BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

127 related articles for article (PubMed ID: 23713656)

  • 1. Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
    Probst G; Aubele DL; Bowers S; Dressen D; Garofalo AW; Hom RK; Konradi AW; Marugg JL; Mattson MN; Neitzel ML; Semko CM; Sham HL; Smith J; Sun M; Truong AP; Ye XM; Xu YZ; Dappen MS; Jagodzinski JJ; Keim PS; Peterson B; Latimer LH; Quincy D; Wu J; Goldbach E; Ness DK; Quinn KP; Sauer JM; Wong K; Zhang H; Zmolek W; Brigham EF; Kholodenko D; Hu K; Kwong GT; Lee M; Liao A; Motter RN; Sacayon P; Santiago P; Willits C; Bard F; Bova MP; Hemphill SS; Nguyen L; Ruslim L; Tanaka K; Tanaka P; Wallace W; Yednock TA; Basi GS
    J Med Chem; 2013 Jul; 56(13):5261-74. PubMed ID: 23713656
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.
    Aubele DL; Truong AP; Dressen DB; Probst GD; Bowers S; Mattson MN; Semko CM; Sun M; Garofalo AW; Konradi AW; Sham HL; Zmolek W; Wong K; Goldbach E; Quinn KP; Sauer JM; Brigham EF; Wallace W; Nguyen L; Bova MP; Hemphill SS; Basi G
    Bioorg Med Chem Lett; 2011 Oct; 21(19):5791-4. PubMed ID: 21885276
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Dynamics of Aβ42 reduction in plasma, CSF and brain of rats treated with the γ-secretase modulator, GSM-10h.
    Hawkins J; Harrison DC; Ahmed S; Davis RP; Chapman T; Marshall I; Smith B; Mead TL; Medhurst A; Giblin GM; Hall A; Gonzalez MI; Richardson J; Hussain I
    Neurodegener Dis; 2011; 8(6):455-64. PubMed ID: 21389687
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
    Martone RL; Zhou H; Atchison K; Comery T; Xu JZ; Huang X; Gong X; Jin M; Kreft A; Harrison B; Mayer SC; Aschmies S; Gonzales C; Zaleska MM; Riddell DR; Wagner E; Lu P; Sun SC; Sonnenberg-Reines J; Oganesian A; Adkins K; Leach MW; Clarke DW; Huryn D; Abou-Gharbia M; Magolda R; Bard J; Frick G; Raje S; Forlow SB; Balliet C; Burczynski ME; Reinhart PH; Wan HI; Pangalos MN; Jacobsen JS
    J Pharmacol Exp Ther; 2009 Nov; 331(2):598-608. PubMed ID: 19671883
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.
    Albright CF; Dockens RC; Meredith JE; Olson RE; Slemmon R; Lentz KA; Wang JS; Denton RR; Pilcher G; Rhyne PW; Raybon JJ; Barten DM; Burton C; Toyn JH; Sankaranarayanan S; Polson C; Guss V; White R; Simutis F; Sanderson T; Gillman KW; Starrett JE; Bronson J; Sverdlov O; Huang SP; Castaneda L; Feldman H; Coric V; Zaczek R; Macor JE; Houston J; Berman RM; Tong G
    J Pharmacol Exp Ther; 2013 Mar; 344(3):686-95. PubMed ID: 23275065
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
    Mayer SC; Kreft AF; Harrison B; Abou-Gharbia M; Antane M; Aschmies S; Atchison K; Chlenov M; Cole DC; Comery T; Diamantidis G; Ellingboe J; Fan K; Galante R; Gonzales C; Ho DM; Hoke ME; Hu Y; Huryn D; Jain U; Jin M; Kremer K; Kubrak D; Lin M; Lu P; Magolda R; Martone R; Moore W; Oganesian A; Pangalos MN; Porte A; Reinhart P; Resnick L; Riddell DR; Sonnenberg-Reines J; Stock JR; Sun SC; Wagner E; Wang T; Woller K; Xu Z; Zaleska MM; Zeldis J; Zhang M; Zhou H; Jacobsen JS
    J Med Chem; 2008 Dec; 51(23):7348-51. PubMed ID: 19012391
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.
    Toyn JH; Boy KM; Raybon J; Meredith JE; Robertson AS; Guss V; Hoque N; Sweeney F; Zhuo X; Clarke W; Snow K; Denton RR; Zuev D; Thompson LA; Morrison J; Grace J; Berisha F; Furlong M; Wang JS; Lentz KA; Padmanabha R; Cook L; Wei C; Drexler DM; Macor JE; Albright CF; Gasior M; Olson RE; Hong Q; Soares HD; AbuTarif M; Ahlijanian MK
    J Pharmacol Exp Ther; 2016 Jul; 358(1):125-37. PubMed ID: 27189974
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Quantification of gamma-secretase modulation differentiates inhibitor compound selectivity between two substrates Notch and amyloid precursor protein.
    Yang T; Arslanova D; Gu Y; Augelli-Szafran C; Xia W
    Mol Brain; 2008 Nov; 1():15. PubMed ID: 18983676
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Multicenter, randomized, double-blind, placebo-controlled, single-ascending dose study of the oral γ-secretase inhibitor BMS-708163 (Avagacestat): tolerability profile, pharmacokinetic parameters, and pharmacodynamic markers.
    Tong G; Wang JS; Sverdlov O; Huang SP; Slemmon R; Croop R; Castaneda L; Gu H; Wong O; Li H; Berman RM; Smith C; Albright CF; Dockens RC
