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Article
Open AccessIn vivo photocontrol of orexin receptors with a nanomolar light-regulated analogue of orexin-B
Orexinergic neurons are critically involved in regulating arousal, wakefulness, and appetite. Their dysfunction has been associated with slee** disorders, and non-peptide drugs are currently being developed ...
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Article
Anti-EGF nanobodies enhance the antitumoral effect of osimertinib and overcome resistance in non-small cell lung cancer (NSCLC) cellular models
Osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that is effective against the EGFR T790M mutation in patients with advanced non-small-cell lung cancer ...
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Article
Lebetin Peptides, A New Class of Potent Platelet Aggregation Inhibitors: Chemical Synthesis, Biological Activity and NMR Spectroscopic Study
Platelets have a well-established role in atherosclerosis and related diseases. Lebetins from the venom of Vipera lebetina, lacking the RGD sequence, emerged as a new family of platelet aggregation inhibitors. Ho...
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Article
Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation
The development of neuroprotective therapies is a sought-after goal. By screening combinatorial chemical libraries using in vitro assays, we identified the small molecule BN201 that promotes the survival of cultu...
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Article
Open AccessAlgorithm-supported, mass and sequence diversity-oriented random peptide library design
Random peptide libraries that cover large search spaces are often used for the discovery of new binders, even when the target is unknown. To ensure an accurate population representation, there is a tendency to...
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Article
Open AccessA MALDI-TOF-based Method for Studying the Transport of BBB Shuttles—Enhancing Sensitivity and Versatility of Cell-Based In Vitro Transport Models
In recent decades, peptide blood-brain barrier shuttles have emerged as a promising solution for brain drugs that are not able to enter this organ. The research and development of these compounds involve the u...
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Article
Open AccessHAI Peptide and Backbone Analogs—Validation and Enhancement of Biostability and Bioactivity of BBB Shuttles
Low effectiveness and resistance to treatments are commonplace in disorders of the central nervous system (CNS). These issues concern mainly the blood-brain barrier (BBB), which preserves homeostasis in the br...
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Article
Open AccessImmunosilencing peptides by stereochemical inversion and sequence reversal: retro-D-peptides
Peptides are experiencing a new era in medical research, finding applications ranging from therapeutics to vaccines. In spite of the promising properties of peptide pharmaceuticals, their development continues...
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Article
Open AccessCombating virulence of Gram-negative bacilli by OmpA inhibition
Preventing the adhesion of pathogens to host cells provides an innovative approach to tackling multidrug-resistant bacteria. In this regard, the identification of outer membrane protein A (OmpA) as a key bacte...
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Article
Just passing through
Intracellular protein delivery has been a major challenge in the field of cell biology for decades. Engineering such delivery is a key step in the development of protein- and antibody-based therapeutics. Now, ...
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Article
Open AccessAn optimized method for 15N R1 relaxation rate measurements in non-deuterated proteins
15N longitudinal relaxation rates are extensively used for the characterization of protein dynamics; however, their accurate measurement is hindered by systematic errors. 15N CSA/1H–15N dipolar c...
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Article
Reelin delays amyloid-beta fibril formation and rescues cognitive deficits in a model of Alzheimer’s disease
Reelin is an extracellular matrix protein that is crucial for neural development and adult brain plasticity. While the Reelin signalling cascade has been reported to be associated with Alzheimer’s disease (AD)...
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Article
Open AccessDesign of HR1 and HR2 synthetic peptide analogs: Characterization of their antiviral activities and their capacities to induce neutralizing antibodies
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Protocol
NMR Studies of Protein–Ligand Interactions
Nuclear magnetic resonance (NMR) has evolved into a powerful tool for characterizing protein–ligand interactions in solution under near physiological conditions. It is now frequently harnessed to assess the af...
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Chapter and Conference Paper
A novel family of diketopiperazines as a tool for the study of transport across the blood-brain barrier (BBB) and their potential use as BBB-shuttles.
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Article
Open AccessGold Nanoparticles and Microwave Irradiation Inhibit Beta-Amyloid Amyloidogenesis
Peptide-Gold nanoparticles selectively attached to β-amyloid protein (Aβ) amyloidogenic aggregates were irradiated with microwave. This treatment produces dramatic effects on the Aβ aggregates, inhibiting both...
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Article
Perspectives on NMR in drug discovery: a technique comes of age
In the past decade, the ability of nuclear magnetic resonance (NMR) spectroscopy to provide information on intermolecular interactions that is valuable in drug discovery has been increasingly appreciated. Pell...
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Article
Metabolic Cleavage and Translocation Efficiency of Selected Cell Penetrating Peptides: A Comparative Study with Epithelial Cell Cultures
We investigated the metabolic stability of four cell penetrating peptides (CPPs), namely SAP, hCT(9-32)-br, [Pα] and [Pβ], when in contact with either subconfluent HeLa, confluent MDCK or Calu-3 epithelial cel...
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Article
Chemical Synthesis of 19F-labeled HIV-1 Protease using Fmoc-Chemistry and ChemMatrix Resin
HIV-1 protease (PR) has been extensively studied due to its importance as a target in AIDS therapy. The enzyme can be obtained via expression of its cloned gene in an appropriate system, or via chemical synthe...
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Article
Does the Solid-Phase Synthesis of a Tetrapeptide Represent a Challenge at the Onset of the XXI Century? The Case of Cyclo [(3R)-3-hydroxydecanoyl-l-seryl-(3R)-3-hydroxydecanoyl-l-seryl]
At the beginning of the XXI century, 43 years after the description of the first solid-phase synthesis of a tetrapeptide by Bruce Merrifield, the synthesis of a tetrapeptide may still represent a synthetic cha...
