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Items: 32

1.

Fragment screening for a protein-protein interaction inhibitor to WDR5.

Dennis ML, Morrow BJ, Dolezal O, Cuzzupe AN, Stupple AE, Newman J, Bentley J, Hattarki M, Nuttall SD, Foitzik RC, Street IP, Stupple PA, Monahan BJ, Peat TS.

Struct Dyn. 2019 Nov 14;6(6):064701. doi: 10.1063/1.5122849. eCollection 2019 Nov.

2.

Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.

Leaver DJ, Cleary B, Nguyen N, Priebbenow DL, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Sabroux HJ, Falk H, Chung MC, Hermans SJ, Parker MW, Thomas T, Baell JB.

J Med Chem. 2019 Aug 8;62(15):7146-7159. doi: 10.1021/acs.jmedchem.9b00665. Epub 2019 Jul 17.

PMID:
31256587
3.

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth.

Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T.

Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1.

PMID:
30069049
4.

De-novo designed library of benzoylureas as inhibitors of BCL-XL: synthesis, structural and biochemical characterization.

Brady RM, Vom A, Roy MJ, Toovey N, Smith BJ, Moss RM, Hatzis E, Huang DC, Parisot JP, Yang H, Street IP, Colman PM, Czabotar PE, Baell JB, Lessene G.

J Med Chem. 2014 Feb 27;57(4):1323-43. doi: 10.1021/jm401948b. Epub 2014 Feb 5.

PMID:
24456288
5.

Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.

Sleebs BE, Kersten WJ, Kulasegaram S, Nikolakopoulos G, Hatzis E, Moss RM, Parisot JP, Yang H, Czabotar PE, Fairlie WD, Lee EF, Adams JM, Chen L, van Delft MF, Lowes KN, Wei A, Huang DC, Colman PM, Street IP, Baell JB, Watson K, Lessene G.

J Med Chem. 2013 Jul 11;56(13):5514-40. doi: 10.1021/jm400556w. Epub 2013 Jun 26.

PMID:
23767404
6.

Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling.

Zhang L, Holmes IP, Hochgräfe F, Walker SR, Ali NA, Humphrey ES, Wu J, de Silva M, Kersten WJ, Connor T, Falk H, Allan L, Street IP, Bentley JD, Pilling PA, Monahan BJ, Peat TS, Daly RJ.

J Proteome Res. 2013 Jul 5;12(7):3104-16. doi: 10.1021/pr3008495. Epub 2013 Jun 25.

PMID:
23692254
7.

Structure-guided design of a selective BCL-X(L) inhibitor.

Lessene G, Czabotar PE, Sleebs BE, Zobel K, Lowes KN, Adams JM, Baell JB, Colman PM, Deshayes K, Fairbrother WJ, Flygare JA, Gibbons P, Kersten WJ, Kulasegaram S, Moss RM, Parisot JP, Smith BJ, Street IP, Yang H, Huang DC, Watson KG.

Nat Chem Biol. 2013 Jun;9(6):390-7. doi: 10.1038/nchembio.1246. Epub 2013 Apr 21.

PMID:
23603658
8.

An in vivo large-scale chemical screening platform using Drosophila for anti-cancer drug discovery.

Willoughby LF, Schlosser T, Manning SA, Parisot JP, Street IP, Richardson HE, Humbert PO, Brumby AM.

Dis Model Mech. 2013 Mar;6(2):521-9. doi: 10.1242/dmm.009985. Epub 2012 Sep 20.

9.

Synthesis of conformationally constrained benzoylureas as BH3-mimetics.

Brady RM, Hatzis E, Connor T, Street IP, Baell JB, Lessene G.

Org Biomol Chem. 2012 Jul 21;10(27):5230-7. doi: 10.1039/c2ob25618e. Epub 2012 May 30.

PMID:
22648632
10.

An efficient high-throughput screening method for MYST family acetyltransferases, a new class of epigenetic drug targets.

Falk H, Connor T, Yang H, Loft KJ, Alcindor JL, Nikolakopoulos G, Surjadi RN, Bentley JD, Hattarki MK, Dolezal O, Murphy JM, Monahan BJ, Peat TS, Thomas T, Baell JB, Parisot JP, Street IP.

J Biomol Screen. 2011 Dec;16(10):1196-205. doi: 10.1177/1087057111421631. Epub 2011 Nov 14.

PMID:
22086725
11.

Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors.

Sleebs BE, Nikolakopoulos G, Street IP, Falk H, Baell JB.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5992-4. doi: 10.1016/j.bmcl.2011.07.050. Epub 2011 Jul 23. Erratum in: Bioorg Med Chem Lett. 2012 Jan 1;22(1):755-7.

PMID:
21852129
12.

Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: discovery, synthesis, and characterization of their binding mode by protein crystallography.

Patterson S, Alphey MS, Jones DC, Shanks EJ, Street IP, Frearson JA, Wyatt PG, Gilbert IH, Fairlamb AH.

J Med Chem. 2011 Oct 13;54(19):6514-30. doi: 10.1021/jm200312v. Epub 2011 Sep 1.

13.

Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.

Sleebs BE, Czabotar PE, Fairbrother WJ, Fairlie WD, Flygare JA, Huang DC, Kersten WJ, Koehler MF, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H, Baell JB.

J Med Chem. 2011 Mar 24;54(6):1914-26. doi: 10.1021/jm101596e. Epub 2011 Mar 2.

PMID:
21366295
14.

Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi.

Holloway GA, Parisot JP, Novello PM, Watson KG, Armstrong T, Thompson RC, Street IP, Baell JB.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1816-8. doi: 10.1016/j.bmcl.2010.02.022. Epub 2010 Feb 8.

PMID:
20185305
15.

Inhibitors of Leishmania GDP-mannose pyrophosphorylase identified by high-throughput screening of small-molecule chemical library.

Lackovic K, Parisot JP, Sleebs N, Baell JB, Debien L, Watson KG, Curtis JM, Handman E, Street IP, Kedzierski L.

Antimicrob Agents Chemother. 2010 May;54(5):1712-9. doi: 10.1128/AAC.01634-09. Epub 2010 Feb 16.

16.

Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.

Holloway GA, Charman WN, Fairlamb AH, Brun R, Kaiser M, Kostewicz E, Novello PM, Parisot JP, Richardson J, Street IP, Watson KG, Baell JB.

Antimicrob Agents Chemother. 2009 Jul;53(7):2824-33. doi: 10.1128/AAC.01568-08. Epub 2009 Apr 13.

17.

Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening.

Holloway GA, Baell JB, Fairlamb AH, Novello PM, Parisot JP, Richardson J, Watson KG, Street IP.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1422-7. Epub 2006 Dec 3.

18.

Substituted glycals as probes of glycosidase mechanisms.

Lai EC, Morris SA, Street IP, Withers SG.

Bioorg Med Chem. 1996 Nov;4(11):1929-37.

PMID:
9007277
19.
20.

A continuous fluorescence-based assay for the human high-molecular-weight cytosolic phospholipase A2.

Huang Z, Laliberté F, Tremblay NM, Weech PK, Street IP.

Anal Biochem. 1994 Oct;222(1):110-5.

PMID:
7856835
21.
22.

NMR structural studies of the tight complex between a trifluoromethyl ketone inhibitor and the 85-kDa human phospholipase A2.

Trimble LA, Street IP, Perrier H, Tremblay NM, Weech PK, Bernstein MA.

Biochemistry. 1993 Nov 30;32(47):12560-5.

PMID:
8251473
23.

Human group II phospholipase A2 expressed in Trichoplusia ni larvae--isolation and kinetic properties of the enzyme.

Tremblay NM, Kennedy BP, Street IP, Kaupp WJ, Laliberté F, Weech PK.

Protein Expr Purif. 1993 Oct;4(5):490-8.

PMID:
8251761
24.

Slow- and tight-binding inhibitors of the 85-kDa human phospholipase A2.

Street IP, Lin HK, Laliberté F, Ghomashchi F, Wang Z, Perrier H, Tremblay NM, Huang Z, Weech PK, Gelb MH.

Biochemistry. 1993 Jun 15;32(23):5935-40.

PMID:
8018213
25.

Interfacial catalysis and production of a high ratio of leukotriene A4 to 5-HPETE by 5-lipoxygenase in a coupled assay with phospholipase A2.

Riendeau D, Falgueyret JP, Meisner D, Sherman MM, Laliberté F, Street IP.

J Lipid Mediat. 1993 Mar-Apr;6(1-3):23-30.

PMID:
8395245
27.

Inhibition of enzymatic activity of phospholipases A2 by minocycline and doxycycline.

Pruzanski W, Greenwald RA, Street IP, Laliberte F, Stefanski E, Vadas P.

Biochem Pharmacol. 1992 Sep 25;44(6):1165-70.

PMID:
1417938
29.
30.

Fluorinated and deoxygenated substrates as probes of transition-state structure in glycogen phosphorylase.

Street IP, Rupitz K, Withers SG.

Biochemistry. 1989 Feb 21;28(4):1581-7.

PMID:
2719921
31.

2-Deoxy-2-fluoro-D-glycosyl fluorides. A new class of specific mechanism-based glycosidase inhibitors.

Withers SG, Rupitz K, Street IP.

J Biol Chem. 1988 Jun 15;263(17):7929-32.

32.

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