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Akademický článek

C286, an orally available retinoic acid receptor β agonist drug, regulates multiple pathways to achieve spinal cord injury repair

Autor: Maria B. Goncalves, Yue Wu, Earl Clarke, John Grist, Julien Moehlin, Marco Antonio Mendoza-Parra, Carl Hobbs, Barret Kalindjian, Henry Fok, Adrian P. Mander, Hana Hassanin, Daryl Bendel, Jörg Täubel, Tim Mant, Thomas Carlstedt, Julian Jack, Jonathan P. T. Corcoran

Publikováno v: Frontiers in Molecular Neuroscience, Vol 17 (2024)

Retinoic acid receptor β2 (RARβ2) is an emerging therapeutic target for spinal cord injuries (SCIs) with a unique multimodal regenerative effect. We have developed a first-in-class RARβ agonist drug, C286, that modulates neuron-glial pathways to i

Externí odkaz: https://doaj.org/article/fc6f78e235584c4a814b98223f1ff1d8

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Akademický článek

RARβ Agonist Drug (C286) Demonstrates Efficacy in a Pre-clinical Neuropathic Pain Model Restoring Multiple Pathways via DNA Repair Mechanisms

Autor: Maria B. Goncalves, Julien Moehlin, Earl Clarke, John Grist, Carl Hobbs, Antony M. Carr, Julian Jack, Marco Antonio Mendoza-Parra, Jonathan P.T. Corcoran

Publikováno v: iScience, Vol 20, Iss , Pp 554-566 (2019)

Summary: Neuropathic pain (NP) is associated with profound gene expression alterations within the nociceptive system. DNA mechanisms, such as epigenetic remodeling and repair pathways have been implicated in NP. Here we have used a rat model of perip

Externí odkaz: https://doaj.org/article/8551eb581aa8412dbb09b8e31da54c5a

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Akademický článek

Retinoic acid synthesis by NG2 expressing cells promotes a permissive environment for axonal outgrowth

Autor: Maria B. Goncalves, Yue Wu, Diogo Trigo, Earl Clarke, Tony Malmqvist, John Grist, Carl Hobbs, Thomas P. Carlstedt, Jonathan P.T. Corcoran

Publikováno v: Neurobiology of Disease, Vol 111, Iss , Pp 70-79 (2018)

Stimulation of retinoic acid (RA) mediated signalling pathways following neural injury leads to regeneration in the adult nervous system and numerous studies have shown that the specific activation of the retinoic acid receptor β (RARβ) is required

Externí odkaz: https://doaj.org/article/8c968baf906f42549a15f27578a639b1

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RARβ agonist drug (C286) demonstrates efficacy in a pre-clinical neuropathic pain model restoring multiple pathways via DNA repair mechanisms

Autor: Antony M. Carr, Carl Hobbs, Jonathan Corcoran, Julian Jack, Maria B. Goncalves, Julien Moehlin, John Grist, Earl Clarke, Marco Antonio Mendoza-Parra

Publikováno v: Goncalves, M B, Moehlin, J, Clarke, E, Grist, J, Hobbs, C, Carr, A M, Jack, J, Mendoza-Parra, M A & Corcoran, J P T 2019, ' RARβ agonist drug (C286) demonstrates efficacy in a pre-clinical neuropathic pain model restoring multiple pathways via DNA repair mechanisms ', iScience, vol. 20, pp. 554-566 . https://doi.org/10.1016/j.isci.2019.09.020
iScience
iScience, Elsevier, 2019, 20, pp.554-566. ⟨10.1016/j.isci.2019.09.020⟩
iScience, 2019, 20, pp.554-566. ⟨10.1016/j.isci.2019.09.020⟩
iScience, Vol 20, Iss, Pp 554-566 (2019)

Summary Neuropathic pain (NP) is associated with profound gene expression alterations within the nociceptive system. DNA mechanisms, such as epigenetic remodeling and repair pathways have been implicated in NP. Here we have used a rat model of periph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83ec446be6531d3c4f27cfa5676ad5e9
https://kclpure.kcl.ac.uk/ws/files/124208802/RAR_agonist_drug_C286_demonstrates_GONCALVES_Accepted12September2019_Published25October2019_GOLD_VoR_CC_BY_.pdf

