GHB analogs confer neuroprotection through specific interaction with the CaMKII alpha hub domain

Autor: Geeske M. van Woerden, Christian D. Kelstrup, Emma K. Gowing, Inge S. Villumsen, Anders B. Klein, Birgitte Rahbek Kornum, Christine L. Gee, Nane Griem-Krey, Mohamed A. Shehata, Ulrike Leurs, Rasmus P. Clausen, Stine J. Gauger, Andrew N. Clarkson, Louise Hamborg, Anne Sofie G. Larsen, Chris C. Chi, Robert O. Burnie, Anders Bach, D. Steven Kerr, Jesper V. Olsen, Sara Marie Øie Solbak, Petrine Wellendorph, John Kuriyan, Ethan D McSpadden, Josh Houlton, Stine B. Vogensen, Selina M. W. Teurlings, Bente Frølund, Line B. Palmelund

Publikováno v: Leurs, U, Klein, A B, McSpadden, E D, Griem-Krey, N, Solbak, S M O, Houlton, J, Villumsen, I S, Vogensen, S B, Hamborg, L, Gauger, S J, Palmelund, L B, Larsen, A S G, Shehata, M A, Kelstrup, C D, Olsen, J V, Bach, A, Burnie, R O, Kerr, D S, Gowing, E K, Teurlings, S M W, Chi, C C, Gee, C L, Frølund, B, Kornum, B R, van Woerden, G M, Clausen, R P, Kuriyan, J, Clarkson, A N & Wellendorph, P 2021, ' GHB analogs confer neuroprotection through specific interaction with the CaMKII alpha hub domain ', Proceedings of the National Academy of Sciences of the United States of America, vol. 118, no. 31 . https://doi.org/10.1073/pnas.2108079118
Proceedings of the National Academy of Sciences of the United States of America, 118(31):e2108079118. National Academy of Sciences
Proceedings of the National Academy of Sciences of the United States of America
Proceedings of the National Academy of Sciences of the United States of America, vol 118, iss 31

Significance GHB is a natural brain metabolite of GABA, previously reported to be neuroprotective. However, the high-affinity binding site for GHB has remained elusive for almost 40 y. We here unveil CaMKIIα, a highly important neuronal kinase, as t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3968f82757f44ca335598be37cbc1e0
https://curis.ku.dk/portal/da/publications/ghb-analogs-confer-neuroprotection-through-specific-interaction-with-the-camkii-alpha-hub-domain(df178a50-331d-40f4-ae3d-8333cff82958).html

Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs

Autor: Rasmus P. Clausen, Claus H. Jensen, Sara Björk Sigurdardóttir, Kenneth T. Kongstad, David E. Gloriam, Petrine Wellendorph, Mia Nittegaard-Nielsen, Christina Birkedahl Falk-Petersen, Francesco Bavo, Yongsong Tian, Jan Kehler, Kasper Harpsøe, Jacob Krall, Stine B. Vogensen, Bente Frølund, Anne S. Haugaard

Publikováno v: Journal of Medicinal Chemistry. 60:9022-9039

γ-hydroxybutyric acid (GHB) is a neuroactive substance with specific high-affinity binding sites. To facilitate target identification and ligand optimization, we herein report a comprehensive structure-affinity relationship study for novel ligands t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::371f91bb7a8a910a778dba45c5ffc706
https://doi.org/10.1021/acs.jmedchem.7b01351

Radiosynthesis and Evaluation of [11C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites

Autor: Gitte M. Knudsen, Matthias M. Herth, Claus H. Jensen, Tina Bay, Rasmus P. Clausen, Szabolcs Lehel, Christoffer Bundgaard, Stine B. Vogensen, Bente Frølund, Petrine Wellendorph, Hanne D. Hansen, Louise Thiesen

Publikováno v: ACS Chemical Neuroscience. 8:22-27

γ-Hydroxybutyric acid (GHB) is an endogenous neuroactive substance and proposed neurotransmitter with affinity for both low- and high-affinity binding sites. A radioligand with high and specific affinity toward the high-affinity GHB binding site wou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::53cf9e1794123f459aa32efbd4bad9f7
https://doi.org/10.1021/acschemneuro.6b00335

γ-Aminobutyric Acid and Glycine Neurotransmitter Transporters

Autor: Arne Schousboe, Jonas Skovgaard-Petersen, Gerhard F. Ecker, Stine B. Vogensen, Julie Mie Jacobsen, Andreas Jurik, Povl Krogsgaard-Larsen, Rasmus P. Clausen, Petrine Wellendorph

Publikováno v: Transporters as Drug Targets

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c775aae85f2eea079c8f3fc2a2e21d8d
https://doi.org/10.1002/9783527679430.ch4

Pharmacological Identification of a Guanidine-Containing β-Alanine Analogue with Low Micromolar Potency and Selectivity for the Betaine/GABA Transporter 1 (BGT1)

Autor: Maria E. K. Lie, Petrine Wellendorph, Bente Frølund, Maria Damgaard, Stine B. Vogensen, Hans Bräuner-Osborne, Mette H. Jensen, Anas Al-Khawaja, Bolette Kragholm, Rasmus P. Clausen, Jette G. Petersen

Publikováno v: Neurochemical Research. 39:1988-1996

The γ-aminobutyric acid (GABA) transporters (GATs) are key membrane transporter proteins involved in the termination of GABAergic signaling at synapses in the mammalian brain and proposed drug targets in neurological disorders such as epilepsy. To d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::822fd1d5fdf5e9bcd4ab324c4befdeab
https://doi.org/10.1007/s11064-014-1336-9