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Number of items: 47.

Baldwin, Alex

, Foley, David, Collins, Ross, Lee, Hyunah, Jones, D. Heulyn, Wahab, Ben, Waters, Loren, Pedder, Josephine, Paine, Marie, Feng, Gui, Privitera, Lucia, Ashall-Kelly, Alexander, Thomas, Carys, Gillespie, Jason, Schino, Lauramariu, Belelli, Delia, Rocha, Cecilia, Maussion, Gilles, Krahn, Andrea, Durcan, Thomas, Elkins, Jonathan, Lambert, Jeremy, Atack, John

and Ward, Simon

2025. Discovery of MDI-114215: A potent and selective LIMK inhibitor to treat Fragile X Syndrome. Journal of Medicinal Chemistry 68 (1) , pp. 719-752. 10.1021/acs.jmedchem.4c02694

Baldwin, Alex G.

, Foley, David W.

, Collins, Ross, Lee, Hyunah, Jones, D. Heulyn, Wahab, Ben, Waters, Loren, Pedder, Josephine, Paine, Marie, Feng, Gui Jie, Privitera, Lucia, Ashall-Kelly, Alexander, Thomas, Carys, Gillespie, Jason A., Schino, Lauramariú, Belelli, Delia, Rocha, Cecilia, Maussion, Gilles, Krahn, Andrea I., Durcan, Thomas M., Elkins, Jonathan M., Lambert, Jeremy J., Atack, John R.

and Ward, Simon E.

2025. Discovery of MDI-114215: A potent and selective LIMK inhibitor to treat fragile X syndrome. Journal of Medicinal Chemistry 68 (1) , pp. 719-752. 10.1021/acs.jmedchem.4c02694

Mitchell, Scott J., Phillips, Grant D., Tench, Becks, Li, Yunkai, Belelli, Delia, Martin, Stephen J., Swinny, Jerome D., Kelly, Louise, Atack, John R.

, Paradowski, Michael and Lambert, Jeremy J. 2024. Neurosteroid modulation of synaptic and extrasynaptic GABAA receptors of the mouse nucleus accumbens. Biomolecules 14 (4) , 460. 10.3390/biom14040460

An, Haiyan, Elvers, Karen T., Gillespie, Jason A., Jones, Kimberley, Atack, John R.

, Grubisha, Olivera

and Shelkovnikova, Tatyana A.

2022. A toolkit for the identification of NEAT1_2/paraspeckle modulators. Nucleic Acids Research 50 (20) , e119. 10.1093/nar/gkac771

University College Cardiff Consultants Limited 2022. Heteroaryl compounds useful in the treatment of cognitive disorders. WO2022/234271. [Patent].

Collins, Ross, Lee, Hyunah, Jones, Dyfyr, Elkins, Jonathan M., Gillespie, Jason A., Thomas, Carys, Baldwin, Alex G.

, Jones, Kimberley, Waters, Loren, Paine, Marie, Atack, John R.

, Ward, Simon E.

, Grubisha, Olivera

and Foley, David W.

2022. Comparative analysis of small-molecule limk1/2 inhibitors: chemical synthesis, biochemistry, and cellular activity. Journal of Medicinal Chemistry 10.1021/acs.jmedchem.2c00751

Noble, James W. and Atack, John R.

2022. Exploring Calbindin-IMPase fusion proteins structure and activity. Biochemistry and Biophysics Reports 30 , 101266. 10.1016/j.bbrep.2022.101266

Gendron, Thibault, Destro, Gianluca, Straathof, Natan J. W, Sap, Jeroen B. I, Guibbal, Florian, Vriamont, Charles, Caygill, Claire, Atack, John

, Watkins, Andrew, Marshall, Christopher

, Hueting, Rebekka, Warnier, Corentin, Gouverneur, Veronique and Tredwell, Matthew

2022. Multi‐patient dose synthesis of [18F] Flumazenil via a copper‐mediated 18F‐fluorination. EJNMMI Radiopharmacy and Chemistry 7 , 5. 10.1186/s41181-022-00158-z

Manzo, Marc A., Wang, Dian-Shi, Li, Winston W., Pinguelo, Arsène, Popa, Mariana O., Khodaei, Shahin, Atack, John R.

