WorldCat Identities

Giralt, Ernest

Overview
Works: 101 works in 190 publications in 3 languages and 1,082 library holdings
Genres: Conference papers and proceedings 
Roles: Author, Contributor, Editor, Thesis advisor, Publishing director, Other, Opponent, dgs
Classifications: QP551, 547.75
Publication Timeline
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Most widely held works by Ernest Giralt
Protein surface recognition : approaches for drug discovery by Ernest Giralt( )

19 editions published between 2010 and 2011 in English and held by 338 WorldCat member libraries worldwide

A new perspective on the design of molecular therapeutics is emerging. This new strategy emphasizes the rational complementation of functionality along extended patches of a protein surface with the aim of inhibiting protein/protein interactions. The successful development of compounds able to inhibit these interactions offers a unique chance to selectively intervene in a large number of key cellular processes related to human disease. Protein Surface Recognition presents a detailed treatment of this strategy, with topics including:
Chemical approaches to the synthesis of peptides and proteins by Paul Lloyd-Williams( Book )

11 editions published between 1997 and 2020 in English and held by 309 WorldCat member libraries worldwide

This book describes the state of the art in efficient methods for the synthesis of both natural and artificial large peptide and protein molecules. Topics include an introduction to basic concepts, linear solid-phase synthesis of peptides, peptide synthesis in solution, convergent solid-phase synthesis, methods for the synthesis of branched peptides, and much more. Strategies and tactics that must be considered for the successful synthesis of peptides are emphasized
Piperidine : structure, preparation, reactivity, and synthetic applications of piperidine and its derivatives by Mario Rubiralta( Book )

9 editions published in 1991 in English and held by 173 WorldCat member libraries worldwide

Piperidine, one of the simplest heterocyclic systems, is found in nature as part of several alkaloid compounds. Both natural and especially unnatural piperidine derivatives present interesting pharmacological properties. From a structural viewpoint, the conformation of piperidine has been the subject of one of the fiercest controversies in structural organic chemistry in the last few years. As a result of the combined use of several spectroscopic techniques, the conformational behavior of most types of piperidine-related compounds has been clarified. Some piperidine derivatives, namely, N>
Peptides, 1990 : proceedings of the Twenty-First European Peptide Symposium, September 2-8, 1990, Platja d'Aro, Spain by European Peptide Symposium( Book )

8 editions published between 1990 and 1991 in English and held by 49 WorldCat member libraries worldwide

Percepció social de la biotecnologia = Percepción social de la biotecnología = The social perception of biotechnology by Victoria Camps( )

2 editions published in 2000 in Spanish and English and held by 38 WorldCat member libraries worldwide

Introducción a la estereoquímica de los compuestos orgánicos by Ernest Giralt( Book )

4 editions published in 1984 in Spanish and Undetermined and held by 16 WorldCat member libraries worldwide

Reconeixement molecular de superfícies proteiques by Ernest Giralt( Book )

2 editions published in 2008 in Catalan and held by 8 WorldCat member libraries worldwide

Piperidine by Mario Rubiralta( Book )

2 editions published in 1991 in English and held by 5 WorldCat member libraries worldwide

Reconeixement molecular de superfícies proteiques by Ernest Giralt( Book )

3 editions published in 2008 in Catalan and held by 5 WorldCat member libraries worldwide

Problemas de sintesis en el grupo del 6,7-Benzomorfano by Ernest Giralt( Book )

4 editions published in 1975 in Spanish and held by 4 WorldCat member libraries worldwide

Structural studies of proteins and protein complexes by mass spectrometry and atomic force microscopy by Stéphanie Boussert( Book )

3 editions published in 2008 in English and held by 3 WorldCat member libraries worldwide

Desarrollo y aplicación de experimentos de 1H-RMN multidimentsionales homonucleares al estudio de sistemas complejos by Francisco Cárdenas López( )

2 editions published in 2012 in Spanish and held by 2 WorldCat member libraries worldwide

Development of new antimicrobial peptides and peptidomimetics and mechanism of resistance to peptide antibiotics by Xavier Vila Farrés( Book )

2 editions published between 2014 and 2015 in English and held by 2 WorldCat member libraries worldwide

