Full Text Journal Articles by
Author Yves Jacquot

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Bioinspired Hybrid Fluorescent Ligands for the FK1 Domain of FKBP52.

Inès Li de la Sierra-Gallay, Mathilde Belnou, Béatrice Chambraud, Melanie Genet, Herman van Tilbeurgh, Magali Aumont-Nicaise, Michel Desmadril, Etienne-Emile Baulieu, Yves Jacquot, Cillian Byrne,

The protein FKBP52 is a steroid hormone receptor coactivator likely involved in neurodegenerative disease. A series of small, water-soluble, bioinspired, pseudopeptidic fluorescent ligands for the FK1 domain of this protein are described. The design is such that engulfing of the ligand in the pocket of this domain is accompanied by ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2020, 63(18):10330-10338]

Cited: 0 times

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Computational Approaches for the Discovery of GPER Targeting Compounds.

Fedora Grande, Maria A Occhiuzzi, Rosamaria Lappano, Francesca Cirillo, Rita Guzzi, Antonio Garofalo, Yves Jacquot, Marcello Maggiolini, Bruno Rizzuti,

Estrogens exert a panel of biological activities mainly through the estrogen receptors α and β, which belong to the nuclear receptor superfamily. Diverse studies have shown that the G protein-coupled estrogen receptor 1 (GPER, previously known as GPR30) also mediates the multifaceted effects of estrogens in numerous pathophysiological events, including ... Read more >>

Front Endocrinol (Lausanne) (Frontiers in endocrinology)
[2020, 11:517]

Cited: 0 times

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Improvement of the anti-proliferative activity of the peptide ERα17p in MCF-7 breast cancer cells using nanodiamonds.

François Yip, Fariba Nemati, Rania El Botty, Mathilde Belnou, Didier Decaudin, Christelle Mansuy, Yves Jacquot,

Nanodiamonds (NDs) are emerging delivery systems with biomedical applications and interesting perspectives in oncology. Their use has been proposed to assist the internalization of anticancer drugs and to decrease administered drug doses. The pro-apoptotic peptide ERα17p, which is issued from the hinge/N-terminus parts of the AF2 region of the human ... Read more >>

Ann Pharm Fr (Annales pharmaceutiques francaises)
[2019, 77(6):488-495]

Cited: 1 time

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GPCR Modulation in Breast Cancer.

Rosamaria Lappano, Yves Jacquot, Marcello Maggiolini,

Breast cancer is the most prevalent cancer found in women living in developed countries. Endocrine therapy is the mainstay of treatment for hormone-responsive breast tumors (about 70% of all breast cancers) and implies the use of selective estrogen receptor modulators and aromatase inhibitors. In contrast, triple-negative breast cancer (TNBC), a ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2018, 19(12):]

Cited: 6 times

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Identification of the Tau phosphorylation pattern that drives its aggregation.

Clément Despres, Cillian Byrne, Haoling Qi, François-Xavier Cantrelle, Isabelle Huvent, Béatrice Chambraud, Etienne-Emile Baulieu, Yves Jacquot, Isabelle Landrieu, Guy Lippens, Caroline Smet-Nocca,

Determining the functional relationship between Tau phosphorylation and aggregation has proven a challenge owing to the multiple potential phosphorylation sites and their clustering in the Tau sequence. We use here in vitro kinase assays combined with NMR spectroscopy as an analytical tool to generate well-characterized phosphorylated Tau samples and show ... Read more >>

Proc Natl Acad Sci U S A (Proceedings of the National Academy of Sciences of the United States of America)
[2017, 114(34):9080-9085]

Cited: 29 times

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ERE-dependent transcription and cell proliferation: Independency of these two processes mediated by the introduction of a sulfone function into the weak estrogen estrothiazine.