, Ross, Ruth A. and Orser, Beverley A. 2021. Inhibition of a tonic inhibitory conductance in mouse hippocampal neurones by negative allosteric modulators of α5 subunit-containing γ-aminobutyric acid type A receptors: implications for treating cognitive deficits. British Journal of Anaesthesia 126 (3) , pp. 674-683. 10.1016/j.bja.2020.11.032

Fenn, Gareth, Waller-Evans, Helen

, Atack, John R.

and Bax, Benjamin D.

2020. Crystallization and structure of ebselen bound to cysteine 141 of human inositol monophosphatase (IMPase). Acta Crystallographica Section F: Structural Biology Communications F76 (10) , pp. 469-476. 10.1107/S2053230X20011310

Maramai, Samuele, Benchekroun, Mohamed, Ward, Simon E.

and Atack, John R.

2020. Subtype selective y-Aminobutyric acid type A receptor (GABAAR) modulators acting at the benzodiazepine binding site: An update. Journal of Medicinal Chemistry 63 (7) , pp. 3425-3446. 10.1021/acs.jmedchem.9b01312

Koulouris, Chloe R., Bax, Benjamin D.

, Atack, John R.

and Roe, S. Mark 2020. Conformational flexibility within the small domain of human serine racemase. Acta Crystallographica Section F: Structural Biology Communications 76 (2) , pp. 65-73. 10.1107/S2053230X20001193

Ward, Simon E.

, Harries, Mark H., Aldegheri, Laura, Bradford, Andrea M., Ballini, Elisa, Dawson, Lee, Lacroix, Laurent, Pardoe, Joanne, Starr, Kathryn, Weil, Annette, Waters, Kerry, Atack, John R.

and Woolley, Marie 2020. Pharmacological characterisation of MDI-222, a novel AMPA receptor positive allosteric modulator with an improved safety profile. Journal of Psychopharmacology 34 (1) , pp. 93-102. 10.1177/0269881119872198

Raulin, Ana-Caroline, Kraft, Lucas, Al-Hilaly, Youssra K., Xue, Wei-Feng, McGeehan, John E., Atack, John R.

and Serpell, Louise 2019. The molecular basis for apolipoprotein E4 as the major risk factor for late-onset Alzheimer's disease. Journal of Molecular Biology 431 (12) , pp. 2248-2265. 10.1016/j.jmb.2019.04.019

Kraft, Lucas, Serpell, Louise C and Atack, John R

2019. A biophysical approach to the identification of novel ApoE chemical probes. Biomolecules 9 (2) , 48. 10.3390/biom9020048

Noble, James W., Almalki, Rehab, Roe, S. Mark, Wagner, Armin, Duman, Ramona and Atack, John R.

2018. The X-ray structure of human calbindin-D28K: an improved model. Acta Crystallographica. Section D: Structural Biology 74 (10) , pp. 1008-1014. 10.1107/S2059798318011610

Duke, Angela N., Meng, Zhiqiang, Platt, Donna M., Atack, John R.

, Dawson, Gerard R., Reynolds, David S., Tiruveedhula, V. V. N. Phani Babu, Li, Guanguan, Stephen, Michael Rajesh, Sieghart, Werner, Cook, James M. and Rowlett, James K. 2018. Evidence that sedative effects of benzodiazepines involve unexpected GABAA receptor subtypes: Quantitative observation studies in rhesus monkeys. Journal of Pharmacology and Experimental Therapeutics 366 (1) , pp. 145-157. 10.1124/jpet.118.249250

Kraft, Lucas, Roe, S. Mark, Gill, Raj and Atack, John R.

2018. Co-crystallization of human inositol monophosphatase with the lithium mimetic L-690,330. Acta Crystallographica. Section D: Structural Biology 74 (10) , p. 973. 10.1107/S2059798318010380

West, Ryan A., O'Doherty, Oran G., Askwith, Trevor, Atack, John

, Beswick, Paul, Laverick, Jamie, Paradowski, Michael, Pennicott, Lewis E., Rao, Srinivasa P.S., Williams, Gareth and Ward, Simon

2017. African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase. European Journal of Medicinal Chemistry 141 , pp. 676-689. 10.1016/j.ejmech.2017.09.067

Khan, Raysa, Boonseng, Sarote, Kemmitt, Paul D., Felix, Robert, Coles, Simon J., Tizzard, Graham J., Williams, Gareth, Simmonds, Olivia, Harvey, Jessica-Lily, Atack, John

