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Page 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. Prasad CV, et al. Among authors: loo a. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4006-11. doi: 10.1016/j.bmcl.2007.04.082. Epub 2007 Apr 30. Bioorg Med Chem Lett. 2007. PMID: 17502137
Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor.
Barten DM, Guss VL, Corsa JA, Loo A, Hansel SB, Zheng M, Munoz B, Srinivasan K, Wang B, Robertson BJ, Polson CT, Wang J, Roberts SB, Hendrick JP, Anderson JJ, Loy JK, Denton R, Verdoorn TA, Smith DW, Felsenstein KM. Barten DM, et al. Among authors: loo a. J Pharmacol Exp Ther. 2005 Feb;312(2):635-43. doi: 10.1124/jpet.104.075408. Epub 2004 Sep 27. J Pharmacol Exp Ther. 2005. PMID: 15452193
2,3-Benzodiazepin-1,4-diones as peptidomimetic inhibitors of gamma-secretase.
Prasad CV, Vig S, Smith DW, Gao Q, Polson CT, Corsa JA, Guss VL, Loo A, Barten DM, Zheng M, Felsenstein KM, Roberts SB. Prasad CV, et al. Among authors: loo a. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3535-8. doi: 10.1016/j.bmcl.2004.04.056. Bioorg Med Chem Lett. 2004. PMID: 15177468
Amino-caprolactam derivatives as gamma-secretase inhibitors.
Parker MF, Bronson JJ, Barten DM, Corsa JA, Du W, Felsenstein KM, Guss VL, Izzarelli D, Loo A, McElhone KE, Marcin LR, Padmanabha R, Pak R, Polson CT, Toyn JH, Varma S, Wang J, Wong V, Zheng M, Roberts SB. Parker MF, et al. Among authors: loo a. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5790-5. doi: 10.1016/j.bmcl.2007.08.047. Epub 2007 Aug 26. Bioorg Med Chem Lett. 2007. PMID: 17869509
2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors.
Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Dee MF, Gai Y, Guss VL, Higgins MA, Keavy DJ, Loo A, Mate RA, Marcin LR, McElhone KE, Polson CT, Roberts SB, Macor JE. Parker MF, et al. Among authors: loo a. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6828-31. doi: 10.1016/j.bmcl.2012.09.057. Epub 2012 Sep 24. Bioorg Med Chem Lett. 2012. PMID: 23046960
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P. Schoepfer J, et al. Among authors: loo a. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. J Med Chem. 2018. PMID: 30137981
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
Burks HE, Abrams T, Kirby CA, Baird J, Fekete A, Hamann LG, Kim S, Lombardo F, Loo A, Lubicka D, Macchi K, McDonnell DP, Mishina Y, Norris JD, Nunez J, Saran C, Sun Y, Thomsen NM, Wang C, Wang J, Peukert S. Burks HE, et al. Among authors: loo a. J Med Chem. 2017 Apr 13;60(7):2790-2818. doi: 10.1021/acs.jmedchem.6b01468. Epub 2017 Mar 15. J Med Chem. 2017. PMID: 28296398
The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.
Wylie AA, Schoepfer J, Jahnke W, Cowan-Jacob SW, Loo A, Furet P, Marzinzik AL, Pelle X, Donovan J, Zhu W, Buonamici S, Hassan AQ, Lombardo F, Iyer V, Palmer M, Berellini G, Dodd S, Thohan S, Bitter H, Branford S, Ross DM, Hughes TP, Petruzzelli L, Vanasse KG, Warmuth M, Hofmann F, Keen NJ, Sellers WR. Wylie AA, et al. Among authors: loo a. Nature. 2017 Mar 30;543(7647):733-737. doi: 10.1038/nature21702. Epub 2017 Mar 22. Nature. 2017. PMID: 28329763
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
Cho YS, Angove H, Brain C, Chen CH, Cheng H, Cheng R, Chopra R, Chung K, Congreve M, Dagostin C, Davis DJ, Feltell R, Giraldes J, Hiscock SD, Kim S, Kovats S, Lagu B, Lewry K, Loo A, Lu Y, Luzzio M, Maniara W, McMenamin R, Mortenson PN, Benning R, O'Reilly M, Rees DC, Shen J, Smith T, Wang Y, Williams G, Woolford AJ, Wrona W, Xu M, Yang F, Howard S. Cho YS, et al. Among authors: loo a. ACS Med Chem Lett. 2012 May 17;3(6):445-9. doi: 10.1021/ml200241a. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900493 Free PMC article.
270 results