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

Accelerating GPCR Drug Discovery With Conformation-Stabilizing VHHs

Autor: Toon Laeremans, Zara A. Sands, Pieter Claes, Ann De Blieck, Stephane De Cesco, Sarah Triest, Andreas Busch, David Felix, Abhinav Kumar, Veli-Pekka Jaakola, Christel Menet

Publikováno v: Frontiers in Molecular Biosciences, Vol 9 (2022)

The human genome encodes 850 G protein-coupled receptors (GPCRs), half of which are considered potential drug targets. GPCRs transduce extracellular stimuli into a plethora of vital physiological processes. Consequently, GPCRs are an attractive drug

Externí odkaz: https://doaj.org/article/ea4599d8f7de44b08618672b548d1833

Reconstruction of apo A2A receptor activation pathways reveal ligand-competent intermediates and state-dependent cholesterol hotspots

Autor: Alberto Cuzzolin, Silvia Lovera, Gianni De Fabritiis, Sebastian Kelm, Zara A. Sands

Publikováno v: Scientific Reports, Vol 9, Iss 1, Pp 1-10 (2019)
Scientific Reports
Recercat. Dipósit de la Recerca de Catalunya
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G-protein coupled receptors (GPCRs) play a pivotal role in transmitting signals at the cellular level. Structural insights can be exploited to support GPCR structure-based drug discovery endeavours. Despite advances in GPCR crystallography, active st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17a342d45234e4b9f487e36fb1ba75fc
http://link.springer.com/article/10.1038/s41598-019-50752-6

GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containing NMDA receptors

Autor: Véronique M. André, Philippe Ghisdal, Zara A. Sands, Brice Mullier, Rafal M. Kaminski, Christian Wolff, Pierandrea Muglia

Publikováno v: Neuropharmacology. 123:322-331

De novo gain of function mutations in GRIN2B encoding the GluN2B subunit of the N-methyl-d-aspartate (NMDA) receptor have been linked with epileptic encephalopathies, including infantile spasms. We investigated the effects of radiprodil, a selective

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::311861d7ee5cb84ed532ca34ef996a46
https://doi.org/10.1016/j.neuropharm.2017.05.017

The Aminotriazole Antagonist Cmpd-1 Stabilises a Distinct Inactive State of the Adenosine 2A Receptor

Autor: Silvia Lovera, David McMillan, Joël Mercier, Zara A. Sands, Lisa Joedicke, Gianni De Fabritiis, Richard J. K. Taylor, Erik J. B. Landin, Sebastian Kelm, Matthew P. Crump, Richard B. Sessions

Publikováno v: Landin, E, Lovera, S, de Fabritiis, G, Kelm, S, Mercier, J, McMillan, D, Sessions, R, Taylor, R J, Sands, Z, Joedicke, L & Crump, M 2019, ' The Aminotriazole Antagonist Cmpd-1 Stabilises a Novel Inactive State of the Adenosine 2A Receptor ', Angewandte Chemie-International Edition, vol. 58, no. 28, pp. 9399-9403 . https://doi.org/10.1002/anie.201902852

The widely expressed G-protein coupled receptors (GPCRs) are versatile signal transducer proteins that are attractive drug targets but structurally challenging to study. GPCRs undergo a number of conformational rearrangements when transitioning from

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb00482976c0bfbf28b97abcb163890e
https://pubmed.ncbi.nlm.nih.gov/31095849