Elena Pazos

University of A Coruña | UDC · Centre for Advanced Scientific Research (CICA) and Department of Chemistry

Long-term delivery is a successful strategy used to reduce the adverse effects of monoclonal antibody (mAb)-based treatments. Macroporous hydrogels and affinity-based strategies have shown promising results in sustained and localized delivery of the mAbs. Among the potential tools for affinity-based delivery systems, the de novo designed Ecoil and...

A C-N bond-forming cross-dehydrogenative coupling of a collection of Tyr-containing peptides and estrogens with heteroarenes is described. This oxidative coupling is distinguished by its scalability, operational simplicity, and air tolerance and enables the appendance of phenothiazines and phenoxazines in phenol-like compounds. When incorporated in...

We present herein the synthesis of a new polycationic pseudo[1]rotaxane, self-assembled in excellent yield through hydrazone bonds in aqueous media of three different aldehyde and hydrazine building blocks. A thermodynamically controlled process has been studied sequentially by analyzing the [1 + 1] reaction of a bisaldehyde and a trishydrazine lea...

Tyrosine nitration, a post-translational modification (PTM) that takes place under nitrosative stress conditions, occurs through a non-enzymatic peroxynitrite-mediated reaction. Although protein nitration has long been considered an irreversible PTM involved in nitrosative stress-associated diseases, it has also been suggested to be a regulatory me...

We present herein the development of a series of viologen–amino acid hybrids, obtained in good yields either by successive alkylations of 4,4′-bipyridine, or by Zincke reactions followed by a second alkylation step. The potential of the obtained amino acids has been exemplified, either as typical guests of the curcubituril family of hosts (particul...

Many cellular processes in living organisms are regulated by complex regulatory networks, built from noncovalent interactions between relatively few proteins that perform their functions by switching between homo- and heterooligomeric assemblies or mono- and bivalent states. Herein, we demonstrate that the conjugation of a 4,4'-bipyridinium scaffol...

We present herein the implementation of pH-responsiveness into a new polycationic macrobicyclic structure, namely what we have termed the “red cage”. The hydrolytically-stable cryptand–like compound has been prepared in an...

Peptides have become excellent platforms for the design of peptide–nanoparticle hybrid superstructures, owing to their self-assembly and binding/recognition capabilities. Morover, peptide sequences can be encoded and modified to finely tune the structure of the hybrid systems and pursue functionalities that hold promise in an array of high-end appl...

Synthetic supramolecular chemistry pursues not only the construction of new matter, but also control over its inherently dynamic behaviour. In this context, classic host–guest chemistry, based on the development of a myriad of macrocyclic receptors with fine-tuned affinities and selectivities, has enormously contributed to the discovery of new chem...

We present herein the development of a new synthetic strategy for the conjugation of 4,4′-bipyridinium derivatives into peptide scaffolds. The methodology, based on the development of a solid-phase version of the Zincke reaction between activated pyridinium salts and amines, is able to produce the desired conjugates in a straightforward fashion, wi...

Functional imaging has become an important tool in oncology because it not only provides information about the size and localization of the tumour, but also about the pathophysiological features of the tumoural cells. One of the characteristic features of some tumour types is that their fast growth leads to deficient intratumoral vascularization, w...

The use of cucurbit[8]uril as molecular host has emerged in the chemical literature as a reliable strategy for the creation of dynamic chemical systems, due to its ability to form homo and heteroternary complexes in aqueous media with appropriate molecular switches as guests. In that manner, CB[8]‐based supramolecular switches can be designed in a...

The use of cucurbit[8]uril as molecular host has emerged in the chemical literature as a reliable strategy for the creation of dynamic chemical systems, due to its ability to form homo and heteroternary complexes in aqueous media with appropriate molecular switches as guests. In that manner, CB[8]‐based supramolecular switches can be designed in a...

In article number 1600163, Ramon A. Alvarez-Puebla and co-workers combine surface-enhanced Raman scattering encoded particles, biorecognition elements (aptamer/antibody) and microfluidics into a device for the optical detection of Staphylococcus aureus in human fluids. The bacteria quantification is achieved for short acquisition time (10 min mL⁻¹)...

Staphylococcus aureus is a common cause of serious infections. One of the main drawbacks in its treatment is the time required for a positive diagnosis, over 24 h, as most methods are still based in bacterial culture. Herein, a microfluidic optical device for the rapid and ultrasensitive quantification of S. aureus in real human fluids is designed....

