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

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Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein that is overexpressed on the surface of cancerous prostate cells both in primary tumors and in metastases. Small organic ligands targeting PSMA have been broadly and successfully use ...

Cysteine cathepsins proteases are enzymes that play essential physiological roles, but their activity is also associated to different aspects of cancer progression and to the development of other diseases. Therefore, cysteine cathepsins are relevant and pr ...

Retinoblastoma, while relatively rare, stands as the most prevalent intraocular cancer. In Switzerland, the survival rate approaches 100%, but it drops to less than 50% in low-income countries. The current treatment options for retinoblastoma rely on a lim ...

The serine proteases CAP1/Prss8 and CAP3/St14 are identified as ENaC channel-activating proteases in vitro, highly suggesting that they are required for proteolytic activation of ENaC in vivo. The present study tested whether CAP3/St14 is relevant for rena ...

Gain-of-function mutations in NOTCH1 are among the most frequent genetic alterations in T-cell acute lymphoblastic leukemia (T-ALL), highlighting the Notch signaling pathway as a promising therapeutic target for personalized medicine. Yet, a major limitati ...

Peptides represent a promising molecular class for drug development. They combine several strengths of small molecules (e.g. efficient tissue diffusion, low immunogenicity and access to chemical synthesis) and key properties of biologics such as monoclonal ...

Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...

The goal of retinoblastoma (RB) treatment is to save the child's life, eyes and functional vision, with that order of priority. The management of RB is complex and involves strategically chosen methods of surgical enucleation, external beam radiotherapy, i ...

Therapeutic Drug Monitoring (TDM) is a key concept in precision medicine. The goal of TDM is to avoid therapeutic failure or toxic effects of a drug due to insufficient or excessive circulating concentration exposure related to between-patient variability ...

Human serum albumin (hSA) is the major carrier protein for fatty acids (FAs) in plasma. Its ability to bind multiple FA moieties with moderate to high affinity has inspired the use of FA conjugation as a safe and natural platform to generate long-lasting t ...

Peptides represent a promising format for the development of therapeutics since they combine the advantages of proteins and small molecules. Several techniques based on rational design or in vitro evolution can be used to develop peptides as therapeutics. ...

Cyclic peptides can bind to protein targets with high affinities and selectivities, which makes them an attractive modality for the development of research reagents and therapeutics. Additional properties, including low inherent toxicity, efficient chemica ...

Cyclic peptides are ring-shaped molecules that emerged as a promising class of therapeutics. While it is often difficult to find small molecule binders for challenging disease targets, cyclic peptides can bind to featureless surfaces or inhibit protein-pro ...

Mass spectrometry (MS) has emerged over the last two decades as the analytical technique of choice in systems-level protein studies, known as proteomics. Two are the MS-based approaches generally applied to proteomics: bottom-up (BU), which relies on the p ...

Nanoparticle-based drug delivery systems have the potential for increasing the efficiency of chemotherapeutics by enhancing the drug accumulation at specific target sites, therebyreducing adverse side effects and mitigating patient acquired resistance. In ...

Regenerative medicine aims to repair body tissues when natural mechanisms fail. Growth factors (GFs) are essential proteins that promote tissue regeneration upon injury, and as such, are very promising therapeutic drugs in regenerative medicine. Due to the ...

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...

In order to improve the efficacy and safety of treatments, drug dosage needs to be adjusted to the actual needs of each patient in a truly personalized medicine approach. Key for widespread dosage adjustment is the availability of point-of-care devices abl ...

Therapeutic Drug Monitoring (TDM) is considered one of the most successful approaches to personalized medicine. However, the accuracy requirements on the quantification of drug concentration and the challenges in the dose adjustment limit the application o ...

Nowadays, drug encapsulation and drug release from cellulose nanofibrils systems are intense research topics, and commercial grades of cellulose nanomaterials are currently available. In this work we present an ester-containing prodrug of metronidazole tha ...

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

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PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer

Development of cysteine cathepsin inhibitors combined with cell type-specific delivery for the treatment of B-cell lymphoma and solid tumors

Optimised three-dimensional in vitro retinoblastoma models tailored for drug discovery and clinical translatability

Kidney-Specific Membrane-Bound Serine Proteases CAP1/Prss8 and CAP3/St14 Affect ENaC Subunit Abundances but Not Its Activity

Resistance mechanism to Notch inhibition and combination therapy in human T-cell acute lymphoblastic leukemia

Development of cyclic peptide inhibitors of coagulation factor XII and matrix metalloproteinase 2

Development of cyclic peptides that can be administered orally to inhibit disease targets

Repurposed drug combination via high-throughput screening and dual drug delivery system development for the treatment of retinoblastoma

TUCUXI: TUCUXI: An Intelligent System for Personalized Medicine from Individualization of Treatments to Research Databases and Back

Molecular analysis and therapeutic applications of human serum albumin-fatty acid interactions

Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics

Phage Selection of Cyclic Peptides for Application in Research and Drug Development

De novo developed small cyclic peptides that are orally available

Middle-down approaches for mass spectrometry-based protein identification and characterization

Photoresponsive Nanocarriers Based on Lithium Niobate Nanoparticles for Harmonic Imaging and On-Demand Release of Anticancer Chemotherapeutics

Therapeutic Proteins Engineered for Super-Affinity to the Extracellular Matrix in Regenerative Medicine

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Label-Free Detection of Tobramycin in Serum by Transmission-Localized Surface Plasmon Resonance

Quantification of low molecular weight drugs : from the selection of nucleic acid-based capture molecules to the characterization in patient samples

Two-step immobilization of metronidazole prodrug on TEMPO cellulose nanofibrils through thiol-yne click chemistry for in situ controlled release