Actualment al mon hi ha un greu problema derivat de dos factors relacionats, el primer factor es el increment de la resistència, especialment del bacteris del grup ESKAPE. El segon factor es la disminució dràstica en el nombre d'antibiòtics aprovats per la FDA. Aquests dos problemes fan que hi hagi una urgència per trobar nous antimicrobians efectius en front d'aquestes soques resistents. En aquesta tesi hem abordat dos temes diferents però que estan relacionats a la hora de trobar nous antibiòtics. El primer tema abordat es el de conèixer a fons els mecanismes de resistència de certs antibiòtics, en aquest cas peptídics, en front diferents tipus de soques tant Gram-positives (S. mitis) com Gram-negatives (A. nosocomialis). Els dos antibiòtics peptídics pels que s'ha estudiat la resistència son daptomicina i colistina, en front de S. mitis i A. nosocomialis respectivament. Ambdós pèptids actuen a nivell de membrana, per tant ens centrarem en veure les modificacions produïdes en els soques resistents. Per part de S. mitis resistent a daptomicina, es pot veure una sobreexpressió de dues proteïnes que tenen dominis homòlegs amb altres proteïnes involucrades en la resistència a daptomicina en altres bacteris. En la resistència a colistina es pot apreciar com les soques resistents d'A. nosocomialis presenten una deficiència del LPS. També hem proposat diferents alternatives com a nous antibiòtics, en aquest cas en front de soques A. baumannii. Dos tipus d'aproximacions van ser utilitzades, la primera, i mes clàssica es la de trobar nous antimicrobians, vàrem trobar mastoparan i va diferents paràmetres van ser optimitzat però sense obtindré bons resultats in vivo. També es van provar diferents pèptids provinents de les secrecions de les granotes, presentant bona activitat en front soques d'Acinetobacter, i per últim, les ceragenines, anàlegs del àcid cólic, que tenen bona activitat en front de totes les soques tant colistina sensibles com colistina resistents en Gram-negatius. La segona aproximació es buscant pèptids capaços d'inhibir l'adherència entre el bacteri i la cèl·lula del hoste bloquejant l'acció de la proteïna OmpA. S'ha trobat un pèptid amb bona activitat fins i tot in vivo
Study of the conformational dynamics of prolyl oligopeptidase by Abraham López Asamar( Book )

2 editions published in 2015 in English and held by 2 WorldCat member libraries worldwide

La prolil oligopeptidasa (POP) es un enzim de 81 KDa que hidrolitza pèptids curts amb contingut en prolina. La POP actua en el sistema nerviós central mitjançant interaccions proteïna-proteïna (IPP), i la seva funció biològica està relacionada amb la memòria i els processos cognitius. Per aquesta raó, els inhibidors de la POP són compostos d'interès terapèutic per al tractament dels dèficits cognitius. Recentment, s'ha descobert que els inhibidors de la POP poden prevenir la patogènesis de la malaltia de Pàrkinson, probablement a través d'una interacció directa entre la POP i l'a-sinucleïna (la principal proteïna causant dels processos neurodegeneratius de la malaltia de Parkinson). Tot i que l'estructura cristal·logràfica de la POP està ben definida, no es sap quines són les transicions conformacionals que permeten completar el cicle catalític de la POP. Probablement, aquesta riquesa conformacional també té un paper rellevant en el control de les IPP. Malauradament, l'estudi conformacional complet de la POP és tot un repte degut al seu elevat pes molecular. En aquesta tesis doctoral s'ha emprat una combinació de tècniques biofísiques avançades (en concret, la resonància magnètica nuclear, la dispersió de raigs X de baix angle, i l'espectrometria de masses de mobilitat iònica) conjuntament amb simulacions de dinàmica molecular, per tal d'analitzar la dinàmica conformacional de la POP en solució. A més, s'ha estudiat la possible interacció entre la POP i l'a-sinucleïna mitjançant experiments de RMN. Els resultats obtinguts en aquesta tesi doctoral han demostrat que la POP es troba en solució en un equilibri conformacional lent entre conformacions obertes i tancades, originades a partir de la separació entre dos dominis. Els inhibidors de la POP causen una gran estabilització de la conformació tancada, amb la qual cosa l'equilibri dinàmic es desplaça totalment cap a aquesta conformació. A més, es va poder detectar una interacció dèbil i transitòria entre la POP i l'a-sinucleïna, que esdevenia especialment afavorida en la presència d'inhibidors. Així, els nostres resultats suggereixen que la diversitat conformacional de la POP es necessària per a la seva funció, i que els inhibidors poden desencadenar la seva funció biològica desplaçant l'equilibri conformacional
A MALDI-TOF-based Method for Studying the Transport of BBB Shuttles--Enhancing Sensitivity and Versatility of Cell-Based In Vitro Transport Models by Pol Arranz-Gibert( )

1 edition published in 2019 in English and held by 2 WorldCat member libraries worldwide

Design, synthesis and biophysical evaluation of peptides targeting pharmacologically relevant proteins by Salvador Guardiola Bagán( )

2 editions published between 2017 and 2018 in English and held by 2 WorldCat member libraries worldwide

