Beatriz de Pascual‐Teresa

Universidad San Pablo CEU

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Ana Ramos

Universidad San Pablo CEU

José María Zapico

Universidad San Pablo CEU

Sonsoles Martín‐Santamaría

Centro de Investigaciones Biológicas Margarita Salas

Claire Coderch

Universidad San Pablo CEU

Alfredo Martı́nez

Center for Biomedical Research of La Rioja

José Luis López‐Pérez

Universidad de Salamanca

Arturo San Feliciano

Universidad de Salamanca

Kamila Filipiak

Universidad San Pablo CEU

Gonzalo Herradón

Universidad San Pablo CEU

Maciej Masłyk

John Paul II Catholic University of Lublin

Cooperative Institutions

Universidad San Pablo CEU

Consejo Superior de Investigaciones Científicas

Universidad de Alcalá

Universidad San Pablo

Universidad Complutense de Madrid

Centro de Investigaciones Biológicas Margarita Salas

Centre National de la Recherche Scientifique

Instituto de Salud Carlos III

Universidad de Salamanca

Universidad Autónoma de Madrid

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Synthesis, Antitumor Activity, Molecular Modeling, and DNA Binding Properties of a New Series of Imidazonaphthalimides

Journal of Medicinal Chemistry (2002)

Miguel F. Braña Mónica Cacho Mario A. García Beatriz de Pascual‐Teresa Ana Ramos

A series of mono and bisintercalators based on the 5,8-dihydrobenz[de]imidazo[4,5-g]isoquinoline-4,6-dione system were synthesized and evaluated for growth inhibitory properties in several human cell lines. All target compounds showed activity in the micromolar range. Representative compounds were evaluated using UV--vis spectroscopy and viscosimetric determinations, showing that they behave as DNA intercalators. Molecular modeling techniques were used in order to rationalize the moderate activity observed for bisnaphthalimides.

Molecular model

10.1021/jm020950q

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Citations (60)

Labdane acids from polar extracts of Juniperus thurifera

Phytochemistry (1992)

Arturo San Feliciano José M. Miguel del Corral José Luis López‐Pérez Beatriz de Pascual‐Teresa

Labdane

10.1016/0031-9422(92)83134-k

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Citations (7)

Synthesis, cytotoxic activities and proposed mode of binding of a series of bis{[(9-oxo-9,10-dihydroacridine-4-carbonyl)amino]alkyl}alkylamines

European Journal of Medicinal Chemistry (2002)

Miguel F. Braña Luis Casarrubios Gema Domı́nguez Carlos Vilas José M. Pérez

Ethidium bromide

Acridine

Acridine orange

10.1016/s0223-5234(02)01348-x

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Citations (14)

New Advances in the Exploration of Esterases wit PET and Fluorescent Probes

Alba Gil-Rivas Beatriz de Pascual‐Teresa Irene Ortín Ana Ramos

Esterases are hydrolases that catalyze the hydrolysis of esters into the corresponding acids and alcohols. The development of fluorescent probes for detecting esterases is of great importance due to their wide spectrum of biological and industrial applications. These probes can provide a rapid and sensitive method for detecting the presence and activity of esterases in various samples, including biological fluids, food products, and environmental samples. Fluorescent probes can also be used for monitoring the effects of drugs and environmental toxins on esterase activity, as well as to study the functions and mechanisms of these enzymes in several biological systems. Additionally, fluorescent probes can be designed to selectively target specific types of esterases, such as those found in pathogenic bacteria or cancer cells. In this review, we summarize the recent fluorescent probes described for the visualization of cell viability and some applications for in vivo imaging. On the other hand, Positron Emission Tomography (PET) is a nuclear-based molecular imaging modality of great value to study the activity of enzymes in vivo. We provide some examples of PET probes for imaging acetylcholinesterases and butyrylcholinesterases in brain, which are valuable tools for diagnosing dementia and monitoring the effects of anticholinergic drugs on the central nervous system.

Esterase

Molecular Imaging

10.20944/preprints202308.0118.v1

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Citations (1)

Control of the exo and endo Pathways of the Diels-Alder Reaction by Antibody Catalysis

Science (1993)

Véronique Gouverneur K. N. Houk Beatriz de Pascual‐Teresa Brett R. Beno Kim D. Janda

Catalytic antibodies that control the reaction pathways of the Diels-Alder cycloaddition have been generated. One antibody catalyzes the favored endo and the other the disfavored exo pathway to yield the respective cis and trans adducts in enantiomerically pure form. A comparison of the x-ray structure of the hapten with the calculated geometry of the transition structure showed that [2.2.2] bicyclic compounds are excellent mimics of the transition state of the Diels-Alder reaction. To achieve catalysis and the high degree of stereoselectivity shown here, the antibody must simultaneously control the conformation of the individual reactants and their relation to each other. In the case of the disfavored process, binding energy must be used to reroute the reaction along a higher energy pathway. The rerouting of reaction pathways has become a major focus of antibody catalysis and other disfavored reactions can be expected to be catalyzed so long as the energy barrier is not extreme. The energy requirements needed for absolute control of all of the stereoisomers of many Diels-Alder reactions fall in the energy range (approximately 20 kilocalories per mole) deliverable by antibody binding.

