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Items: 1 to 20 of 228

1.

Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.

Vicik R, Hoerr V, Glaser M, Schultheis M, Hansell E, McKerrow JH, Holzgrabe U, Caffrey CR, Ponte-Sucre A, Moll H, Stich A, Schirmeister T.

Bioorg Med Chem Lett. 2006 May 15;16(10):2753-7. Epub 2006 Mar 3.

PMID:
16516467
2.

Design, synthesis and biological evaluation of potent azadipeptide nitrile inhibitors and activity-based probes as promising anti-Trypanosoma brucei agents.

Yang PY, Wang M, Li L, Wu H, He CY, Yao SQ.

Chemistry. 2012 May 21;18(21):6528-41. doi: 10.1002/chem.201103322. Epub 2012 Apr 4.

PMID:
22488888
3.

Improved trypanocidal activities of cathepsin L inhibitors.

Nkemgu NJ, Grande R, Hansell E, McKerrow JH, Caffrey CR, Steverding D.

Int J Antimicrob Agents. 2003 Aug;22(2):155-9.

PMID:
12927956
4.

Cysteine proteinase inhibitors kill cultured bloodstream forms of Trypanosoma brucei brucei.

Troeberg L, Morty RE, Pike RN, Lonsdale-Eccles JD, Palmer JT, McKerrow JH, Coetzer TH.

Exp Parasitol. 1999 Apr;91(4):349-55.

PMID:
10092479
5.

Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi.

Greenbaum DC, Mackey Z, Hansell E, Doyle P, Gut J, Caffrey CR, Lehrman J, Rosenthal PJ, McKerrow JH, Chibale K.

J Med Chem. 2004 Jun 3;47(12):3212-9.

PMID:
15163200
6.

Cysteine protease inhibitors as chemotherapy for parasitic infections.

McKerrow JH, Engel JC, Caffrey CR.

Bioorg Med Chem. 1999 Apr;7(4):639-44. Review.

PMID:
10353643
7.

A cathepsin B-like protease is required for host protein degradation in Trypanosoma brucei.

Mackey ZB, O'Brien TC, Greenbaum DC, Blank RB, McKerrow JH.

J Biol Chem. 2004 Nov 12;279(46):48426-33. Epub 2004 Aug 23.

8.

Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.

Waag T, Gelhaus C, Rath J, Stich A, Leippe M, Schirmeister T.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5541-3. doi: 10.1016/j.bmcl.2010.07.062. Epub 2010 Aug 6.

PMID:
20692829
9.

Identification of non-peptidic cysteine reactive fragments as inhibitors of cysteine protease rhodesain.

McShan D, Kathman S, Lowe B, Xu Z, Zhan J, Statsyuk A, Ogungbe IV.

Bioorg Med Chem Lett. 2015 Oct 15;25(20):4509-12. doi: 10.1016/j.bmcl.2015.08.074. Epub 2015 Sep 2.

10.

Evaluation of trypanocidal activity of combinations of anti-sleeping sickness drugs with cysteine protease inhibitors.

Steverding D.

Exp Parasitol. 2015 Apr-May;151-152:28-33. doi: 10.1016/j.exppara.2015.01.016. Epub 2015 Feb 4.

PMID:
25662707
11.

Antitrypanosomal and cysteine protease inhibitory activities of alkyldiamine cryptolepine derivatives.

Lavrado J, Mackey Z, Hansell E, McKerrow JH, Paulo A, Moreira R.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6256-60. doi: 10.1016/j.bmcl.2012.07.104. Epub 2012 Aug 15.

PMID:
22926067
12.

Chalcone, acyl hydrazide, and related amides kill cultured Trypanosoma brucei brucei.

Troeberg L, Chen X, Flaherty TM, Morty RE, Cheng M, Hua H, Springer C, McKerrow JH, Kenyon GL, Lonsdale-Eccles JD, Coetzer TH, Cohen FE.

Mol Med. 2000 Aug;6(8):660-9.

13.

The Inhibition of Cysteine Proteases Rhodesain and TbCatB: A Valuable Approach to Treat Human African Trypanosomiasis.

Ettari R, Previti S, Tamborini L, Cullia G, Grasso S, Zappalà M.

Mini Rev Med Chem. 2016;16(17):1374-1391. Review.

PMID:
27156518
14.

Active site mapping, biochemical properties and subcellular localization of rhodesain, the major cysteine protease of Trypanosoma brucei rhodesiense.

Caffrey CR, Hansell E, Lucas KD, Brinen LS, Alvarez Hernandez A, Cheng J, Gwaltney SL 2nd, Roush WR, Stierhof YD, Bogyo M, Steverding D, McKerrow JH.

Mol Biochem Parasitol. 2001 Nov;118(1):61-73.

PMID:
11704274
15.

Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.

Micale N, Ettari R, Schirmeister T, Evers A, Gelhaus C, Leippe M, Zappalà M, Grasso S.

Bioorg Med Chem. 2009 Sep 15;17(18):6505-11. doi: 10.1016/j.bmc.2009.08.013. Epub 2009 Aug 12.

PMID:
19709887
16.

Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids.

Breuning A, Degel B, Schulz F, Büchold C, Stempka M, Machon U, Heppner S, Gelhaus C, Leippe M, Leyh M, Kisker C, Rath J, Stich A, Gut J, Rosenthal PJ, Schmuck C, Schirmeister T.

J Med Chem. 2010 Mar 11;53(5):1951-63. doi: 10.1021/jm900946n.

PMID:
20131843
17.

Chemotherapeutic strategies against Trypanosoma brucei: drug targets vs. drug targeting.

Lüscher A, de Koning HP, Mäser P.

Curr Pharm Des. 2007;13(6):555-67. Review.

PMID:
17346174
18.

Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.

Du X, Guo C, Hansell E, Doyle PS, Caffrey CR, Holler TP, McKerrow JH, Cohen FE.

J Med Chem. 2002 Jun 20;45(13):2695-707.

PMID:
12061873
19.
20.

Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.

Mallari JP, Shelat A, Kosinski A, Caffrey CR, Connelly M, Zhu F, McKerrow JH, Guy RK.

Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. doi: 10.1016/j.bmcl.2008.03.083. Epub 2008 Apr 8.

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