Blood-based biomarkers (liquid biopsy) offer extremely valua-ble tools for the non-invasive diagnosis and monitoring of tumors. The protein c-MYC, a transcription factor that has been shown to be deregulated in up to 70% of human cancers, can be used as a robust proteomic signature for cancer. Herein, we developed a rapid, highly specific and sensi...

Efficient treatments in bacterial infections require the fast and accurate recognition of pathogens, with concentrations as low as one per milliliter in the case of septicemia. Detecting and quantifying bacteria in such low concentrations is challenging and typically demands cultures of large samples of blood (~1 milliliter) extending over 24–72 ho...

Silver nanoparticles have been of great interest as plasmonic substrates for sensing and imaging, catalysts, or antimicrobial systems. Their physical properties are strongly dependent on parameters that remain challenging to control such as size, chemical composition, and spatial distribution. We report here on supramolecular assemblies of a novel...

A peptide sensor that integrates the 4-dimethylaminophthalimide (4-DMAP) fluorophore in a short cyclin A binding sequence displays a large fluorescence emission increase upon interacting with the cyclin A Binding Groove (CBG). Competitive displacement assays of this probe allow the straightforward identification of peptides that interact with the C...

We describe a ds-oligonucleotide-peptide conjugate that is able to efficiently dismount preformed DNA complexes of the bZIP regions of oncoproteins c-Fos and c-Jun (AP-1), and therefore might be useful as disrupters of AP-1-mediated gene expression pathways.

Signaling pathways based on protein phosphorylation and dephosphorylation play critical roles in the orchestration of complex biochemical events and form the core of most signaling pathways in cells (i.e. cell cycle regulation, cell motility, apoptosis, etc.). The understanding of these complex signaling networks is based largely on the biochemical...

A SERS (surface-enhanced Raman scattering) based sensor was developed for the detection of the oncoprotein c-Jun at nanomolar levels. c-Jun is a member of the bZIP (basic zip-per) family of dimeric transcriptional activators and its overexpression has been associated to carcinogenic mecha-nisms in several human cancers. For our sensing purpose, we...

We report the rational design of a 20-mer basic peptide, derived from the transcriptional antitermination protein N of bacteriophage P22, equipped with a luminescent DOTA[Tb3+] macrocyclic complex and a sensitizing tryptophan antenna. Folding of this peptide into an α helical conformation, which occurs upon binding to its target boxB RNA hairpin, r...

Appending negatively charged Glu(8) tails to a peptide dimer derived from the GCN4 transcription factor leads to an effective suppression of its DNA binding. The specific DNA recognition can be restored by irradiation with UV light by using a photolabile linker between the acidic tail and the DNA binding peptide.

The luminescence of a designed peptide equipped with a coordinatively-unsaturated lanthanide complex is modulated by the phosphorylation state of a serine residue in the sequence. While the phosphorylated state is weakly emissive, even in the presence of an external antenna, removal of the phosphate allows coordination of the sensitizer to the meta...

The interaction of transcription factors with specific DNA sites is key for the regulation of gene expression. Despite the availability of a large body of structural data on protein-DNA complexes, we are still far from fully understanding the molecular and biophysical bases underlying such interactions. Therefore, the development of non-natural age...

We report the design and development of a fluorescent sensor specifically designed to target cyclin A, a protein that plays a key role in the regulation of the cell cycle. Computational studies provide a molecular picture that explains the observed emission increase, suggesting that the 4-DMAP fluorophore in the peptide is protected from the bulk s...

Designed terbium-chelating peptides were used to monitor the formation of leucine zipper associations. The sensing strategy is based on the modulation of the antenna effect from a Trp residue donor and the luminescence increase arising from the folding that takes place upon the formation of the coiled-coil structure. An application in the specific...

The use of fluorescent techniques in biological research is widespread. Many of the techniques rely on the use of fluorescent genetically-encoded tags (namely GFP and its different variants), but small molecules and nanoparticle-based approaches are being increasingly used. Peptides, owing to their modular nature, synthetic accessibility and biomol...

Intermolecular sensitization of lanthanide ions was effectively implemented in the development of fluorescent sensors targeting cyclin A. A chelating unit has been conjugated to peptides containing a known cyclin A binding motif (CBM). Upon interaction of the modified terbium-chelating peptides with the cyclin A substrate recruitment groove, the Tb...