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Items: 32


Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.

Xie SC, Gillett DL, Spillman NJ, Tsu C, Luth MR, Ottilie S, Duffy S, Gould AE, Hales P, Seager BA, Charron CL, Bruzzese F, Yang X, Zhao X, Huang SC, Hutton CA, Burrows JN, Winzeler EA, Avery VM, Dick LR, Tilley L.

J Med Chem. 2018 Nov 21;61(22):10053-10066. doi: 10.1021/acs.jmedchem.8b01161. Epub 2018 Nov 7.


Co-inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity.

Basler M, Lindstrom MM, LaStant JJ, Bradshaw JM, Owens TD, Schmidt C, Maurits E, Tsu C, Overkleeft HS, Kirk CJ, Langrish CL, Groettrup M.

EMBO Rep. 2018 Dec;19(12). pii: e46512. doi: 10.15252/embr.201846512. Epub 2018 Oct 2.


Proteasome inhibitors bortezomib and carfilzomib used for the treatment of multiple myeloma do not inhibit the serine protease HtrA2/Omi.

Csizmadia V, Hales P, Tsu C, Ma J, Chen J, Shah P, Fleming P, Senn JJ, Kadambi VJ, Dick L, Wolenski FS.

Toxicol Res (Camb). 2016 Aug 25;5(6):1619-1628. doi: 10.1039/c6tx00220j. eCollection 2016 Nov 1.


Cleavage Specificity of Mycobacterium tuberculosis ClpP1P2 Protease and Identification of Novel Peptide Substrates and Boronate Inhibitors with Anti-bacterial Activity.

Akopian T, Kandror O, Tsu C, Lai JH, Wu W, Liu Y, Zhao P, Park A, Wolf L, Dick LR, Rubin EJ, Bachovchin W, Goldberg AL.

J Biol Chem. 2015 Apr 24;290(17):11008-20. doi: 10.1074/jbc.M114.625640. Epub 2015 Mar 10.


Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.

Blackburn C, Barrett C, Brunson M, Chin J, England D, Garcia K, Gigstad K, Gould A, Gutierrez J, Hoar K, Rowland RS, Tsu C, Ringeling J, Wager K, Xu H.

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5450-4.


Identification of potent and selective non-covalent inhibitors of the Plasmodium falciparum proteasome.

Li H, Tsu C, Blackburn C, Li G, Hales P, Dick L, Bogyo M.

J Am Chem Soc. 2014 Oct 1;136(39):13562-5. doi: 10.1021/ja507692y. Epub 2014 Sep 19.


Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.

Blackburn C, Barrett C, Chin J, Garcia K, Gigstad K, Gould A, Gutierrez J, Harrison S, Hoar K, Lynch C, Rowland RS, Tsu C, Ringeling J, Xu H.

J Med Chem. 2013 Sep 26;56(18):7201-11. doi: 10.1021/jm400385r. Epub 2013 Sep 4.


N,C-Capped dipeptides with selectivity for mycobacterial proteasome over human proteasomes: role of S3 and S1 binding pockets.

Lin G, Chidawanyika T, Tsu C, Warrier T, Vaubourgeix J, Blackburn C, Gigstad K, Sintchak M, Dick L, Nathan C.

J Am Chem Soc. 2013 Jul 10;135(27):9968-71. doi: 10.1021/ja400021x. Epub 2013 Jun 25.


Why the structure but not the activity of the immunoproteasome subunit low molecular mass polypeptide 2 rescues antigen presentation.

Basler M, Lauer C, Moebius J, Weber R, Przybylski M, Kisselev AF, Tsu C, Groettrup M.

J Immunol. 2012 Aug 15;189(4):1868-77. doi: 10.4049/jimmunol.1103592. Epub 2012 Jul 6.


Mechanistic studies of substrate-assisted inhibition of ubiquitin-activating enzyme by adenosine sulfamate analogues.

Chen JJ, Tsu CA, Gavin JM, Milhollen MA, Bruzzese FJ, Mallender WD, Sintchak MD, Bump NJ, Yang X, Ma J, Loke HK, Xu Q, Li P, Bence NF, Brownell JE, Dick LR.

J Biol Chem. 2011 Nov 25;286(47):40867-77. doi: 10.1074/jbc.M111.279984. Epub 2011 Oct 3.


Preclinical evaluation of the antitumor activity of bortezomib in combination with vitamin C or with epigallocatechin gallate, a component of green tea.

Bannerman B, Xu L, Jones M, Tsu C, Yu J, Hales P, Monbaliu J, Fleming P, Dick L, Manfredi M, Claiborne C, Bolen J, Kupperman E, Berger A.

Cancer Chemother Pharmacol. 2011 Nov;68(5):1145-54. doi: 10.1007/s00280-011-1591-2. Epub 2011 Mar 13.


Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome.

Blackburn C, Barrett C, Blank JL, Bruzzese FJ, Bump N, Dick LR, Fleming P, Garcia K, Hales P, Hu Z, Jones M, Liu JX, Sappal DS, Sintchak MD, Tsu C, Gigstad KM.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6581-6. doi: 10.1016/j.bmcl.2010.09.032. Epub 2010 Sep 15.


Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit.

Blackburn C, Gigstad KM, Hales P, Garcia K, Jones M, Bruzzese FJ, Barrett C, Liu JX, Soucy TA, Sappal DS, Bump N, Olhava EJ, Fleming P, Dick LR, Tsu C, Sintchak MD, Blank JL.

Biochem J. 2010 Sep 15;430(3):461-76. doi: 10.1042/BJ20100383. Erratum in: Biochem J. 2010 Oct 11;431(3):433.


Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer.

Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu J, Yang Y, Hales P, Bruzzese F, Liu J, Blank J, Garcia K, Tsu C, Dick L, Fleming P, Yu L, Manfredi M, Rolfe M, Bolen J.

Cancer Res. 2010 Mar 1;70(5):1970-80. doi: 10.1158/0008-5472.CAN-09-2766. Epub 2010 Feb 16. Erratum in: Cancer Res. 2010 May 1;70(9):3853. Hales, Paul [added].


Development of a charcoal paper adenosine triphosphate:pyrophosphate exchange assay: kinetic characterization of NEDD8 activating enzyme.

Bruzzese FJ, Tsu CA, Ma J, Loke HK, Wu D, Li Z, Tayber O, Dick LR.

Anal Biochem. 2009 Nov 1;394(1):24-9. doi: 10.1016/j.ab.2009.07.011. Epub 2009 Jul 12.


Distinct specificities of Mycobacterium tuberculosis and mammalian proteasomes for N-acetyl tripeptide substrates.

Lin G, Tsu C, Dick L, Zhou XK, Nathan C.

J Biol Chem. 2008 Dec 5;283(49):34423-31. doi: 10.1074/jbc.M805324200. Epub 2008 Oct 1.


Comparison of biochemical and biological effects of ML858 (salinosporamide A) and bortezomib.

Williamson MJ, Blank JL, Bruzzese FJ, Cao Y, Daniels JS, Dick LR, Labutti J, Mazzola AM, Patil AD, Reimer CL, Solomon MS, Stirling M, Tian Y, Tsu CA, Weatherhead GS, Zhang JX, Rolfe M.

Mol Cancer Ther. 2006 Dec;5(12):3052-61.


Correlation of serpin-protease expression by comparative analysis of real-time PCR profiling data.

Badola S, Spurling H, Robison K, Fedyk ER, Silverman GA, Strayle J, Kapeller R, Tsu CA.

Genomics. 2006 Aug;88(2):173-84. Epub 2006 May 18.


The Caenorhabditis elegans muscle specific serpin, SRP-3, neutralizes chymotrypsin-like serine peptidases.

Pak SC, Tsu C, Luke CJ, Askew YS, Silverman GA.

Biochemistry. 2006 Apr 11;45(14):4474-80.


Mycobacterium tuberculosis prcBA genes encode a gated proteasome with broad oligopeptide specificity.

Lin G, Hu G, Tsu C, Kunes YZ, Li H, Dick L, Parsons T, Li P, Chen Z, Zwickl P, Weich N, Nathan C.

Mol Microbiol. 2006 Mar;59(5):1405-16.


SRP-2 is a cross-class inhibitor that participates in postembryonic development of the nematode Caenorhabditis elegans: initial characterization of the clade L serpins.

Pak SC, Kumar V, Tsu C, Luke CJ, Askew YS, Askew DJ, Mills DR, Brömme D, Silverman GA.

J Biol Chem. 2004 Apr 9;279(15):15448-59. Epub 2004 Jan 22.


The serpin SQN-5 is a dual mechanistic-class inhibitor of serine and cysteine proteinases.

Al-Khunaizi M, Luke CJ, Askew YS, Pak SC, Askew DJ, Cataltepe S, Miller D, Mills DR, Tsu C, Brömme D, Irving JA, Whisstock JC, Silverman GA.

Biochemistry. 2002 Mar 5;41(9):3189-99.


Circulating serpin tumor markers SCCA1 and SCCA2 are not actively secreted but reside in the cytosol of squamous carcinoma cells.

Uemura Y, Pak SC, Luke C, Cataltepe S, Tsu C, Schick C, Kamachi Y, Pomeroy SL, Perlmutter DH, Silverman GA.

Int J Cancer. 2000 Jul 20;89(4):368-77.


Simple modifications of the serpin reactive site loop convert SCCA2 into a cysteine proteinase inhibitor: a critical role for the P3' proline in facilitating RSL cleavage.

Luke C, Schick C, Tsu C, Whisstock JC, Irving JA, Brömme D, Juliano L, Shi GP, Chapman HA, Silverman GA.

Biochemistry. 2000 Jun 20;39(24):7081-91.


Structural basis for the broad substrate specificity of fiddler crab collagenolytic serine protease 1.

Tsu CA, Perona JJ, Fletterick RJ, Craik CS.

Biochemistry. 1997 May 6;36(18):5393-401.


Crystal structure of an ecotin-collagenase complex suggests a model for recognition and cleavage of the collagen triple helix.

Perona JJ, Tsu CA, Craik CS, Fletterick RJ.

Biochemistry. 1997 May 6;36(18):5381-92.


Substrate recognition by recombinant serine collagenase 1 from Uca pugilator.

Tsu CA, Craik CS.

J Biol Chem. 1996 May 10;271(19):11563-70.


The substrate specificity of Uca pugilator collagenolytic serine protease 1 correlates with the bovine type I collagen cleavage sites.

Tsu CA, Perona JJ, Schellenberger V, Turck CW, Craik CS.

J Biol Chem. 1994 Jul 29;269(30):19565-72.


Relocating a negative charge in the binding pocket of trypsin.

Perona JJ, Tsu CA, McGrath ME, Craik CS, Fletterick RJ.

J Mol Biol. 1993 Apr 5;230(3):934-49.


Crystal structures of rat anionic trypsin complexed with the protein inhibitors APPI and BPTI.

Perona JJ, Tsu CA, Craik CS, Fletterick RJ.

J Mol Biol. 1993 Apr 5;230(3):919-33.


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