, Cox, Hazel and Spencer, John 2017. Combining Sanford Arylations on Benzodiazepines with the nuisance effect. Advanced Synthesis & Catalysis 359 (18) , pp. 3261-3269. 10.1002/adsc.201700626

Hornyak, Peter, Askwith, Trevor, Walker, Sarah, Komulainen, Emilia, Paradowski, Michael, Pennicott, Lewis E., Bartlett, Edward J., Brissett, Nigel C., Raoof, Ali, Watson, Mandy, Jordan, Allan M., Ogilvie, Donald J., Ward, Simon E.

, Atack, John R.

, Pearl, Laurence H., Caldecott, Keith W. and Oliver, Antony W. 2016. Mode of action of DNA-competitive small molecule inhibitors of tyrosyl DNA phosphodiesterase 2. Biochemical Journal 473 (13) , pp. 1869-1879. 10.1042/BCJ20160180

Gaekens, Tim, Guillaume, Michel, Borghys, Herman, De Zwart, Loeckie L., de Vries, Ronald, Embrechts, Roger C.A., Vermeulen, An, Megens, Anton A.H.P., Leysen, Josée E., Herdewijn, Piet, Annaert, Pieter P. and Atack, John R.

2016. Lipophilic nalmefene prodrugs to achieve a one-month sustained release. Journal of Controlled Release 232 , p. 196. 10.1016/j.jconrel.2016.04.029

Spurny, Radovan, Debaveye, Sarah, Farinha, Ana, Veys, Ken, Vos, Ann M., Gossas, Thomas, Atack, John

, Bertrand, Sonia, Bertrand, Daniel, Danielson, U. Helena, Tresadern, Gary and Ulens, Chris 2015. Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor. Proceedings of the National Academy of Sciences of the United States of America 112 (19) , E2543. 10.1073/pnas.1418289112

Atack, John R.

, Shook, Brian C., Rassnick, Stefanie, Jackson, Paul F., Rhodes, Kenneth, Drinkenburg, Wilhelmus H., Ahnaou, Abdallah, te Riele, Paula, Langlois, Xavier, Hrupka, Brian, De Haes, Patrick, Hendrickx, Herman, Aerts, Nancy, Hens, Koen, Wellens, Annemie, Vermeire, Jef and Megens, Anton A. H. P. 2014. JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease. ACS Chemical Neuroscience 5 (10) , pp. 1005-1019. 10.1021/cn5001606

Walker, Sarah, Meisenberg, Cornelia, Bibby, Rachel A., Askwith, Trevor, Williams, Gareth, Rininsland, Frauke H., Pearl, Laurence H., Oliver, Antony W., El-Khamisy, Sherif, Ward, Simon

and Atack, John R.

2014. Development of an oligonucleotide-based fluorescence assay for the identification of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors. Analytical Biochemistry 454 , pp. 17-22. 10.1016/j.ab.2014.03.004

Lavreysen, Hilde and Atack, John

2014. Receptors: Functional assays. Stolerman, Ian P. and Price, Lawrence H., eds. Encyclopedia of Psychopharmacology, Berlin and Heidelberg: Springer, (10.1007/978-3-642-27772-6_208-2)

Lavreysen, H., Langlois, X., Ahnaou, A., Drinkenburg, W., te Riele, P., Biesmans, I., Van der Linden, I., Peeters, L., Megens, A., Wintmolders, C., Cid, J. M., Trabanco, A. A., Andres, J. I., Dautzenberg, F. M., Lutjens, R., Macdonald, G. and Atack, J. R.

2013. Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782. Journal of Pharmacology and Experimental Therapeutics 346 (3) , pp. 514-527. 10.1124/jpet.113.204990

Shinday, Nina M, Sawyer, Eileen K, Fischer, Bradford D, Platt, Donna M, Licata, Stephanie C, Atack, John R

, Dawson, Gerard R, Reynolds, David S and Rowlett, James K 2013. Reinforcing effects Of compounds lacking intrinsic efficacy at α1 subunit-containing GABAA receptor subtypes in midazolam- but not cocaine-experienced Rhesus Monkeys. Neuropsychopharmacology 38 (6) , pp. 1006-1014. 10.1038/npp.2012.265

Langlois, X., Megens, A., Lavreysen, H., Atack, J.

