It is All About Proteases: From Drug Delivery to In Vivo Imaging and Photomedicine

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Drug discovery and development is a high-risk enterprise that requires significant investments in capital, time and scientific expertise. The studies of xenobiotic metabolism remain as one of the main topics in the research and development of drugs, cosmet ...

The disulfide bonds that form between two cysteine residues are important in defining and rigidifying the structures of proteins and peptides. In polypeptides containing multiple cysteine residues, disulfide isomerization can lead to multiple products with ...

The oral administration of peptide drugs is hampered by their metabolic instability and limited intestinal uptake. Here, we describe a method for the generation of small target-specific peptides (less than 1,600 Da in size) that resist gastrointestinal pro ...

Despite the recent advances in structural analysis of monoclonal antibodies with bottom-up, middle-down, and top-down mass spectrometry (MS), further improvements in analysis accuracy, depth, and speed are needed. The remaining challenges include quantitat ...

Polymorphonuclear neutrophils contain at least four serine endopeptidases, namely neutrophil elastase (NE), proteinase 3 (PR3), cathepsin G (CatG), and NSP4, which contribute to the regulation of infection and of inflammatory processes. In physiological co ...

Many naturally occurring cyclic peptides or derivatives thereof are used as therapeutics such as the human hormones vasopressin and oxytocin or the antibiotics vancomycin and daptomycin. The success of cyclic peptide therapeutics is based on their ability ...

Caenorhabditis elegans(C. elegans) constitutes an important model organism for use in nutrition and aging studies. We report a novel method for studying the dynamics ofEscherichia coli(E. coli) bacterial transit through the worms' intestine. A microfluidic ...

In arthropods, the melanization reaction consists in the rapid synthesis of melanin at the site of infection and injury. A key enzyme in the melanization process is phenoloxidase (PO), which catalyzes the oxidation of phenols to quinones that subsequently ...

Hemostasis is a complex physiological process responsible for the prevention of blood loss caused by vascular injury. The dysregulation of this delicate mechanism can lead to thromboembolic diseases, the leading cause of death worldwide. Anticoagulants are ...

Hsp70 molecular chaperones are abundant ATP-dependent nanomachines that actively reshape non-native, misfolded proteins and assist a wide variety of essential cellular processes. Here, we combine complementary theoretical approaches to elucidate the struct ...

Peptides derived from the HR1 or HR2 regions of the HIV-1 envelope glycoprotein gp41 have been shown to be effective inhibitors to prevent virus-host cell membrane fusion. These peptide drugs, however, suffer from relatively short plasma half-lives and are ...

It is All About Proteases: From Drug Delivery to In Vivo Imaging and Photomedicine

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Antihypertensive drugs metabolism: an update to pharmacokinetic profiles and computational approaches

Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides

De novo development of proteolytically resistant therapeutic peptides for oral administration

Advantages of Extended Bottom-Up Proteomics Using Sap9 for Analysis of Monoclonal Antibodies

Human proteinase 3 resistance to inhibition extends to alpha-2 macroglobulin

Directed Evolution of Bicyclic Peptides for Therapeutic Application

Anin vivomicrofluidic study of bacterial transit inC. elegansnematodes

Role and regulation of the melanization reaction in Drosophila immune response

Development of cyclic peptide inhibitors of coagulation factor XIa for safer anticoagulation

Efficient conversion of chemical energy into mechanical work by Hsp70 chaperones

Site-Specific PEGylation of HR2 Peptides: Effects of PEG Conjugation Position and Chain Length on HIV-1 Membrane Fusion Inhibition and Proteolytic Degradation