Diels–Alder reaction

Reactivity

Transition state

10.1126/science.8211138

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Citations (210)

Inhibition of RPTPβ/ζ blocks ethanol-induced conditioned place preference in pleiotrophin knockout mice

Behavioural Brain Research (2019)

Rosalía Fernández‐Calle Esther Gramage José María Zapico Beatriz de Pascual‐Teresa Ana Ramos

Pleiotrophin

Conditioned place preference

Midkine

Knockout mouse

10.1016/j.bbr.2019.111933

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Citations (12)

Small‐Molecule Negative Modulators of Adrenomedullin: Design, Synthesis, and 3D‐QSAR Study

ChemMedChem (2008)

Virginia Roldós Sonsoles Martín‐Santamaría Miguel Julián Alfredo Martı́nez Laurence Choulier

Adrenomedullin (AM) is a peptidic hormone that was isolated in 1993, the function of which is related to several diseases such as diabetes, hypertension, and cancer. Compound 1 is one of the first nonpeptidic small-molecule negative modulators of AM, identified in a high-throughput screen carried out at the National Cancer Institute. Herein we report the synthesis of a series of analogues of 1. The ability of the synthesized compounds to disrupt the binding between AM and its monoclonal antibody has been measured, together with surface plasmon resonance (SPR)-based binding assays as implemented with Biacore technology. These data were used to derive a three-dimensional quantitative structure-activity relationship (3D-QSAR) model, with a q(2) (LOO) value of 0.8240. This study has allowed us to identify relevant features for effective binding to AM: the presence of a hydrogen-bond donor group and an aromatic ring. Evaluation of the ability of selected compounds to modify cAMP production in Rat2 cells showed that the presence of a free carboxylic acid is essential for negative AM modulation.

Adrenomedullin

High-Throughput Screening

Loo

10.1002/cmdc.200800066

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Citations (8)

Stereoselectivities of thermal and Lewis acid catalyzed Diels-Alder reactions of 1,2,2-trimethylpropyl acrylate with cyclopentadiene

Tetrahedron Letters (1994)

Beatriz de Pascual‐Teresa K. N. Houk

Cyclopentadiene

Diels–Alder reaction

Methyl acrylate

Lewis acid catalysis

10.1016/s0040-4039(00)76518-x

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Citations (4)

Pharmacological inhibition of Receptor Protein Tyrosine Phosphatase β/ζ (PTPRZ1) modulates behavioral responses to ethanol

Neuropharmacology (2018)

Rosalía Fernández‐Calle Marta Vicente‐Rodríguez Miryam Pastor Esther Gramage Bruno Di Geronimo

Pleiotrophin

Midkine

10.1016/j.neuropharm.2018.04.027

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Citations (18)

Dietary gallic acid and anthocyanin cytotoxicity on human fibrosarcoma HT1080 cells. A study on the mode of action

Food & Function (2013)

Kamila Filipiak Manuel Hidalgo José Manuel Silván Benjamin Fabre Rodrigo J. Carbajo

Gallic acid and anthocyanins are abundant plant food bioactives present in many fruits and vegetables, being especially important in the composition of berries. Gallic acid has been shown to possess cytotoxic properties in several cancer cell lines and to inhibit carcinogenesis in animal models. However, its mechanism of action is not yet fully understood. The aim of this study was to elucidate whether the observed inhibitory activity of gallic acid against gelatinases corresponds to its cytotoxic activity in HT1080 cells and to determine if anthocyanins could exhibit a similar behavior. Gallic acid and delphinidin-3-glucoside have shown selective cytotoxicity towards HT1080 cells. Further analysis by a migration and invasion assay showed anti-invasive activities of gallic acid, delphinidin and pelargonidin-3-glucosides. Zymographic analysis demonstrated the inhibitory activity of gallic acid at the level of secreted and activated gelatinases. Moreover, gallic acid inhibited MMP-2 and MMP-9 proteolytic activity with very similar potency. NMR and molecular modelling experiments confirmed the interaction of gallic acid with MMP-2, and suggested that it takes place within the catalytic center. In this work we give some new experimental data supporting the role of these compounds in the inhibition of metalloproteases as the mechanism for their cytotoxic activity against fibrosarcoma.

HT1080

Mode of Action

10.1039/c3fo60465a

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Citations (40)