, Cik, M., te Riele, P., Peeters, L., Wouters, R., Vermeire, J., Hendrickx, H., Macdonald, G. and De Bruyn, M. 2012. Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. Journal of Pharmacology and Experimental Therapeutics 342 (1) , pp. 91-105. 10.1124/jpet.111.190702

Mirza, Naheed R., Atack, John

and Wafford, Keith 2012. Receptor subtypes: novel targets for novel medicines. Advances in Pharmacological Sciences 2012 , 529861. 10.1155/2012/529861

Swanson, Devin M., Wong, Victoria D., Jablonowski, Jill A., Shah, Chandra, Rudolph, Dale A., Dvorak, Curt A., Seierstad, Mark, Dvorak, Lisa K., Morton, Kirsten, Nepomuceno, Diane, Atack, John R.

, Bonaventure, Pascal, Lovenberg, Timothy W. and Carruthers, Nicholas I. 2011. The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y2 receptor. Bioorganic and Medicinal Chemistry Letters 21 (18) , pp. 5552-5556. 10.1016/j.bmcl.2011.06.136

Fischer, Bradford D., Atack, John R.

, Platt, Donna M., Reynolds, David S., Dawson, Gerard R. and Rowlett, James K. 2011. Contribution of GABAA receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys. Psychopharmacology 215 (2) , pp. 311-319. 10.1007/s00213-010-2142-y

Atack, JR

, Wafford, KA, Street, LJ, Dawson, GR, Tye, S, Van Laere, K, Bormans, G, Sanabria-Bohórquez, SM, De Lepeleire, I, de Hoon, JN, Van Hecken, A, Burns, HD, McKernan, RM, Murphy, MG and Hargreaves, RJ 2011. MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. Journal of Psychopharmacology 25 (3) , pp. 314-328. 10.1177/0269881109354927

Atack, JR

, Hallett, DJ, Tye, S, Wafford, KA, Ryan, C, Sanabria-Bohórquez, SM, Eng, Wai-si, Gibson, RE, Burns, HD, Dawson, GR, Carling, RW, Street, LJ, Pike, A, De Lepeleire, I, Van Laere, K, Bormans, G, de Hoon, JN, Van Hecken, A, McKernan, RM, Murphy, MG and Hargreaves, RJ 2011. Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist. Journal of Psychopharmacology 25 (3) , pp. 329-344. 10.1177/0269881109354928

Atack, John

2011. GABAA receptor subtype-selective modulators. II. α5-selective inverse agonists for cognition enhancement. Current Topics in Medicinal Chemistry 11 (9) , pp. 1203-1214. 10.2174/156802611795371314

Atack, John

2011. GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics. Current Topics in Medicinal Chemistry 11 (9) , pp. 1176-1202. 10.2174/156802611795371350

Eng, W., Atack, J.R.

, Bergstrom, M., Sanabria, S., Appel, L., Dawson, G.R., Sciberras, D., Hargreaves, R.J., Langstrom, B. and Burns, H.D. 2010. Occupancy of human brain GABAA receptors by the novel α5 subtype-selective benzodiazepine site inverse agonist α5IA as measured using [11C]flumazenil PET imaging. Neuropharmacology 59 (7-8) , pp. 635-639. 10.1016/j.neuropharm.2010.07.024

Atack, John R.

2010. Development of subtype-selective GABAA receptor compounds for the treatment of anxiety, sleep disorders and epilepsy. Monti, James M., Pandi-Perumal, Seithikurippu Ratnas and Mohler, Hanns, eds. GABA and Sleep, Basel: Springer, pp. 25-72. (10.1007/978-3-0346-0226-6_2)

Letavic, Michael A., Aluisio, Leah, Atack, John R.

, Bonaventure, Pascal, Carruthers, Nicholas I., Dugovic, Christine, Everson, Anita, Feinstein, Mark A., Fraser, Ian C., Hoey, Kenway, Jiang, Xiaohui, Keith, John M., Koudriakova, Tatiana, Leung, Perry, Lord, Brian, Lovenberg, Timothy W., Ly, Kiev S., Morton, Kirsten L., Timothy Motley, S., Nepomuceno, Diane, Rizzolio, Michele, Rynberg, Raymond, Sepassi, Kia and Shelton, Jonathan 2010. Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: Identification of candidates for clinical development. Bioorganic and Medicinal Chemistry Letters 20 (14) , pp. 4210-4214. 10.1016/j.bmcl.2010.05.041

Stocking, Emily M., Aluisio, Leah, Atack, John R.

