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Page 1
A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.
Graham TH, Liu W, Verras A, Reibarkh M, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xie D, Xu S, Xiao J, Hale JJ, Pinto S, Shen DM. Graham TH, et al. Among authors: bleasby k. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2818-22. doi: 10.1016/j.bmcl.2012.02.077. Epub 2012 Mar 1. Bioorg Med Chem Lett. 2012. PMID: 22444685
The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.
Graham TH, Shen HC, Liu W, Xiong Y, Verras A, Bleasby K, Bhatt UR, Chabin RM, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Lassman ME, Shen Z, Tong X, Tung EC, Xie D, Xu S, Colletti SL, Tata JR, Hale JJ, Pinto S, Shen DM. Graham TH, et al. Among authors: bleasby k. Bioorg Med Chem Lett. 2012 Jan 1;22(1):658-65. doi: 10.1016/j.bmcl.2011.10.060. Epub 2011 Oct 24. Bioorg Med Chem Lett. 2012. PMID: 22079761
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.
Wu Z, Yang C, Graham TH, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Shen Z, Chen Q, Bleasby K, Sinharoy R, Hale JJ, Tata JR, Pinto S, Colletti SL, Shen DM. Wu Z, et al. Among authors: bleasby k. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1727-30. doi: 10.1016/j.bmcl.2011.12.098. Epub 2012 Jan 8. Bioorg Med Chem Lett. 2012. PMID: 22290078
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
Graham TH, Liu W, Verras A, Sebhat IK, Xiong Y, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xiao J, Xie D, Xu S, Hale JJ, Pinto S, Shen DM. Graham TH, et al. Among authors: bleasby k. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2811-7. doi: 10.1016/j.bmcl.2012.02.075. Epub 2012 Mar 1. Bioorg Med Chem Lett. 2012. PMID: 22444683
Nicotinic acids: liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy.
Powell DA, Black WC, Bleasby K, Chan CC, Deschenes D, Gagnon M, Gordon R, Guay J, Guiral S, Hafey MJ, Huang Z, Isabel E, Leblanc Y, Styhler A, Xu LJ, Zhang L, Oballa RM. Powell DA, et al. Among authors: bleasby k. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7281-6. doi: 10.1016/j.bmcl.2011.10.040. Epub 2011 Oct 18. Bioorg Med Chem Lett. 2011. PMID: 22047692
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, Guiral S, Hafey MJ, Hamelin E, Huang Z, Kennedy B, Lachance N, Landry F, Li CS, Mancini J, Normandin D, Pocai A, Powell DA, Ramtohul YK, Skorey K, Sørensen D, Sturkenboom W, Styhler A, Waddleton DM, Wang H, Wong S, Xu L, Zhang L. Oballa RM, et al. Among authors: bleasby k. J Med Chem. 2011 Jul 28;54(14):5082-96. doi: 10.1021/jm200319u. Epub 2011 Jun 28. J Med Chem. 2011. PMID: 21661758
Impact of passive permeability and gut efflux transport on the oral bioavailability of novel series of piperidine-based renin inhibitors in rodents.
Lévesque JF, Bleasby K, Chefson A, Chen A, Dubé D, Ducharme Y, Fournier PA, Gagné S, Gallant M, Grimm E, Hafey M, Han Y, Houle R, Lacombe P, Laliberté S, MacDonald D, Mackay B, Papp R, Tschirret-Guth R. Lévesque JF, et al. Among authors: bleasby k. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5547-51. doi: 10.1016/j.bmcl.2011.06.095. Epub 2011 Jun 28. Bioorg Med Chem Lett. 2011. PMID: 21784634
25 results