96 related articles for article (PubMed ID: 17502137)
1. Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Prasad CV; Zheng M; Vig S; Bergstrom C; Smith DW; Gao Q; Yeola S; Polson CT; Corsa JA; Guss VL; Loo A; Wang J; Sleczka BG; Dangler C; Robertson BJ; Hendrick JP; Roberts SB; Barten DM
Bioorg Med Chem Lett; 2007 Jul; 17(14):4006-11. PubMed ID: 17502137
[TBL] [Abstract][Full Text] [Related]
2. Ex vivo occupancy of gamma-secretase inhibitors correlates with brain beta-amyloid peptide reduction in Tg2576 mice.
Goldstein ME; Cao Y; Fiedler T; Toyn J; Iben L; Barten DM; Pierdomenico M; Corsa J; Prasad CV; Olson RE; Li YW; Zaczek R; Albright CF
J Pharmacol Exp Ther; 2007 Oct; 323(1):102-8. PubMed ID: 17640949
[TBL] [Abstract][Full Text] [Related]
3. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse.
Hyde LA; McHugh NA; Chen J; Zhang Q; Manfra D; Nomeir AA; Josien H; Bara T; Clader JW; Zhang L; Parker EM; Higgins GA
J Pharmacol Exp Ther; 2006 Dec; 319(3):1133-43. PubMed ID: 16946102
[TBL] [Abstract][Full Text] [Related]
4. Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.
Abramowski D; Wiederhold KH; Furrer U; Jaton AL; Neuenschwander A; Runser MJ; Danner S; Reichwald J; Ammaturo D; Staab D; Stoeckli M; Rueeger H; Neumann U; Staufenbiel M
J Pharmacol Exp Ther; 2008 Nov; 327(2):411-24. PubMed ID: 18687920
[TBL] [Abstract][Full Text] [Related]
5. Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].
Best JD; Jay MT; Otu F; Ma J; Nadin A; Ellis S; Lewis HD; Pattison C; Reilly M; Harrison T; Shearman MS; Williamson TL; Atack JR
J Pharmacol Exp Ther; 2005 May; 313(2):902-8. PubMed ID: 15743924
[TBL] [Abstract][Full Text] [Related]
6. Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY-411575).
Lanz TA; Hosley JD; Adams WJ; Merchant KM
J Pharmacol Exp Ther; 2004 Apr; 309(1):49-55. PubMed ID: 14718585
[TBL] [Abstract][Full Text] [Related]
7. 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]
8. Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897.
Anderson JJ; Holtz G; Baskin PP; Turner M; Rowe B; Wang B; Kounnas MZ; Lamb BT; Barten D; Felsenstein K; McDonald I; Srinivasan K; Munoz B; Wagner SL
Biochem Pharmacol; 2005 Feb; 69(4):689-98. PubMed ID: 15670587
[TBL] [Abstract][Full Text] [Related]
9. 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]
10. 1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicity.
Imbimbo BP; Del Giudice E; Colavito D; D'Arrigo A; Dalle Carbonare M; Villetti G; Facchinetti F; Volta R; Pietrini V; Baroc MF; Serneels L; De Strooper B; Leon A
J Pharmacol Exp Ther; 2007 Dec; 323(3):822-30. PubMed ID: 17895400
[TBL] [Abstract][Full Text] [Related]
11. Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.
Asberom T; Zhao Z; Bara TA; Clader JW; Greenlee WJ; Hyde LA; Josien HB; Li W; McPhail AT; Nomeir AA; Parker EM; Rajagopalan M; Song L; Wong GT; Zhang L; Zhang Q; Pissarnitski DA
Bioorg Med Chem Lett; 2007 Jan; 17(2):511-6. PubMed ID: 17079141
[TBL] [Abstract][Full Text] [Related]
12. Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.
Peters JU; Galley G; Jacobsen H; Czech C; David-Pierson P; Kitas EA; Ozmen L
Bioorg Med Chem Lett; 2007 Nov; 17(21):5918-23. PubMed ID: 17869099
[TBL] [Abstract][Full Text] [Related]
13. Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.
Lu Y; Zhang L; Nolan CE; Becker SL; Atchison K; Robshaw AE; Pustilnik LR; Osgood SM; Miller EH; Stepan AF; Subramanyam C; Efremov I; Hallgren AJ; Riddell D
J Pharmacol Exp Ther; 2011 Dec; 339(3):922-34. PubMed ID: 21930801
[TBL] [Abstract][Full Text] [Related]
14. Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: preparation of (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement.
Churcher I; Williams S; Kerrad S; Harrison T; Castro JL; Shearman MS; Lewis HD; Clarke EE; Wrigley JD; Beher D; Tang YS; Liu W
J Med Chem; 2003 Jun; 46(12):2275-8. PubMed ID: 12773031
[TBL] [Abstract][Full Text] [Related]
15. Differential effects of gamma-secretase and BACE1 inhibition on brain Abeta levels in vitro and in vivo.
Elvang AB; Volbracht C; Pedersen LØ; Jensen KG; Karlsson JJ; Larsen SA; Mørk A; Stensbøl TB; Bastlund JF
J Neurochem; 2009 Sep; 110(5):1377-87. PubMed ID: 19519664
[TBL] [Abstract][Full Text] [Related]
16. Pharmacological evidences for DFK167-sensitive presenilin-independent gamma-secretase-like activity.
Sevalle J; Ayral E; Hernandez JF; Martinez J; Checler F
J Neurochem; 2009 Jul; 110(1):275-83. PubMed ID: 19457123
[TBL] [Abstract][Full Text] [Related]
17. Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.
Lanz TA; Karmilowicz MJ; Wood KM; Pozdnyakov N; Du P; Piotrowski MA; Brown TM; Nolan CE; Richter KE; Finley JE; Fei Q; Ebbinghaus CF; Chen YL; Spracklin DK; Tate B; Geoghegan KF; Lau LF; Auperin DD; Schachter JB
J Pharmacol Exp Ther; 2006 Nov; 319(2):924-33. PubMed ID: 16920992
[TBL] [Abstract][Full Text] [Related]
18. Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
Kreft AF; Martone R; Porte A
J Med Chem; 2009 Oct; 52(20):6169-88. PubMed ID: 19694467
[No Abstract] [Full Text] [Related]
19. Secretase inhibitors and modulators for Alzheimer's disease treatment.
Tomita T
Expert Rev Neurother; 2009 May; 9(5):661-79. PubMed ID: 19402777
[TBL] [Abstract][Full Text] [Related]
20. Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.
McBriar MD; Clader JW; Chu I; Del Vecchio RA; Favreau L; Greenlee WJ; Hyde LA; Nomeir AA; Parker EM; Pissarnitski DA; Song L; Zhang L; Zhao Z
Bioorg Med Chem Lett; 2008 Jan; 18(1):215-9. PubMed ID: 17988864
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