Yves Jacquot, Dany Spaggiari, Julie Schappler, Eric Lesniewska, Serge Rudaz, Guy Leclercq,

The synthetic coumestrol derivative 6,12-dihydro-3-methoxy-1-benzopyrano[3,4-b][1,4]benzothiazin-6-one (estrothiazine, ESTZ) has been identified as a weak estrogen receptor α (ERα) ligand unable to compete with tritiated estradiol. The biological activity of this compound, supported by a methoxy group in position 3, seems mainly to result from its capacity to activate ERα dimerization without ... Read more >>

Eur J Pharm Sci (European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences)
[2017, 109:169-181]

Cited: 2 times

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A β-Turn Motif in the Steroid Hormone Receptor's Ligand-Binding Domains Interacts with the Peptidyl-prolyl Isomerase (PPIase) Catalytic Site of the Immunophilin FKBP52.

Cillian Byrne, Morkos A Henen, Mathilde Belnou, François-Xavier Cantrelle, Amina Kamah, Haoling Qi, Julien Giustiniani, Béatrice Chambraud, Etienne-Emile Baulieu, Guy Lippens, Isabelle Landrieu, Yves Jacquot,

The immunophilin FKBP52 interacts with nuclear steroid hormone receptors. Studying the crystal structure of human estrogen receptor α (hERα) and using nuclear magnetic resonance, we show here that the short V(364)PGF(367) sequence, which is located within its ligand-binding domain and adopts a type II β-turn conformation in the protein, binds ... Read more >>

Biochemistry (Biochemistry)
[2016, 55(38):5366-5376]

Cited: 1 time

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ERα dimerization: a key factor for the weak estrogenic activity of an ERα modulator unable to compete with estradiol in binding assays.

Guy Leclercq, Ioanna Laïos, Céline Elie-Caille, Denis Leiber, Guy Laurent, Eric Lesniewska, Zahra Tanfin, Yves Jacquot,

Estrothiazine (ESTZ) is a weak estrogen sharing structural similarities with coumestrol. ESTZ failed to compete with [3H]17β-estradiol ([3H]17β-E2) for binding to the estrogen receptor α (ERα), questioning its ability to interact with the receptor. However, detection by atomic force spectroscopy (AFS) of an ESTZ-induced ERα dimerization has eliminated any remaining ... Read more >>

J. Recept. Signal Transduct. Res. (Journal of receptor and signal transduction research)
[2017, 37(2):149-166]

Cited: 1 time

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Application of Circular Dichroism Spectroscopy to the Analysis of the Interaction Between the Estrogen Receptor Alpha and Coactivators: The Case of Calmodulin.

Emeric Miclet, Sandrine Bourgoin-Voillard, Cillian Byrne, Yves Jacquot,

The estrogen receptor α ligand-binding domain (ERα-LBD) binds the natural hormone 17β-estradiol (E2) to induce transcription and cell proliferation. This process occurs with the contribution of protein and peptide partners (also called coactivators) that can modulate the structure of ERα, and therefore its specificity of action. As with most transcription ... Read more >>

Methods Mol. Biol. (Methods in molecular biology (Clifton, N.J.))
[2016, 1366:241-259]

Cited: 0 times

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The sequence Pro295-Thr311 of the hinge region of oestrogen receptor α is involved in ERK1/2 activation via GPR30 in leiomyoma cells.

Denis Leiber, Fabienne Burlina, Cillian Byrne, Philippe Robin, Christophe Piesse, Lucie Gonzalez, Guy Leclercq, Zahra Tanfin, Yves Jacquot,

The ERα (oestrogen receptor α)-derived peptide ERα17p activates rapid signalling events in breast carcinoma cells under steroid-deprived conditions. In the present study, we investigated its effects in ELT3 leiomyoma cells under similar conditions. We show that it activates ERK1/2 (extracellular-signal-regulated kinase 1/2), the Gαi protein, the trans-activation of EGFR (epidermal ... Read more >>

Biochem. J. (The Biochemical journal)
[2015, 472(1):97-109]

Cited: 6 times

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A Phosphorylation-Induced Turn Defines the Alzheimer's Disease AT8 Antibody Epitope on the Tau Protein.