Protein-protein interactions (PPIs) and protein surfaces are considered challenging targets for drug discovery. In this field, conventional medicinal chemistry (i.e. small molecules) has largely failed to provide effective hits. On the other hand, peptides are endowed with a higher degree of structural flexibility (which allows them to better adapt to irregular targets) and are able to display a variety of tailor-made topologies, emerging as an alternative to target proteins that were considered undruggable. In this thesis, we have explored the potential of designed peptides to modulate the function of two therapeutically relevant protein targets involved in cancer (epidermal growth factor, EGF) and cognitive disorders (prolyloligopeptidase, POP). Regarding the discovery of peptide ligands against EGF, docking tools have allowed the de novo design of a family of small peptides, which have shown a reproducible, albeit weak, binding to EGF. In order to obtain more active candidates, the relevant interacting regions of EGFR have been identified and mimicked with a diversity of cycle-constrained peptides. These are larger and structurally richer scaffolds that have proved more efficient in targeting a small and featureless protein, such as EGF. The best peptide hit, a 28-mer cyclic miniprotein (cp28), has served as the starting point in a computer-guided optimization process that strived for more active and structurally constrained analogues. Our design effort has resulted in a series of bicyclic peptides that mimic the mode of binding of cp28 to EGF, albeit with reduced size, increased hydrophilicity and a more restrained topology. The chemical synthesis of these complex bicyclic molecules was enabled by state-of-the-art native chemical ligation techniques. In order to assess the binding of our peptides with EGF, an array of suitable biophysical techniques was explored, and the most suitable ones were implemented to our discovery process. In particular, NMR spectroscopy (combined with expression of recombinant 15N-EGF) has allowed the monitoring of ligand-induced changes on the protein NMR spectra. In parallel, a recently developed acoustic biosensor (SAW) was set up as a low-cost, label-free, and highly sensitive technique to quantify the interactions with EGF. Moreover, our best peptide candidates (cp28 and cp23G) were able to disrupt the EGF-EGFR interaction, an effect that has been tested in several cell-like and living cell assays. Indeed, these peptides were able to halt the proliferation of EGFR(+) human carcinoma cells, an effect that underlines their biological efficacy. Moreover, the bicycle-constrained analogues display an exceptional level of biological stability, especially in serum and hepatic media. In the last part of this thesis, a series of bioactive peptides has been designed with a fundamentally different mechanism of action. Peptides typically possess fast dissociation rates from the protein target, a feature that represents an obstacle when competing with endogenous ligands for the binding to cavities, such as catalytic sites in enzymes. As a proof of concept, a novel class of covalent-acting peptidomimetics were developed to supress the activity of POP, a protease involved in neurodegenerative disorders. In these bifunctional molecules, the peptide backbone and side chains formed a template that selectively binds to the POP active site, whereas a novel sulfonyl fluoride electrophile was optimally positioned to react with the catalytic Ser residue. These compounds showed a high potency in vitro, being able to inactivate POP at low nM concentrations, and their mechanism of action as irreversible inhibitors was confirmed by kinetic assays. Moreover, they displayed a remarkable selectivity against closely related proteases, and they were able to permeate through a lipid bilayer that mimics the composition of the blood- brain barrier. In summary, our findings show how two completely different classes of peptides, bicycle-constrained miniproteins and covalent-acting peptidomimetics, with binding affinities several orders of magnitude apart, can be efficiently designed to target specific protein surfaces. With PPIs and challenging binding sites becoming the focus of current drug discovery projects, these type of ligands are ideally positioned to deliver new drugs for the treatment of disease. -- TDX
Peptide tools for intracellular delivery by Irene Martín Badajoz( )

2 editions published in 2012 in English and held by 2 WorldCat member libraries worldwide

Use of calix[4]arenes to recover the self-assembly ability of mutated p53 tetramerization domains by Susana Gordo Villoslada( )

2 editions published in 2008 in Spanish and English and held by 2 WorldCat member libraries worldwide

Algorithm-supported, mass and sequence diversity-oriented random peptide library design by Daniela Kalafatovic( )

1 edition published in 2019 in English and held by 2 WorldCat member libraries worldwide

NMR in drug discovery from screening to structure-based design of antitumoral agents by Ricard A Rodríguez Mias( Book )

2 editions published between 2006 and 2007 in English and held by 2 WorldCat member libraries worldwide

 
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Chemical approaches to the synthesis of peptides and proteins
Covers
Chemical approaches to the synthesis of peptides and proteins
Alternative Names
Ernest Giralt i Lledó chimiste espagnol

Ernest Giralt i Lledó Químic català

Ernest Giralt i Lledó Spaans hoogleraar

Ernest Giralt i Lledó Spanish university teacher, researcher and professor

Ernest Giralt Lledó químico y catedrático universitario español

Giralt, Ernest.

Giralt, Ernest (Giralt Lledó)

Giralt i Lledó, Ernest

Giralt Lledó, Ernesto

Lledó, Ernest Giralt.

Languages
English (66)

Spanish (11)

Catalan (5)