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Page 1
Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.
Imbriglio JE, Shen DM, Liang R, Marby K, You M, Youm HW, Feng Z, London C, Xiong Y, Tata J, Verras A, Garcia-Calvo M, Song X, Addona GH, McLaren DG, He T, Murphy B, Metzger DE, Salituro G, Deckman D, Chen Q, Jin X, Stout SJ, Wang SP, Wilsie L, Palyha O, Han S, Hubbard BK, Previs SF, Pinto S, Taggart A. Imbriglio JE, et al. Among authors: chen q. J Med Chem. 2015 Dec 10;58(23):9345-53. doi: 10.1021/acs.jmedchem.5b01345. Epub 2015 Nov 20. J Med Chem. 2015. PMID: 26561979
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
Wu Z, Yang C, Xiong Y, Feng Z, Lombardo M, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen Q, Sinharoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL. Wu Z, et al. Among authors: chen q. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1774-8. doi: 10.1016/j.bmcl.2011.12.064. Epub 2011 Dec 24. Bioorg Med Chem Lett. 2012. PMID: 22248857
Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors.
Graham TH, Shu M, Verras A, Chen Q, Garcia-Calvo M, Li X, Lisnock J, Tong X, Tung EC, Wiltsie J, Hale JJ, Pinto S, Shen DM. Graham TH, et al. Among authors: chen q. Bioorg Med Chem Lett. 2014 Apr 1;24(7):1657-60. doi: 10.1016/j.bmcl.2014.02.070. Epub 2014 Mar 6. Bioorg Med Chem Lett. 2014. PMID: 24636945
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: chen q, chen d. 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 benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.
Shen HC, Ding FX, Jiang J, Verras A, Chabin RM, Xu S, Tong X, Chen Q, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Murphy BA, Gorski JN, Wiltsie J, SinhaRoy R, Hale JJ, Pinto S, Shen DM. Shen HC, et al. Among authors: chen q. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1550-6. doi: 10.1016/j.bmcl.2012.01.002. Epub 2012 Jan 10. Bioorg Med Chem Lett. 2012. PMID: 22264488
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: chen q. 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: chen q. 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
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: chen q. 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: chen q, chen d. 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
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Hoyt SB, Park MK, London C, Xiong Y, Tata J, Bennett DJ, Cooke A, Cai J, Carswell E, Robinson J, MacLean J, Brown L, Belshaw S, Clarkson TR, Liu K, Liang GB, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Kuethe J, Rivera N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Ali A. Hoyt SB, et al. Among authors: chen q. ACS Med Chem Lett. 2015 Apr 7;6(5):573-8. doi: 10.1021/acsmedchemlett.5b00054. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005536 Free PMC article.
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