Výsledky vyhledávání - "Florence Lebon"

Akademický článek

Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist

Autor: Bingfa Sun, Dan Feng, Matthew Ling-Hon Chu, Inbar Fish, Silvia Lovera, Zara A. Sands, Sebastian Kelm, Anne Valade, Martyn Wood, Tom Ceska, Tong Sun Kobilka, Florence Lebon, Brian K. Kobilka

Publikováno v: Nature Communications, Vol 12, Iss 1, Pp 1-9 (2021)

Recently, a class of non-catechol Dopamine D1 receptor (D1R) selective agonists with novel scaffold and improved pharmacological properties were reported. Here, authors report the crystal structure of D1R in complex with stimulatory G protein (Gs) an

Externí odkaz: https://doaj.org/article/2dbb4259799647b08364c62567b2949b

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Akademický článek

The potential for opportunistic identification of vertebral fractures in patients undergoing a CT scan as part of daily clinical practice: Descriptive study using registry data

Autor: Michael Kriegbaum Skjødt, Joeri Nicolaes, Christopher Dyer Smith, Jonas Banefelt, Florence Lebon, Cesar Libanati, Kim Rose Olsen, Cyrus Cooper, Bo Abrahamsen

Publikováno v: Bone Reports, Vol 13, Iss , Pp 100555- (2020)

Externí odkaz: https://doaj.org/article/ae48fe2a848c49a396dccedb0e47d6a9

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Akademický článek

Exploring the interaction of SV2A with racetams using homology modelling, molecular dynamics and site-directed mutagenesis.

Autor: Joanna Lee, Veronique Daniels, Zara A Sands, Florence Lebon, Jiye Shi, Philip C Biggin

Publikováno v: PLoS ONE, Vol 10, Iss 2, p e0116589 (2015)

The putative Major Facilitator Superfamily (MFS) transporter, SV2A, is the target for levetiracetam (LEV), which is a successful anti-epileptic drug. Furthermore, SV2A knock out mice display a severe seizure phenotype and die after a few weeks. Despi

Externí odkaz: https://doaj.org/article/ae42f1295e90453ba5296467551df3bc

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Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist

Autor: Sebastian Kelm, Bingfa Sun, Inbar Fish, Matthew Ling-Hon Chu, Florence Lebon, Zara A. Sands, Martyn Wood, Dan Feng, Tong Sun Kobilka, Brian K. Kobilka, Silvia Lovera, Tom Ceska, Anne Valade

Publikováno v: Nature Communications
Nature Communications, Vol 12, Iss 1, Pp 1-9 (2021)

Dopamine D1 receptor (D1R) is an important drug target implicated in many psychiatric and neurological disorders. Selective agonism of D1R are sought to be the therapeutic strategy for these disorders. Most selective D1R agonists share a dopamine-lik

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b9b0b7a549f0537d2457a0993a82997
http://europepmc.org/articles/PMC8175458

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Crystal structure of the adenosine A 2A receptor bound to an antagonist reveals a potential allosteric pocket

Autor: Zara A. Sands, Florence Lebon, Matthew Ling-Hon Chu, Tong Sun Kobilka, Joël Mercier, Priti Bachhawat, Tom Ceska, Brian K. Kobilka, Martyn Wood, Bingfa Sun

Publikováno v: Proceedings of the National Academy of Sciences. 114:2066-2071

The adenosine A2A receptor (A2AR) has long been implicated in cardiovascular disorders. As more selective A2AR ligands are being identified, its roles in other disorders, such as Parkinson’s disease, are starting to emerge, and A2AR antagonists are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e5111950850a954b0b1feb0b2564e766
https://doi.org/10.1073/pnas.1621423114

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The potential for opportunistic identification of vertebral fractures in patients undergoing a CT scan as part of daily clinical practice: Descriptive study using registry data

Autor: Joeri Nicolaes, Jonas Banefelt, Bo Abrahamsen, Christopher D. Smith, Florence Lebon, Cesar Libanati, Michael K Skjødt, Kim Rose Olsen, Cyrus Cooper

