SFGH MALARIA LABORATORY PUBLICATIONS

Subramanian S, Sijwali PS, Rosenthal PJ.  Falcipain cysteine proteases require bipartite motifs for trafficking to the Plasmodium falciparum food vacuole.  J Biol Chem. 2007 Jun 12; [Epub ahead of print]

Leon C, Rodrigues J, Gamboa de Dominguez N, Charris J, Gut J, Rosenthal PJ, Dominguez JN.  Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials. Eur J Med Chem. 2007 Jun;42(6):735-42. Epub 2007 Jan 14.

Singh A, Walker KJ, Sijwali PS, Lau AL, Rosenthal PJ.  A chimeric cysteine protease of Plasmodium berghei engineered to resemble the Plasmodium falciparum protease falcipain-2. Protein Eng Des Sel. 2007 Apr;20(4):171-7. Epub 2007 Apr 12.

Sijwali PS, Koo J, Singh N, Rosenthal PJ.  Gene disruptions demonstrate independent roles for the four falcipain cysteine proteases of Plasmodium falciparum.  Mol Biochem Parasitol. 2006 Nov;150(1):96-106. Epub 2006 Jul 20.

Pandey KC, Singh N, Arastu-Kapur S, Bogyo M, Rosenthal PJ.  Falstatin, a cysteine protease inhibitor of Plasmodium falciparum, facilitates erythrocyte invasion.  PLoS Pathog. 2006 Nov;2(11):e117.

Dahl EL, Shock JL, Shenai BR, Gut J, DeRisi JL, Rosenthal PJ.  Tetracyclines specifically target the apicoplast of the malaria parasite Plasmodium falciparum.  Antimicrob Agents Chemother. 2006 Sep;50(9):3124-31.

Wang SX, Pandey KC, Somoza JR, Sijwali PS, Kortemme T, Brinen LS, Fletterick RJ, Rosenthal PJ, McKerrow JH.  Structural basis for unique mechanisms of folding and hemoglobin binding by a malarial protease.  Proc Natl Acad Sci U S A. 2006 Aug 1;103(31):11503-8. Epub 2006 Jul 24.

Desai PV, Patny A, Gut J, Rosenthal PJ, Tekwani B, Srivastava A, Avery M.  Identification of novel parasitic cysteine protease inhibitors by use of virtual screening. 2. The available chemical directory.  J Med Chem. 2006 Mar 9;49(5):1576-84.

Dominguez JN, Leon C, Rodrigues J, Gamboa de Dominguez N, Gut J, Rosenthal PJ.  Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.  J Med Chem. 2005 May 19;48(10):3654-8.

Chiyanzu I, Clarkson C, Smith PJ, Lehman J, Gut J, Rosenthal PJ, Chibale K.  Design, synthesis and anti-plasmodial evaluation in vitro of new 4-aminoquinoline isatin derivatives.  Bioorg Med Chem. 2005 May 2;13(9):3249-61.

Fujii N, Mallari JP, Hansell EJ, Mackey Z, Doyle P, Zhou YM, Gut J, Rosenthal PJ, McKerrow JH, Guy RK.  Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain. Bioorg Med Chem Lett. 2005 Jan 3;15(1):121-3.

Desai PV, Patny A, Sabnis Y, Tekwani B, Gut J, Rosenthal P, Srivastava A, Avery M.  Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database.  J Med Chem. 2004 Dec 16;47(26):6609-15.

Rosenthal PJ.  Cysteine proteases of malaria parasites.  Int J Parasitol. 2004 Dec;34(13-14):1489-99. Review.

Na BK, Kim TS, Rosenthal PJ, Lee JK, Kong Y.  Evaluation of cysteine proteases of Plasmodium vivax as antimalarial drug targets: sequence analysis and sensitivity to cysteine protease inhibitors.  Parasitol Res. 2004 Oct;94(4):312-7. Epub 2004 Sep 15.

Go ML, Liu M, Wilairat P, Rosenthal PJ, Saliba KJ, Kirk K.  Antiplasmodial chalcones inhibit sorbitol-induced hemolysis of Plasmodium falciparum-infected erythrocytes.  Antimicrob Agents Chemother. 2004 Sep;48(9):3241-5.

Singh A, Rosenthal PJ.  Selection of cysteine protease inhibitor-resistant malaria parasites is accompanied by amplification of falcipain genes and alteration in inhibitor transport.  J Biol Chem. 2004 Aug 20;279(34):35236-41. Epub 2004 Jun 10.

Sijwali PS, Kato K, Seydel KB, Gut J, Lehman J, Klemba M, Goldberg DE, Miller LH, Rosenthal PJ.  Plasmodium falciparum cysteine protease falcipain-1 is not essential in erythrocytic stage malaria parasites.  Proc Natl Acad Sci U S A. 2004 Jun 8;101(23):8721-6. Epub 2004 May 27.

Fidock DA, Rosenthal PJ, Croft SL, Brun R, Nwaka S.  Antimalarial drug discovery: efficacy models for compound screening.  Nat Rev Drug Discov. 2004 Jun;3(6):509-20. Review.

