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The small molecule CLP257 does not modify activity of the K+-Cl- co-transporter KCC2 but does potentiate GABAA receptor activity.
Cardarelli RA, Jones K, Pisella LI, Wobst HJ, McWilliams LJ, Sharpe PM, Burnham MP, Baker DJ, Chudotvorova I, Guyot J, Silayeva L, Morrow DH, Dekker N, Zicha S, Davies PA, Holenz J, Duggan ME, Dunlop J, Mather RJ, Wang Q, Medina I, Brandon NJ, Deeb TZ, Moss SJ. Cardarelli RA, et al. Among authors: holenz j. Nat Med. 2017 Dec 7;23(12):1394-1396. doi: 10.1038/nm.4442. Nat Med. 2017. PMID: 29216042 Free PMC article. No abstract available.
Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity.
Johansson P, Kaspersson K, Gurrell IK, Bäck E, Eketjäll S, Scott CW, Cebers G, Thorne P, McKenzie MJ, Beaton H, Davey P, Kolmodin K, Holenz J, Duggan ME, Budd Haeberlein S, Bürli RW. Johansson P, et al. Among authors: holenz j. J Med Chem. 2018 Apr 26;61(8):3491-3502. doi: 10.1021/acs.jmedchem.7b01716. Epub 2018 Apr 10. J Med Chem. 2018. PMID: 29617572
Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides.
Swahn BM, Kolmodin K, Karlström S, von Berg S, Söderman P, Holenz J, Berg S, Lindström J, Sundström M, Turek D, Kihlström J, Slivo C, Andersson L, Pyring D, Rotticci D, Ohberg L, Kers A, Bogar K, von Kieseritzky F, Bergh M, Olsson LL, Janson J, Eketjäll S, Georgievska B, Jeppsson F, Fälting J. Swahn BM, et al. Among authors: holenz j. J Med Chem. 2012 Nov 8;55(21):9346-61. doi: 10.1021/jm3009025. Epub 2012 Sep 17. J Med Chem. 2012. PMID: 22924815
Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy.
Swahn BM, Holenz J, Kihlström J, Kolmodin K, Lindström J, Plobeck N, Rotticci D, Sehgelmeble F, Sundström M, Berg Sv, Fälting J, Georgievska B, Gustavsson S, Neelissen J, Ek M, Olsson LL, Berg S. Swahn BM, et al. Among authors: holenz j. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1854-9. doi: 10.1016/j.bmcl.2012.01.079. Epub 2012 Jan 28. Bioorg Med Chem Lett. 2012. PMID: 22325942
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Díaz JL, Cuberes R, Berrocal J, Contijoch M, Christmann U, Fernández A, Port A, Holenz J, Buschmann H, Laggner C, Serafini MT, Burgueño J, Zamanillo D, Merlos M, Vela JM, Almansa C. Díaz JL, et al. Among authors: holenz j. J Med Chem. 2012 Oct 11;55(19):8211-24. doi: 10.1021/jm3007323. Epub 2012 Jul 27. J Med Chem. 2012. PMID: 22784008
Sulfonimidamides as sulfonamides bioisosteres: rational evaluation through synthetic, in vitro, and in vivo studies with γ-secretase inhibitors.
Sehgelmeble F, Janson J, Ray C, Rosqvist S, Gustavsson S, Nilsson LI, Minidis A, Holenz J, Rotticci D, Lundkvist J, Arvidsson PI. Sehgelmeble F, et al. Among authors: holenz j. ChemMedChem. 2012 Mar 5;7(3):396-9. doi: 10.1002/cmdc.201200014. Epub 2012 Feb 3. ChemMedChem. 2012. PMID: 22307979 No abstract available.
43 results