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Corrigendum to 'Discovery and lead optimisation of a potent, selective and orally bioavailable RARβ agonist for the potential treatment of nerve injury' [Bioorg. Med. Chem. Lett. 29(8) (2019) 995–1000]

Autor: Carl Hobbs, S. Barret Kalindjian, John Grist, Thomas Carlstedt, Jonathan Corcoran, Maria B. Goncalves, Peter Mumford, Christopher I. Jarvis, Earl Clarke, Mark Trevor Mills, Jane Theresa Brown, Alan D. Borthwick, Julian Jack, Thomas Pitcher

Publikováno v: Bioorganic & Medicinal Chemistry Letters

Oxadiazole replacement of an amide linkage in an RARα agonist template 1, followed by lead optimisation, has produced a highly potent and selective RARβ agonist 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (10) with good ora

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cac033e762913965dd8ab36d045c10c
https://doi.org/10.1016/j.bmcl.2019.05.058

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Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist

Autor: Earl, Clarke, Christopher I, Jarvis, Maria B, Goncalves, S Barret, Kalindjian, David R, Adams, Jane T, Brown, Jason J, Shiers, David M A, Taddei, Elodie, Ravier, Stephanie, Barlow, Iain, Miller, Vanessa, Smith, Alan D, Borthwick, Jonathan P T, Corcoran

Publikováno v: Bioorganic & Medicinal Chemistry

Graphical abstract
A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::a651db96aeac6253440f0f177d2dd404
https://pubmed.ncbi.nlm.nih.gov/29288071

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Retinoic acid receptor‐α signalling antagonizes both intracellular and extracellular amyloid‐β production and prevents neuronal cell death caused by amyloid‐β

Autor: Malcolm Maden, Maria B. Goncalves, M. Dogruel, S. B. Kalindjian, Earl Clarke, Sarah A. Thomas, Christopher I. Jarvis, Jonathan Corcoran

Publikováno v: European Journal of Neuroscience. 32:1246-1255

Alzheimer's disease (AD) is characterized by amyloid-β (Aβ) deposition in the brain, neuronal cell loss and cognitive decline. We show here that retinoic acid receptor (RAR)α signalling in vitro can prevent both intracellular and extracellular Aβ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::843ea2cbc8006b3d675401799ef83b52
https://doi.org/10.1111/j.1460-9568.2010.07426.x

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Neuronal RARβ Signaling Modulates PTEN Activity Directly in Neurons and via Exosome Transfer in Astrocytes to Prevent Glial Scar Formation and Induce Spinal Cord Regeneration

Autor: Maria B, Goncalves, Tony, Malmqvist, Earl, Clarke, Chantal J, Hubens, John, Grist, Carl, Hobbs, Diogo, Trigo, Mårten, Risling, Maria, Angeria, Peter, Damberg, Thomas P, Carlstedt, Jonathan P T, Corcoran

Publikováno v: The Journal of neuroscience : the official journal of the Society for Neuroscience. 35(47)

Failure of axonal regeneration in the central nervous system (CNS) is mainly attributed to a lack of intrinsic neuronal growth programs and an inhibitory environment from a glial scar. Phosphatase and tensin homolog (PTEN) is a major negative regulat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ddf81e7a78f766e04dff1481cfc2d225
https://pubmed.ncbi.nlm.nih.gov/26609164

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Amyloid β inhibits retinoic acid synthesis exacerbating Alzheimer disease pathology which can be attenuated by an retinoic acid receptor α agonist

Autor: Maria B. Goncalves, Robert M. J. Deacon, Carl Hobbs, Jonathan Corcoran, Earl Clarke, Julian Jack, Tony Malmqvist

Publikováno v: The European Journal of Neuroscience

The retinoic acid receptor (RAR) α system plays a key role in the adult brain, participating in the homeostatic control of synaptic plasticity, essential for memory function. Here we show that RARα signalling is down-regulated by amyloid beta (Aβ)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b0b9e2e9df9a37deda69773b527c480
https://pubmed.ncbi.nlm.nih.gov/23379615

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