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Page 1
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. 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
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. 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: graham th. 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 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. 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
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Debenham JS, Graham TH, Verras A, Zhang Y, Clements MJ, Kuethe JT, Madsen-Duggan C, Liu W, Bhatt UR, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Li X, Lisnock J, Shen Z, Tong X, Tung EC, Wiltsie J, Xu S, Hale JJ, Pinto S, Shen DM. Debenham JS, et al. Among authors: graham th. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6228-33. doi: 10.1016/j.bmcl.2013.09.094. Epub 2013 Oct 8. Bioorg Med Chem Lett. 2013. PMID: 24157366
DGAT2 Inhibition Alters Aspects of Triglyceride Metabolism in Rodents but Not in Non-human Primates.
McLaren DG, Han S, Murphy BA, Wilsie L, Stout SJ, Zhou H, Roddy TP, Gorski JN, Metzger DE, Shin MK, Reilly DF, Zhou HH, Tadin-Strapps M, Bartz SR, Cumiskey AM, Graham TH, Shen DM, Akinsanya KO, Previs SF, Imbriglio JE, Pinto S. McLaren DG, et al. Among authors: graham th. Cell Metab. 2018 Jun 5;27(6):1236-1248.e6. doi: 10.1016/j.cmet.2018.04.004. Epub 2018 Apr 26. Cell Metab. 2018. PMID: 29706567 Free article.
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease.
Candito DA, Simov V, Gulati A, Kattar S, Chau RW, Lapointe BT, Methot JL, DeMong DE, Graham TH, Kurukulasuriya R, Keylor MH, Tong L, Morriello GJ, Acton JJ, Pio B, Liu W, Scott JD, Ardolino MJ, Martinot TA, Maddess ML, Yan X, Gunaydin H, Palte RL, McMinn SE, Nogle L, Yu H, Minnihan EC, Lesburg CA, Liu P, Su J, Hegde LG, Moy LY, Woodhouse JD, Faltus R, Xiong T, Ciaccio P, Piesvaux JA, Otte KM, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Neelamkavil S, Wood HB, Fuller PH, Ellis JM. Candito DA, et al. Among authors: graham th. J Med Chem. 2022 Dec 22;65(24):16801-16817. doi: 10.1021/acs.jmedchem.2c01605. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475697
23 results