, Bonaventure, Pascal, Carruthers, Nicholas I., Dugovic, Christine, Everson, Anita, Fraser, Ian, Jiang, Xiaohui, Leung, Perry, Lord, Brian, Ly, Kiev S., Morton, Kirsten L., Nepomuceno, Diane, Shah, Chandravadan R., Shelton, Jonathan, Soyode-Johnson, Akinola and Letavic, Michael A. 2010. Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists. Bioorganic and Medicinal Chemistry Letters 20 (9) , pp. 2755-2760. 10.1016/j.bmcl.2010.03.071

Dixon, C. I., Morris, H. V., Breen, G., Desrivieres, S., Jugurnauth, S., Steiner, R. C., Vallada, H., Guindalini, C., Laranjeira, R., Messas, G., Rosahl, T. W., Atack, J. R.

, Peden, D. R., Belelli, D., Lambert, J. J., King, S. L., Schumann, G. and Stephens, D. N. 2010. Cocaine effects on mouse incentive-learning and human addiction are linked to α2 subunit-containing GABAA receptors. Proceedings of the National Academy of Sciences 107 (5) , pp. 2289-2294. 10.1073/pnas.0910117107

Licata, Stephanie C., Platt, Donna M., Rüedi-Bettschen, Daniela, Atack, John R.

, Dawson, Gerard R., Van Linn, Michael L., Cook, James M. and Rowlett, James K. 2010. Discriminative stimulus effects of L-838,417 (7-tert-butyl-3-(2,5-difluoro-phenyl)-6-(2-methyl-2H-[1,2,4]triazol-3-ylmethoxy)-[1,2,4]triazolo[4,3-b]pyridazine): Role of GABAA receptor subtypes. Neuropharmacology 58 (2) , pp. 357-364. 10.1016/j.neuropharm.2009.10.004

Shoblock, James R., Welty, Natalie, Nepomuceno, Diane, Lord, Brian, Aluisio, Leah, Fraser, Ian, Motley, S. Timothy, Sutton, Steve W., Morton, Kirsten, Galici, Ruggero, Atack, John R.

, Dvorak, Lisa, Swanson, Devin M., Carruthers, Nicholas I., Dvorak, Curt, Lovenberg, Timothy W. and Bonaventure, Pascal 2010. In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y Y2 receptor. Psychopharmacology 208 (2) , pp. 265-277. 10.1007/s00213-009-1726-x

Atack, J. R.

, Wong, D. F., Fryer, T. D., Ryan, C., Sanabria, S., Zhou, Y., Dannals, R. F., Eng, W.-s., Gibson, R. E., Burns, H. D., Vega, J. M., Vessy, L., Scott-Stevens, P., Beech, J. S., Baron, J.-C., Sohal, B., Schrag, M. L., Aigbirhio, F. I., McKernan, R. M. and Hargreaves, R. J. 2010. Benzodiazepine binding site occupancy by the Novel GABAA receptor subtype-selective drug 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans. Journal of Pharmacology and Experimental Therapeutics 332 (1) , pp. 17-25. 10.1124/jpet.109.157909

Atack, John R.

2010. Preclinical and clinical pharmacology of the GABAA receptor α5 subtype-selective inverse agonist α5IA. Pharmacology and Therapeutics 125 (1) , pp. 11-26. 10.1016/j.pharmthera.2009.09.001

Ator, N. A., Atack, J. R.

, Hargreaves, R. J., Burns, H. D. and Dawson, G. R. 2010. Reducing abuse liability of GABAA/Benzodiazepine ligands via selective partial agonist efficacy at α1 and α2/3 subtypes. Journal of Pharmacology and Experimental Therapeutics 332 (1) , pp. 4-16. 10.1124/jpet.109.158303

Atack, John R.

2009. GABAA receptor α2/α3 subtype-selective modulators as potential nonsedating anxiolytics. Current Topics in Behavioral Neuroscience 2 , pp. 331-360. 10.1007/7854_2009_30

This list was generated on Thu Feb 20 06:39:19 2025 GMT.