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Items: 15

1.

Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening.

Crowe A, Huang W, Ballatore C, Johnson RL, Hogan AM, Huang R, Wichterman J, McCoy J, Huryn D, Auld DS, Smith AB 3rd, Inglese J, Trojanowski JQ, Austin CP, Brunden KR, Lee VM.

Biochemistry. 2009 Aug 18;48(32):7732-45. doi: 10.1021/bi9006435.

2.

2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.

Ferguson GN, Valant C, Horne J, Figler H, Flynn BL, Linden J, Chalmers DK, Sexton PM, Christopoulos A, Scammells PJ.

J Med Chem. 2008 Oct 9;51(19):6165-72. doi: 10.1021/jm800557d. Epub 2008 Sep 5.

3.

Differentiating Alzheimer disease-associated aggregates with small molecules.

Honson NS, Johnson RL, Huang W, Inglese J, Austin CP, Kuret J.

Neurobiol Dis. 2007 Dec;28(3):251-60. Epub 2007 Jul 28.

4.

High throughput screening for small molecule inhibitors of heparin-induced tau fibril formation.

Crowe A, Ballatore C, Hyde E, Trojanowski JQ, Lee VM.

Biochem Biophys Res Commun. 2007 Jun 22;358(1):1-6. Epub 2007 Mar 19.

5.

Interpreting steep dose-response curves in early inhibitor discovery.

Shoichet BK.

J Med Chem. 2006 Dec 14;49(25):7274-7.

PMID:
17149857
6.

Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries.

Inglese J, Auld DS, Jadhav A, Johnson RL, Simeonov A, Yasgar A, Zheng W, Austin CP.

Proc Natl Acad Sci U S A. 2006 Aug 1;103(31):11473-8. Epub 2006 Jul 24.

7.

Inducible expression of Tau repeat domain in cell models of tauopathy: aggregation is toxic to cells but can be reversed by inhibitor drugs.

Khlistunova I, Biernat J, Wang Y, Pickhardt M, von Bergen M, Gazova Z, Mandelkow E, Mandelkow EM.

J Biol Chem. 2006 Jan 13;281(2):1205-14. Epub 2005 Oct 24.

8.

Inhibition of heparin-induced tau filament formation by phenothiazines, polyphenols, and porphyrins.

Taniguchi S, Suzuki N, Masuda M, Hisanaga S, Iwatsubo T, Goedert M, Hasegawa M.

J Biol Chem. 2005 Mar 4;280(9):7614-23. Epub 2004 Dec 17.

9.

Anthraquinones inhibit tau aggregation and dissolve Alzheimer's paired helical filaments in vitro and in cells.

Pickhardt M, Gazova Z, von Bergen M, Khlistunova I, Wang Y, Hascher A, Mandelkow EM, Biernat J, Mandelkow E.

J Biol Chem. 2005 Feb 4;280(5):3628-35. Epub 2004 Nov 2.

10.

A specific mechanism of nonspecific inhibition.

McGovern SL, Helfand BT, Feng B, Shoichet BK.

J Med Chem. 2003 Sep 25;46(20):4265-72.

PMID:
13678405
11.

A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.

McGovern SL, Caselli E, Grigorieff N, Shoichet BK.

J Med Chem. 2002 Apr 11;45(8):1712-22.

PMID:
11931626
12.

Mutations of tau protein in frontotemporal dementia promote aggregation of paired helical filaments by enhancing local beta-structure.

von Bergen M, Barghorn S, Li L, Marx A, Biernat J, Mandelkow EM, Mandelkow E.

J Biol Chem. 2001 Dec 21;276(51):48165-74. Epub 2001 Oct 17.

13.

Mutation-specific functional impairments in distinct tau isoforms of hereditary FTDP-17.

Hong M, Zhukareva V, Vogelsberg-Ragaglia V, Wszolek Z, Reed L, Miller BI, Geschwind DH, Bird TD, McKeel D, Goate A, Morris JC, Wilhelmsen KC, Schellenberg GD, Trojanowski JQ, Lee VM.

Science. 1998 Dec 4;282(5395):1914-7.

14.

Selective inhibition of Alzheimer disease-like tau aggregation by phenothiazines.

Wischik CM, Edwards PC, Lai RY, Roth M, Harrington CR.

Proc Natl Acad Sci U S A. 1996 Oct 1;93(20):11213-8.

15.

Domains of tau protein and interactions with microtubules.

Gustke N, Trinczek B, Biernat J, Mandelkow EM, Mandelkow E.

Biochemistry. 1994 Aug 16;33(32):9511-22.

PMID:
8068626

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