Publikováno v: Bone Reports, Vol 13, Iss, Pp 100555-(2020)
Skjødt, M K, Nicolaes, J, Smith, C D, Banefelt, J, Lebon, F, Libanati, C, Olsen, K R, Cooper, C & Abrahamsen, B 2020, ' The potential for opportunistic identification of vertebral fractures in patients undergoing a CT scan as part of daily clinical practice : Descriptive study using registry data ', Bone Reports, vol. 13, no. Suppl., P257 . https://doi.org/10.1016/j.bonr.2020.100555

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e2fd654156f5f3f9b0fe5405fc37782
https://doi.org/10.1016/j.bonr.2020.100555

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Crystal structure of the adenosine A

Autor: Bingfa, Sun, Priti, Bachhawat, Matthew Ling-Hon, Chu, Martyn, Wood, Tom, Ceska, Zara A, Sands, Joel, Mercier, Florence, Lebon, Tong Sun, Kobilka, Brian K, Kobilka

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America. 114(8)

The A2AR is a G protein-coupled receptor (GPCR) that plays important roles in cardiovascular physiology and immune function. The A2AR is also a target for the treatment of Parkinson’s disease, where A2AR antagonists have been shown to enhance signa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2c85aad0b6af316eccea2c03ae6b2fed
https://pubmed.ncbi.nlm.nih.gov/28167788

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Towards a KCC2 blocker pharmacophore model

Autor: Ledecq Marie, Stéphane Meunier, Benoit Mathieu, Laurent Provins, Christian Wolff, Sébastien Lengelé, Alain Wagner, Anne Frycia, Florence Lebon, Nathalie Bosman, Cecile Pegurier, Kashinath Dhurke, Ananda Kumar Kanduluru

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:3978-3982

A multi-disciplinary approach was used to identify the first pharmacophore model for KCC2 blockers: several physico-chemical studies such as XRD and NMR were combined to molecular modelling techniques, SAR analysis and synthesis of constrained analog

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96363e3acf4c347756f357134ed0d1f8
https://doi.org/10.1016/j.bmcl.2012.04.097

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Discovery of a New Class of Non-imidazole Oxazoline-Based Histamine H3Receptor (H3R) Inverse Agonists

Publikováno v: ChemMedChem, 4(7), 1063-8. John Wiley and Sons Ltd
Celanire, S, Wijtmans, M, Christophe, B, Collart, P, de Esch, I J P, Dassesse, D, Delaunoy, C, Denonne, F, Durieu, V, Gelens, E, Gillard, M, Lallemand, B, Lamberty, Y, Lebon, F, Nicolas, J M, Quere, L, Snip, E, Vanbellinghen, A, Van Houtvin, N, Verbois, V, Timmerman, H, Talaga, P, Leurs, R & Provins, L 2009, ' Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists ', ChemMedChem, vol. 4, no. 7, pp. 1063-8 . https://doi.org/10.1002/cmdc.200900055

H(3)R inverse agonists based on an aminopropoxy-phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse model of recognition memory.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::543d6a72ee98e4081c29c96d0b654379
https://doi.org/10.1002/cmdc.200900055

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4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists

Autor: Bernard Christophe, Philippe P. Collart, Bastiaan J. Venhuis, Maikel Wijtmans, Saskia Hulscher, Benedicte Lallemand, Edith Gelens, Patrice Talaga, Iwan J. P. de Esch, Michel Gillard, Erwin Snip, Sylvain Celanire, Henk Timmerman, Rob Leurs, Henk van der Goot, Florence Lebon, Remko A. Bakker

Publikováno v: Wijtmans, M, Celanire, S, Snip, E, Gillard, M R, Gelens, E, Collart, P P, Venhuis, B J, Christophe, B, Hulscher, ST, van der Goot, H, Lebon, F, Timmerman, H, Bakker, R A, Leurs, R, Lallemand, B I, Talaga, P & de Esch, I J P 2008, ' 4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists ', Journal of Medicinal Chemistry, vol. 51, no. 10, pp. 2944-53 . https://doi.org/10.1021/jm7014149
Journal of Medicinal Chemistry, 51(10), 2944-53. American Chemical Society

Research on the therapeutic applications of the histamine H3 receptor (H3R) has traditionally focused on antagonists/inverse agonists. In contrast, H3R agonists have received less attention despite their potential use in several disease areas. The lo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07dd14a93395558ca6f0ff4ef04ac36c
https://research.vu.nl/en/publications/47ca4fc4-ef36-48d9-b4ba-e809e2b8d47c

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