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Page 1
Identification of a Novel Allosteric Inhibitory Site on Tryptophan Hydroxylase 1 Enabling Unprecedented Selectivity Over all Related Hydroxylases.
Petrassi M, Barber R, Be C, Beach S, Cox B, D'Souza AM, Duggan N, Hussey M, Fox R, Hunt P, Jarai G, Kosaka T, Oakley P, Patel V, Press N, Rowlands D, Scheufler C, Schmidt O, Srinivas H, Turner M, Turner R, Westwick J, Wolfreys A, Pathan N, Watson S, Thomas M. Petrassi M, et al. Among authors: kosaka t. Front Pharmacol. 2017 May 5;8:240. doi: 10.3389/fphar.2017.00240. eCollection 2017. Front Pharmacol. 2017. PMID: 28529483 Free PMC article.
Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.
Shaw D, Hollingworth G, Soldermann N, Sprague E, Schuler W, Vangrevelinghe E, Duggan N, Thomas M, Kosaka T, Waters N, van Eis MJ. Shaw D, et al. Among authors: kosaka t. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4812-7. doi: 10.1016/j.bmcl.2014.09.002. Epub 2014 Sep 6. Bioorg Med Chem Lett. 2014. PMID: 25248678
Discovery of selective and nonpeptidic cathepsin S inhibitors.
Irie O, Ehara T, Iwasaki A, Yokokawa F, Sakaki J, Hirao H, Kanazawa T, Teno N, Horiuchi M, Umemura I, Gunji H, Masuya K, Hitomi Y, Iwasaki G, Nonomura K, Tanabe K, Fukaya H, Kosaka T, Snell CR, Hallett A. Irie O, et al. Among authors: kosaka t. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3959-62. doi: 10.1016/j.bmcl.2008.06.009. Epub 2008 Jun 10. Bioorg Med Chem Lett. 2008. PMID: 18572405
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.
Irie O, Kosaka T, Ehara T, Yokokawa F, Kanazawa T, Hirao H, Iwasaki A, Sakaki J, Teno N, Hitomi Y, Iwasaki G, Fukaya H, Nonomura K, Tanabe K, Koizumi S, Uchiyama N, Bevan SJ, Malcangio M, Gentry C, Fox AJ, Yaqoob M, Culshaw AJ, Allan Hallett. Irie O, et al. Among authors: kosaka t. J Med Chem. 2008 Sep 25;51(18):5502-5. doi: 10.1021/jm800839j. J Med Chem. 2008. PMID: 18754655
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Irie O, Yokokawa F, Ehara T, Iwasaki A, Iwaki Y, Hitomi Y, Konishi K, Kishida M, Toyao A, Masuya K, Gunji H, Sakaki J, Iwasaki G, Hirao H, Kanazawa T, Tanabe K, Kosaka T, Hart TW, Hallett A. Irie O, et al. Among authors: kosaka t. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4642-6. doi: 10.1016/j.bmcl.2008.07.011. Epub 2008 Jul 10. Bioorg Med Chem Lett. 2008. PMID: 18662880
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Irie O, Kosaka T, Kishida M, Sakaki J, Masuya K, Konishi K, Yokokawa F, Ehara T, Iwasaki A, Iwaki Y, Hitomi Y, Toyao A, Gunji H, Teno N, Iwasaki G, Hirao H, Kanazawa T, Tanabe K, Hiestand PC, Malcangio M, Fox AJ, Bevan SJ, Yaqoob M, Culshaw AJ, Hart TW, Hallett A. Irie O, et al. Among authors: kosaka t. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5280-4. doi: 10.1016/j.bmcl.2008.08.067. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2008. PMID: 18783943
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK. Ostermann N, et al. Among authors: kosaka t. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Ehara T, Irie O, Kosaka T, Kanazawa T, Breitenstein W, Grosche P, Ostermann N, Suzuki M, Kawakami S, Konishi K, Hitomi Y, Toyao A, Gunji H, Cumin F, Schiering N, Wagner T, Rigel DF, Webb RL, Maibaum J, Yokokawa F. Ehara T, et al. Among authors: kosaka t. ACS Med Chem Lett. 2014 Apr 21;5(7):787-92. doi: 10.1021/ml500137b. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050166 Free PMC article.
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Lorthiois E, Breitenstein W, Cumin F, Ehrhardt C, Francotte E, Jacoby E, Ostermann N, Sellner H, Kosaka T, Webb RL, Rigel DF, Hassiepen U, Richert P, Wagner T, Maibaum J. Lorthiois E, et al. Among authors: kosaka t. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
1,282 results