Neha S Gandhi, Isabelle Landrieu, Cillian Byrne, Predrag Kukic, Laziza Amniai, François-Xavier Cantrelle, Jean-Michel Wieruszeski, Ricardo L Mancera, Yves Jacquot, Guy Lippens,

Post mortem biochemical staging of Alzheimer's disease is currently based on immunochemical analysis of brain slices with the AT8 antibody. The epitope of AT8 is described around the pSer202/pThr205 region of the hyperphosphorylated form of the neuronal protein tau. In this study, NMR spectroscopy was used to precisely map the ... Read more >>

Angew Chem Int Ed Engl (Angewandte Chemie (International ed. in English))
[2015, 54(23):6819-6823]

Cited: 14 times

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Concentration-dependent and surface-assisted self-assembly properties of a bioactive estrogen receptor α-derived peptide.

Francesco Simone Ruggeri, Cillian Byrne, Lucie Khemtemourian, Guylaine Ducouret, Giovanni Dietler, Yves Jacquot,

We have synthesized a 17-mer peptide (ERα17p) that is issued from the hinge region of the estrogen receptor α and which activates the proliferation of breast carcinoma cells in steroid-deprived conditions. In the present paper, we show that at a concentration of ~50 μM, it rapidly forms amyloid-like fibrils with the ... Read more >>

J. Pept. Sci. (Journal of peptide science : an official publication of the European Peptide Society)
[2015, 21(2):95-104]

Cited: 6 times

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Stabilisation of a short α-helical VIP fragment by side chain to side chain cyclisation: a comparison of common cyclisation motifs by circular dichroism.

Lukasz Frankiewicz, Cecilia Betti, Karel Guillemyn, Dirk Tourwé, Yves Jacquot, Steven Ballet,

A model octapeptide segment derived from vasoactive intestinal peptide (VIP) was utilised to investigate the effect of several conventional cyclisation methods on the α-helical conformation in short peptide fragments. Three of the classical macrocyclisation techniques (i.e. lactamisation, ring-closing metathesis and Huisgen cycloaddition) were applied, and the conformations of the resulting ... Read more >>

J. Pept. Sci. (Journal of peptide science : an official publication of the European Peptide Society)
[2013, 19(7):423-432]

Cited: 7 times

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Electronic effects of 11β substituted 17β-estradiol derivatives and instrumental effects on the relative gas phase acidity.

Sandrine Bourgoin-Voillard, Françoise Fournier, Carlos Afonso, Emilie-Laure Zins, Yves Jacquot, Claude Pèpe, Guy Leclercq, Jean-Claude Tabet,

Numerous studies have highlighted the role of the proton donor characteristics of the phenol group of 17β-estradiol (E(2)) in its association with the estrogen receptor alpha (ERα). Since the substitutions at position C((11)) have been reported to modulate this association, we hypothesized that such substitutions may modify the phenol acidity. ... Read more >>

J. Am. Soc. Mass Spectrom. (Journal of the American Society for Mass Spectrometry)
[2012, 23(12):2167-2177]

Cited: 1 time

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Interactions of isoflavones and other plant derived estrogens with estrogen receptors for prevention and treatment of breast cancer-considerations concerning related efficacy and safety.

Guy Leclercq, Yves Jacquot,

Phytoestrogens are natural endocrine disruptors that interfere with estrogenic pathways. They insert directly within the hormone-binding domain of ERα and β, with a preference for the β isoform of which the concentration predominates in the normal mammary epithelium. Since ERβ antagonizes the growth promoting effect of ERα, which is mainly ... Read more >>

J. Steroid Biochem. Mol. Biol. (The Journal of steroid biochemistry and molecular biology)
[2014, 139:237-244]

Cited: 18 times

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Whole transcriptome analysis of the ERα synthetic fragment P295-T311 (ERα17p) identifies specific ERα-isoform (ERα, ERα36)-dependent and -independent actions in breast cancer cells.

