolic disorders, neurodegenerative disorders, and skin disorders, and antiparasitic and immunosuppressive peptidomimetics.

Peptide drugs. --- Peptide drugs --- Design. --- Peptide pharmaceuticals --- Drugs --- Peptides --- Peptidomimetics --- Drug Design --- pharmacology --- therapeutic use

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Transition metal-catalyzed cross-coupling reactions have proved to be powerful tools for carbon–carbon as well as carbon–heteroatom bond formation in the development of synthetic methodologies for applications ranging from pharmaceuticals to materials. This book, consisting of an editorial, two reviews and two articles, focuses on recent promising research and novel trends in the field of cross-coupling reactions, employing a range of different catalysts. A review by Kostas and Steele provides a survey of the research in the area of cross-coupling catalytic reactions with transition metal complexes based on the thiosemicarbazone unit and a discussion of the prospects for future developments. Another review by Polychronopoulou, Shaya and co-authors describes the progress made over the 21st century concerning the utilization of C(sp3)–organoboranes as partners in metal-catalyzed C(sp3)–C(sp2) cross-couplings, such as B-alkyl Suzuki–Miyaura reactions. The article by Waldvogel, Breinbauer and co-authors demonstrates for the first time the synthetic potential of combining the electro-oxidative dehydrogenative cross coupling of ortho-substituted phenols with Pd-catalyzed cross-coupling reactions. In the second article, Štĕpnička and co-workers describe the preparation of palladium catalysts deposited over silica gel-bearing composite amide-donor functional moieties on the surface, which were evaluated in the Sonogashira-type cross-coupling of acyl chlorides with terminal alkynes.

Technology: general issues --- Suzuki–Miyaura cross-couplings --- C(sp3) –C(sp2) --- alkylboron reagents --- metal catalysis --- alpha-helix --- anode --- CH-activation --- cross-coupling --- electrosynthesis --- oligoarene --- peptidomimetics --- phenol --- protein-protein interactions --- triflate --- thiosemicarbazone --- metal complex --- transition metal catalysis --- cross-coupling reaction --- Heck reaction --- Suzuki reaction --- Sonogashira reaction --- Kumada reaction --- Buchwald–Hartwig reaction --- deposited catalysts --- palladium --- functional amides --- alkynyl ketone synthesis --- n/a --- Suzuki-Miyaura cross-couplings --- C(sp3) -C(sp2) --- Buchwald-Hartwig reaction

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This Special Issue, entitled "Synthetic Peptides and Peptidomimetics: From Basic Science to Biomedical Applications", has included both reviews and original research contributions focused on the chemical design and biomedical applications of structurally modified bioactive peptides. The papers collected show how successful this class of molecules still is, both as model molecules for studying the structure of proteins and as potential therapeutics and diagnostics, and also as laboratory tools for advanced basic and applied studies. The large scientific community working in this field is in fact very active and productive, and is making the most of the potential and versatility of these molecules to generate increasingly interesting and innovative molecules of therapeutic interest and to understand the fundamental molecular mechanisms of life.

Research & information: general --- Biology, life sciences --- polymers --- peptidomimetics --- AFM --- transfection --- molecular modelling --- peptide --- α-helix --- hydrocarbon stapling --- ring-closing metathesis --- i,i + 1 staple --- X-ray structure --- deferoxamine --- RGD peptides --- integrins --- radiodiagnostics --- PET imaging --- retro-inverso peptides --- anticancer peptides --- drug delivery --- peptide antigens --- Aβ --- IAPP --- antimicrobial peptides --- peptides --- diagnostic --- ELISA --- microarray --- PET --- SPECT --- imaging diagnostic --- non-imaging diagnostic --- amphiphilic peptides --- non-viral gene delivery --- nanocarrier --- peptide self-assemblies --- stimuli responsive --- SARS-CoV-2 --- FRET --- molecular docking --- molecular dynamics --- MM-GBSA --- drug repurposing --- antiviral --- cancer --- cyclic peptide --- integrin --- αvβ3 --- ALOS4 --- melanoma --- fluorescent peptide --- environment-sensitive fluorophore --- peptide labeling --- luciferin --- membrane-binding peptide --- antimicrobial peptide --- antitumor peptide --- RGD peptide --- antiproliferative activity --- chirality --- conformational analysis --- density functional theory (DFT) --- ferrocene --- hydrogen bonds --- peptidomimetic --- X-ray --- protein–protein interactions (PPIs) --- voltage-gated Na+ (Nav) channels --- fibroblast growth factor 14 (FGF14) --- medium spiny neurons (MSNs) --- nucleus accumbens (NAc) --- neurotherapeutics --- cyclophilin A (CypA) --- apoptosis-inducing factor (AIF) --- human neuroblastoma SH-SY5Y cells --- staurosporine-mediated cell death --- AIF(370-394) peptide --- caspase-3 --- PARP --- antifungal --- antibacterial --- peptide-based therapies --- synthetic peptides --- polymers --- peptidomimetics --- AFM --- transfection --- molecular modelling --- peptide --- α-helix --- hydrocarbon stapling --- ring-closing metathesis --- i,i + 1 staple --- X-ray structure --- deferoxamine --- RGD peptides --- integrins --- radiodiagnostics --- PET imaging --- retro-inverso peptides --- anticancer peptides --- drug delivery --- peptide antigens --- Aβ --- IAPP --- antimicrobial peptides --- peptides --- diagnostic --- ELISA --- microarray --- PET --- SPECT --- imaging diagnostic --- non-imaging diagnostic --- amphiphilic peptides --- non-viral gene delivery --- nanocarrier --- peptide self-assemblies --- stimuli responsive --- SARS-CoV-2 --- FRET --- molecular docking --- molecular dynamics --- MM-GBSA --- drug repurposing --- antiviral --- cancer --- cyclic peptide --- integrin --- αvβ3 --- ALOS4 --- melanoma --- fluorescent peptide --- environment-sensitive fluorophore --- peptide labeling --- luciferin --- membrane-binding peptide --- antimicrobial peptide --- antitumor peptide --- RGD peptide --- antiproliferative activity --- chirality --- conformational analysis --- density functional theory (DFT) --- ferrocene --- hydrogen bonds --- peptidomimetic --- X-ray --- protein–protein interactions (PPIs) --- voltage-gated Na+ (Nav) channels --- fibroblast growth factor 14 (FGF14) --- medium spiny neurons (MSNs) --- nucleus accumbens (NAc) --- neurotherapeutics --- cyclophilin A (CypA) --- apoptosis-inducing factor (AIF) --- human neuroblastoma SH-SY5Y cells --- staurosporine-mediated cell death --- AIF(370-394) peptide --- caspase-3 --- PARP --- antifungal --- antibacterial --- peptide-based therapies --- synthetic peptides

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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.

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 --- n/a