    Clin Ther; 2012 Mar; 34(3):654-67. PubMed ID: 22381714
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
    Ye XM; Konradi AW; Sun M; Yuan S; Aubele DL; Dappen M; Dressen D; Garofalo AW; Jagodzinski JJ; Latimer L; Probst GD; Sham HL; Wone D; Xu YZ; Ness D; Brigham E; Kwong GT; Willtis C; Tonn G; Goldbach E; Quinn KP; Zhang HH; Sauer JM; Bova M; Basi GS
    Bioorg Med Chem Lett; 2013 Feb; 23(4):996-1000. PubMed ID: 23312944
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central β-Amyloid Reduction and Minimal Covalent Binding Burden.
    Anan K; Iso Y; Oguma T; Nakahara K; Suzuki S; Yamamoto T; Matsuoka E; Ito H; Sakaguchi G; Ando S; Morimoto K; Kanegawa N; Kido Y; Kawachi T; Fukushima T; Teisman A; Urmaliya V; Dhuyvetter D; Borghys H; Austin N; Van Den Bergh A; Verboven P; Bischoff F; Gijsen HJM; Yamano Y; Kusakabe K
    ChemMedChem; 2019 Nov; 14(22):1894-1910. PubMed ID: 31657130
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Discovery of notch-sparing gamma-secretase inhibitors.
    Augelli-Szafran CE; Wei HX; Lu D; Zhang J; Gu Y; Yang T; Osenkowski P; Ye W; Wolfe MS
    Curr Alzheimer Res; 2010 May; 7(3):207-9. PubMed ID: 20088802
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
    Truong AP; Aubele DL; Probst GD; Neitzel ML; Semko CM; Bowers S; Dressen D; Hom RK; Konradi AW; Sham HL; Garofalo AW; Keim PS; Wu J; Dappen MS; Wong K; Goldbach E; Quinn KP; Sauer JM; Brigham EF; Wallace W; Nguyen L; Hemphill SS; Bova MP; Bard F; Yednock TA; Basi G
    Bioorg Med Chem Lett; 2009 Sep; 19(17):4920-3. PubMed ID: 19660943
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Proton myo-inositol cotransporter is a novel γ-secretase associated protein that regulates Aβ production without affecting Notch cleavage.
    Teranishi Y; Inoue M; Yamamoto NG; Kihara T; Wiehager B; Ishikawa T; Winblad B; Schedin-Weiss S; Frykman S; Tjernberg LO
    FEBS J; 2015 Sep; 282(17):3438-51. PubMed ID: 26094765
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.
    Kreft A; Harrison B; Aschmies S; Atchison K; Casebier D; Cole DC; Diamantidis G; Ellingboe J; Hauze D; Hu Y; Huryn D; Jin M; Kubrak D; Lu P; Lundquist J; Mann C; Martone R; Moore W; Oganesian A; Porte A; Riddell DR; Sonnenberg-Reines J; Stock JR; Sun SC; Wagner E; Woller K; Xu Z; Zhou H; Steven Jacobsen J
    Bioorg Med Chem Lett; 2008 Jul; 18(14):4232-6. PubMed ID: 18556202
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.
    Mattson MN; Neitzel ML; Quincy DA; Semko CM; Garofalo AW; Keim PS; Konradi AW; Pleiss MA; Sham HL; Brigham EF; Goldbach EG; Zhang H; Sauer JM; Basi GS
    Bioorg Med Chem Lett; 2010 Apr; 20(7):2148-50. PubMed ID: 20206516
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
    Pu J; Kreft AF; Aschmies SH; Atchison KP; Berkowitz J; Caggiano TJ; Chlenov M; Diamantidis G; Harrison BL; Hu Y; Huryn D; Steven Jacobsen J; Jin M; Lipinski K; Lu P; Martone RL; Morris K; Sonnenberg-Reines J; Riddell DR; Sabalski J; Sun SC; Wagner E; Wang Y; Xu Z; Zhou H; Resnick L
    Bioorg Med Chem; 2009 Jul; 17(13):4708-17. PubMed ID: 19443228
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors.
    Wood S; Wen PH; Zhang J; Zhu L; Luo Y; Babu-Khan S; Chen K; Pham R; Esmay J; Dineen TA; Kaller MR; Weiss MM; Hitchcock SA; Citron M; Zhong W; Hickman D; Williamson T
    J Pharmacol Exp Ther; 2012 Nov; 343(2):460-7. PubMed ID: 22911925
    [TBL] [Abstract][Full Text] [Related]  

  • 19. A formulation strategy for gamma secretase inhibitor ELND006, a BCS class II compound: development of a nanosuspension formulation with improved oral bioavailability and reduced food effects in dogs.
    Quinn K; Gullapalli RP; Merisko-Liversidge E; Goldbach E; Wong A; Liversidge GG; Hoffman W; Sauer JM; Bullock J; Tonn G
    J Pharm Sci; 2012 Apr; 101(4):1462-74. PubMed ID: 22213574
    [TBL] [Abstract][Full Text] [Related]  

  • 20. The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.
    Best JD; Smith DW; Reilly MA; O'Donnell R; Lewis HD; Ellis S; Wilkie N; Rosahl TW; Laroque PA; Boussiquet-Leroux C; Churcher I; Atack JR; Harrison T; Shearman MS
    J Pharmacol Exp Ther; 2007 Feb; 320(2):552-8. PubMed ID: 17099072
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 7.