George Notas, Marilena Kampa, Vassiliki Pelekanou, Maria Troullinaki, Yves Jacquot, Guy Leclercq, Elias Castanas,

ERα17p is a peptide corresponding to the sequence P295LMIKRSKKNSLALSLT311 of the estrogen receptor alpha (ERα) and initially found to interfere with ERα-related calmodulin binding. ERα17p was subsequently found to elicit estrogenic responses in E2-deprived ERα-positive breast cancer cells, increasing proliferation and ERE-dependent gene transcription. Surprisingly, in E2-supplemented media, ERα17p-induced apoptosis ... Read more >>

Mol Oncol (Molecular oncology)
[2013, 7(3):595-610]

Cited: 6 times

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ERα17p, a peptide reproducing the hinge region of the estrogen receptor α associates to biological membranes: A biophysical approach.

Cillian Byrne, Lucie Khemtémourian, Vassiliki Pelekanou, Marilena Kampa, Guy Leclercq, Sandrine Sagan, Elias Castanas, Fabienne Burlina, Yves Jacquot,

Recently, we identified a peptide (ERα17p, P(295)LMIKRSKKNSLALSLT(311)) that corresponds to the 295-311 sequence of the estrogen receptor α (ERα, hinge region) and which exerts a panel of pharmacological effects in breast cancer cells. Remarkably, these effects can result from the interaction of ERα17p with the plasma membrane. Herein, we show ... Read more >>

Steroids (Steroids)
[2012, 77(10):979-987]

Cited: 7 times

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Biophysical studies of the interaction between calmodulin and the R²⁸⁷-T³¹¹ region of human estrogen receptor α reveals an atypical binding process.

Ludovic Carlier, Cillian Byrne, Emeric Miclet, Sandrine Bourgoin-Voillard, Magali Nicaise, Jean-Claude Tabet, Michel Desmadril, Guy Leclercq, Olivier Lequin, Yves Jacquot,

The transcriptional activity of human estrogen receptor ERα is modulated by a number of coregulatory proteins among which calmodulin (CaM). Segment 295-311 in the hinge region of ERα has previously been proposed to be the CaM binding site. In this work, we investigate the molecular mechanism of the interaction of ... Read more >>

Biochem. Biophys. Res. Commun. (Biochemical and biophysical research communications)
[2012, 419(2):356-361]

Cited: 6 times

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ERα17p, an ERα P295 -T311 fragment, modifies the migration of breast cancer cells, through actin cytoskeleton rearrangements.

Marilena Kampa, Vassiliki Pelekanou, Dominique Gallo, George Notas, Maria Troullinaki, Iosif Pediaditakis, Ioannis Charalampopoulos, Yves Jacquot, Guy Leclercq, Elias Castanas,

Recently, our knowledge on estrogen receptor alpha (ERα) functions and fate has progressed: ERα enters in repeated transcription-modulating cycles (nucleus/cytoplasm/membrane trafficking processes and proteasomal degradation) that are governed by specific protein-protein interactions. Receptor fragments, especially those resulting from the proteolysis of its ligand binding domain, as well as corresponding synthetic ... Read more >>

J. Cell. Biochem. (Journal of cellular biochemistry)
[2011, 112(12):3786-3796]

Cited: 6 times

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A critical view of the effects of phytoestrogens on hot flashes and breast cancer risk.

Pascale This, Patricia de Cremoux, Guy Leclercq, Yves Jacquot,

The increased risk of breast cancer recently observed with some specific estro-progestin associations has raised concerns about the harmful effects of menopausal hormone replacement therapy (HRT). It has been proposed that phytoestrogens (PEs), which have a similar chemical structure to estrogens, could be used as HRT. The main selling points ... Read more >>

Maturitas (Maturitas)
[2011, 70(3):222-226]

Cited: 14 times

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Peptides targeting estrogen receptor alpha-potential applications for breast cancer treatment.

