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Items: 1 to 20 of 104

1.

Design, syntheses, and evaluation of Taspase1 inhibitors.

Lee JT, Chen DY, Yang Z, Ramos AD, Hsieh JJ, Bogyo M.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5086-90. doi: 10.1016/j.bmcl.2009.07.045. Epub 2009 Jul 10.

2.

Taspase1: a threonine aspartase required for cleavage of MLL and proper HOX gene expression.

Hsieh JJ, Cheng EH, Korsmeyer SJ.

Cell. 2003 Oct 31;115(3):293-303.

3.

Development of small molecule inhibitors and probes of human SUMO deconjugating proteases.

Albrow VE, Ponder EL, Fasci D, Békés M, Deu E, Salvesen GS, Bogyo M.

Chem Biol. 2011 Jun 24;18(6):722-32. doi: 10.1016/j.chembiol.2011.05.008.

4.

Bioassays to monitor Taspase1 function for the identification of pharmacogenetic inhibitors.

Knauer SK, Fetz V, Rabenstein J, Friedl S, Hofmann B, Sabiani S, Schröder E, Kunst L, Proschak E, Thines E, Kindler T, Schneider G, Marschalek R, Stauber RH, Bier C.

PLoS One. 2011;6(5):e18253. doi: 10.1371/journal.pone.0018253. Epub 2011 May 25.

5.

A substrate-based difluoro ketone selectively inhibits Alzheimer's gamma-secretase activity.

Wolfe MS, Citron M, Diehl TS, Xia W, Donkor IO, Selkoe DJ.

J Med Chem. 1998 Jan 1;41(1):6-9. No abstract available.

PMID:
9438016
6.

3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitors.

Shaw D, Best J, Dinnell K, Nadin A, Shearman M, Pattison C, Peachey J, Reilly M, Williams B, Wrigley J, Harrison T.

Bioorg Med Chem Lett. 2006 Jun 1;16(11):3073-7. Epub 2006 Apr 17.

PMID:
16617016
7.

Design, synthesis, and evaluation of trifluoromethyl ketones as inhibitors of SARS-CoV 3CL protease.

Shao YM, Yang WB, Kuo TH, Tsai KC, Lin CH, Yang AS, Liang PH, Wong CH.

Bioorg Med Chem. 2008 Apr 15;16(8):4652-60. doi: 10.1016/j.bmc.2008.02.040. Epub 2008 Feb 15.

PMID:
18329272
8.

Aspartic vinyl sulfones: inhibitors of a caspase-3-dependent pathway.

Glória PM, Coutinho I, Gonçalves LM, Baptista C, Soares J, Newton AS, Moreira R, Saraiva L, Santos MM.

Eur J Med Chem. 2011 Jun;46(6):2141-6. doi: 10.1016/j.ejmech.2011.02.067. Epub 2011 Mar 5.

PMID:
21439692
9.

Peptide inhibitors of Dengue virus NS3 protease. Part 1: Warhead.

Yin Z, Patel SJ, Wang WL, Wang G, Chan WL, Rao KR, Alam J, Jeyaraj DA, Ngew X, Patel V, Beer D, Lim SP, Vasudevan SG, Keller TH.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):36-9. Epub 2005 Oct 21.

PMID:
16246553
10.

Difluoro ketone peptidomimetics suggest a large S1 pocket for Alzheimer's gamma-secretase: implications for inhibitor design.

Moore CL, Leatherwood DD, Diehl TS, Selkoe DJ, Wolfe MS.

J Med Chem. 2000 Sep 7;43(18):3434-42.

PMID:
10978191
11.

Design and evaluation of inhibitors for dipeptidyl peptidase I (Cathepsin C).

Kam CM, Götz MG, Koot G, McGuire M, Thiele D, Hudig D, Powers JC.

Arch Biochem Biophys. 2004 Jul 15;427(2):123-34.

PMID:
15196986
12.

Novel peptidyl aryl vinyl sulfones as highly potent and selective inhibitors of cathepsins L and B.

Mendieta L, Picó A, Tarragó T, Teixidó M, Castillo M, Rafecas L, Moyano A, Giralt E.

ChemMedChem. 2010 Sep 3;5(9):1556-67. doi: 10.1002/cmdc.201000109.

PMID:
20652927
13.

Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones.

Bandarage UK, Wang T, Come JH, Perola E, Wei Y, Rao BG.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):44-8. Epub 2007 Nov 13.

PMID:
18054488
14.
15.

A pharmacologic inhibitor of the protease Taspase1 effectively inhibits breast and brain tumor growth.

Chen DY, Lee Y, Van Tine BA, Searleman AC, Westergard TD, Liu H, Tu HC, Takeda S, Dong Y, Piwnica-Worms DR, Oh KJ, Korsmeyer SJ, Hermone A, Gussio R, Shoemaker RH, Cheng EH, Hsieh JJ.

Cancer Res. 2012 Feb 1;72(3):736-46. doi: 10.1158/0008-5472.CAN-11-2584. Epub 2011 Dec 13.

16.

Proteolysis of MLL family proteins is essential for taspase1-orchestrated cell cycle progression.

Takeda S, Chen DY, Westergard TD, Fisher JK, Rubens JA, Sasagawa S, Kan JT, Korsmeyer SJ, Cheng EH, Hsieh JJ.

Genes Dev. 2006 Sep 1;20(17):2397-409.

17.

Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.

Ettari R, Nizi E, Di Francesco ME, Dude MA, Pradel G, Vicík R, Schirmeister T, Micale N, Grasso S, Zappalà M.

J Med Chem. 2008 Feb 28;51(4):988-96. doi: 10.1021/jm701141u. Epub 2008 Jan 31.

PMID:
18232656
18.

Cell-based analysis of structure-function activity of threonine aspartase 1.

Bier C, Knauer SK, Klapthor A, Schweitzer A, Rekik A, Krämer OH, Marschalek R, Stauber RH.

J Biol Chem. 2011 Jan 28;286(4):3007-17. doi: 10.1074/jbc.M110.161646. Epub 2010 Nov 17.

19.

N-Terminal peptidic boronic acids selectively inhibit human ClpXP.

Knott K, Fishovitz J, Thorpe SB, Lee I, Santos WL.

Org Biomol Chem. 2010 Aug 7;8(15):3451-6. doi: 10.1039/c004247a. Epub 2010 Jun 4.

PMID:
20523950
20.

Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs).

Zhang YM, Fan X, Yang SM, Scannevin RH, Burke SL, Rhodes KJ, Jackson PF.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):405-8. Epub 2007 Oct 18.

PMID:
17980583

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