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Journal Abstract Search

119 related items for PubMed ID: 22248857

  • 1. 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.
    Bioorg Med Chem Lett; 2012 Feb 15; 22(4):1774-8. PubMed ID: 22248857
    [Abstract] [Full Text] [Related]

  • 2. 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.
    Bioorg Med Chem Lett; 2012 Feb 15; 22(4):1727-30. PubMed ID: 22290078
    [Abstract] [Full Text] [Related]

  • 3. 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.
    Bioorg Med Chem Lett; 2012 Apr 15; 22(8):2811-7. PubMed ID: 22444683
    [Abstract] [Full Text] [Related]

  • 4. 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.
    Bioorg Med Chem Lett; 2012 Feb 15; 22(4):1550-6. PubMed ID: 22264488
    [Abstract] [Full Text] [Related]

  • 5. Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.
    Shen HC, Ding FX, Zhou C, Xiong Y, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen D, Sinharoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL.
    Bioorg Med Chem Lett; 2011 Mar 01; 21(5):1299-305. PubMed ID: 21315588
    [Abstract] [Full Text] [Related]

  • 6. 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.
    Bioorg Med Chem Lett; 2012 Apr 15; 22(8):2818-22. PubMed ID: 22444685
    [Abstract] [Full Text] [Related]

  • 7. 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.
    Bioorg Med Chem Lett; 2013 Dec 01; 23(23):6228-33. PubMed ID: 24157366
    [Abstract] [Full Text] [Related]

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  • 9. Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.
    Zhou C, Garcia-Calvo M, Pinto S, Lombardo M, Feng Z, Bender K, Pryor KD, Bhatt UR, Chabin RM, Geissler WM, Shen Z, Tong X, Zhang Z, Wong KK, Roy RS, Chapman KT, Yang L, Xiong Y.
    J Med Chem; 2010 Oct 14; 53(19):7251-63. PubMed ID: 20857914
    [Abstract] [Full Text] [Related]

  • 10. Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
    Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.
    Bioorg Med Chem Lett; 2011 Dec 01; 21(23):7006-12. PubMed ID: 22018461
    [Abstract] [Full Text] [Related]

  • 11. Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.
    Erlanson DA, Arndt JW, Cancilla MT, Cao K, Elling RA, English N, Friedman J, Hansen SK, Hession C, Joseph I, Kumaravel G, Lee WC, Lind KE, McDowell RS, Miatkowski K, Nguyen C, Nguyen TB, Park S, Pathan N, Penny DM, Romanowski MJ, Scott D, Silvian L, Simmons RL, Tangonan BT, Yang W, Sun L.
    Bioorg Med Chem Lett; 2011 May 15; 21(10):3078-83. PubMed ID: 21459573
    [Abstract] [Full Text] [Related]

  • 12. Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
    Moffett K, Konteatis Z, Nguyen D, Shetty R, Ludington J, Fujimoto T, Lee KJ, Chai X, Namboodiri H, Karpusas M, Dorsey B, Guarnieri F, Bukhtiyarova M, Springman E, Michelotti E.
    Bioorg Med Chem Lett; 2011 Dec 01; 21(23):7155-65. PubMed ID: 22014550
    [Abstract] [Full Text] [Related]

  • 13. Discovery of novel SCD1 inhibitors: 5-alkyl-4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4'-piperidine] analogs.
    Uto Y, Ueno Y, Kiyotsuka Y, Miyazawa Y, Kurata H, Ogata T, Takagi T, Wakimoto S, Ohsumi J.
    Eur J Med Chem; 2011 May 01; 46(5):1892-6. PubMed ID: 21356569
    [Abstract] [Full Text] [Related]

  • 14. Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.
    Kim S, Jung JK, Lee HS, Kim Y, Kim J, Choi K, Baek DJ, Moon B, Oh KS, Lee BH, Shin KJ, Pae AN, Nam G, Roh EJ, Cho YS, Choo H.
    Bioorg Med Chem Lett; 2011 May 15; 21(10):3002-6. PubMed ID: 21489792
    [Abstract] [Full Text] [Related]

  • 15. Prolylcarboxypeptidase (PrCP) inhibitors and the therapeutic uses thereof: a patent review.
    Graham TH.
    Expert Opin Ther Pat; 2017 Oct 15; 27(10):1077-1088. PubMed ID: 28699813
    [Abstract] [Full Text] [Related]

  • 16. Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.
    Staben ST, Siu M, Goldsmith R, Olivero AG, Do S, Burdick DJ, Heffron TP, Dotson J, Sutherlin DP, Zhu BY, Tsui V, Le H, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Sideris S, Wiesmann C, Wu P.
    Bioorg Med Chem Lett; 2011 Jul 01; 21(13):4054-8. PubMed ID: 21636270
    [Abstract] [Full Text] [Related]

  • 17. Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound.
    McElroy WT, Tan Z, Basu K, Yang SW, Smotryski J, Ho GD, Tulshian D, Greenlee WJ, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R.
    Bioorg Med Chem Lett; 2012 Feb 01; 22(3):1335-9. PubMed ID: 22227212
    [Abstract] [Full Text] [Related]

  • 18. Discovery of novel benzoxazinones as potent and orally active long chain fatty acid elongase 6 inhibitors.
    Mizutani T, Ishikawa S, Nagase T, Takahashi H, Fujimura T, Sasaki T, Nagumo A, Shimamura K, Miyamoto Y, Kitazawa H, Kanesaka M, Yoshimoto R, Aragane K, Tokita S, Sato N.
    J Med Chem; 2009 Nov 26; 52(22):7289-300. PubMed ID: 19883081
    [Abstract] [Full Text] [Related]

  • 19. Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors.
    Yun W, Ahmad M, Chen Y, Gillespie P, Conde-Knape K, Kazmer S, Li S, Qian Y, Taub R, Wertheimer SJ, Whittard T, Bolin D.
    Bioorg Med Chem Lett; 2011 Dec 01; 21(23):7205-9. PubMed ID: 22001092
    [Abstract] [Full Text] [Related]

  • 20. Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
    Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, Shieh H, Xing L, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Messing D, Yang J, Mao MK, Yalamanchili G, Vonder Embse R, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB.
    Bioorg Med Chem Lett; 2011 Jul 01; 21(13):4066-71. PubMed ID: 21641211
    [Abstract] [Full Text] [Related]

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