Guy Leclercq, Dominique Gallo, Janine Cossy, Ioanna Laïos, Denis Larsimont, Guy Laurent, Yves Jacquot,

Activation of the estrogen receptor alpha (ERα) is of prime importance for the development of hormone-dependent breast cancers. Hence, drugs able to impede the emergence of an active folding of ERα have been used for a long time as a first line therapeutic strategy. Aromatase inhibitors that block estradiol synthesis ... Read more >>

Curr. Pharm. Des. (Current pharmaceutical design)
[2011, 17(25):2632-2653]

Cited: 7 times

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The estrogen receptor alpha-derived peptide ERα17p (P(295)-T(311)) exerts pro-apoptotic actions in breast cancer cells in vitro and in vivo, independently from their ERα status.

Vassiliki Pelekanou, Marilena Kampa, Dominique Gallo, George Notas, Maria Troullinaki, Hugues Duvillier, Yves Jacquot, Efstathios N Stathopoulos, Elias Castanas, Guy Leclercq,

In recent years, our knowledge on estrogen receptors (ER) has been modified profoundly with the identification and the deciphering of the role of its protein effectors, as well as with the deeper insight of its molecular structure/function dynamics, characteristics associated with its nucleo-cytoplasmic-membrane shuttling properties. Also, significant progress has been made ... Read more >>

Mol Oncol (Molecular oncology)
[2011, 5(1):36-47]

Cited: 9 times

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Lack of sufficient information on the specificity and selectivity of commercial phytoestrogens preparations for therapeutic purposes.

Guy Leclercq, Patricia de Cremoux, Pascale This, Yves Jacquot,

Phytoestrogens (PEs) are polyphenols of plant origin among which flavones, flavanones, isoflavones, coumarins, chalcones, lignans and stilbenes are the best representatives. By interacting with specific residues of the estradiol-binding pocket of estrogen receptors (ERs), they induce estrogenic responses, supporting the concept that they could be of benefits against the menopausal ... Read more >>

Maturitas (Maturitas)
[2011, 68(1):56-64]

Cited: 11 times

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Capacity of type I and II ligands to confer to estrogen receptor alpha an appropriate conformation for the recruitment of coactivators containing a LxxLL motif-Relationship with the regulation of receptor level and ERE-dependent transcription in MCF-7 cells.

Sandrine Bourgoin-Voillard, Dominique Gallo, Ioanna Laïos, Anny Cleeren, Latifa El Bali, Yves Jacquot, Denis Nonclercq, Guy Laurent, Jean-Claude Tabet, Guy Leclercq,

Estrogen receptor alpha (ERalpha) belongs to the superfamily of nuclear receptors and as such acts as a ligand-modulated transcription factor. Ligands elicit in ERalpha conformational changes leading to the recruitment of coactivators required for the transactivation of target genes via cognate response elements. In many cells, activated ERalpha also undergoes ... Read more >>

Biochem. Pharmacol. (Biochemical pharmacology)
[2010, 79(5):746-757]

Cited: 13 times

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Controversies concerning the use of phytoestrogens in menopause management: bioavailability and metabolism.

Patricia de Cremoux, Pascale This, Guy Leclercq, Yves Jacquot,

It has been proposed that the use of phytoestrogens (PE) in menopausal therapy could be beneficial to woman health, particularly with respect to hot flushes. Indeed, PE may compensate the lack of endogenous 17beta-estradiol occurring during menopause. However, therapeutic benefits remain questionable, as highlighted by recent publications. Indeed, data are ... Read more >>

Maturitas (Maturitas)
[2010, 65(4):334-339]

Cited: 18 times

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