Sijwali PS, Rosenthal PJ.  Gene disruption confirms a critical role for the cysteine protease falcipain-2 in hemoglobin hydrolysis by Plasmodium falciparum.  Proc Natl Acad Sci U S A. 2004 Mar 30;101(13):4384-9. Epub 2004 Mar 15.

Na BK, Shenai BR, Sijwali PS, Choe Y, Pandey KC, Singh A, Craik CS, Rosenthal PJ. Identification and biochemical characterization of vivapains, cysteine proteases of the malaria parasite Plasmodium vivax.  Biochem J. 2004 Mar 1;378(Pt 2):529-38.

Lee BJ, Singh A, Chiang P, Kemp SJ, Goldman EA, Weinhouse MI, Vlasuk GP, Rosenthal PJ.  Antimalarial activities of novel synthetic cysteine protease inhibitors.  Antimicrob Agents Chemother. 2003 Dec;47(12):3810-4.

Locher CP, Ruben PC, Gut J, Rosenthal PJ.  5HT1A serotonin receptor agonists inhibit Plasmodium falciparum by blocking a membrane channel.  Antimicrob Agents Chemother. 2003 Dec;47(12):3806-9.

Boyom FF, Ngouana V, Zollo PH, Menut C, Bessiere JM, Gut J, Rosenthal PJ.  Composition and anti-plasmodial activities of essential oils from some Cameroonian medicinal plants.  Phytochemistry. 2003 Dec;64(7):1269-75.

Rosenthal PJ.  Antimalarial drug discovery: old and new approaches.  J Exp Biol. 2003 Nov;206(Pt 21):3735-44. Review.

Sabnis YA, Desai PV, Rosenthal PJ, Avery MA.  Probing the structure of falcipain-3, a cysteine protease from Plasmodium falciparum: comparative protein modeling and docking studies.  Protein Sci. 2003 Mar;12(3):501-9.

Shenai BR, Lee BJ, Alvarez-Hernandez A, Chong PY, Emal CD, Neitz RJ, Roush WR, Rosenthal PJ.  Structure-activity relationships for inhibition of cysteine protease activity and development of Plasmodium falciparum by peptidyl vinyl sulfones.  Antimicrob Agents Chemother. 2003 Jan;47(1):154-60.

Singh A, Shenai BR, Choe Y, Gut J, Sijwali PS, Craik CS, Rosenthal PJ.  Critical role of amino acid 23 in mediating activity and specificity of vinckepain-2, a papain-family cysteine protease of rodent malaria parasites.  Biochem J. 2002 Nov 15;368(Pt 1):273-81.

Shenai BR, Semenov AV, Rosenthal PJ.  Stage-specific antimalarial activity of cysteine protease inhibitors.  Biol Chem. 2002 May;383(5):843-7.

Sijwali PS, Shenai BR, Rosenthal PJ.  Folding of the Plasmodium falciparum cysteine protease falcipain-2 is mediated by a chaperone-like peptide and not the prodomain.  J Biol Chem. 2002 Apr 26;277(17):14910-5. Epub 2002 Feb 4.

Sabnis Y, Rosenthal PJ, Desai P, Avery MA.  Homology modeling of falcipain-2: validation, de novo ligand design and synthesis of novel inhibitors.  J Biomol Struct Dyn. 2002 Apr;19(5):765-74.

Rosenthal PJ.  Hydrolysis of erythrocyte proteins by proteases of malaria parasites.  Curr Opin Hematol. 2002 Mar;9(2):140-5. Review.

Rosenthal PJ, Sijwali PS, Singh A, Shenai BR.  Cysteine proteases of malaria parasites: targets for chemotherapy.  Curr Pharm Des. 2002;8(18):1659-72. Review.

Sijwali PS, Shenai BR, Gut J, Singh A, Rosenthal PJ. Expression and characterization of the Plasmodium falciparum haemoglobinase falcipain-3.  Biochem J. 2001 Dec 1;360(Pt 2):481-9.

Joachimiak MP, Chang C, Rosenthal PJ, Cohen FE.  The impact of whole genome sequence data on drug discovery--a malaria case study.  Mol Med. 2001 Oct;7(10):698-710.

Dominguez JN, Charris JE, Lobo G, Gamboa de Dominguez N, Moreno MM, Riggione F, Sanchez E, Olson J, Rosenthal PJ.  Synthesis of quinolinyl chalcones and evaluation of their antimalarial activity.  Eur J Med Chem. 2001 Jun;36(6):555-60.

Rosenthal PJ.  Malaria in a Trinidadian man.  N Engl J Med. 2000 Oct 5;343(14):1047.

Shenai BR, Sijwali PS, Singh A, Rosenthal PJ.  Characterization of native and recombinant falcipain-2, a principal trophozoite cysteine protease and essential hemoglobinase of Plasmodium falciparum.  J Biol Chem. 2000 Sep 15;275(37):29000-10.

Olson JE, Lee GK, Semenov A, Rosenthal PJ.  Antimalarial effects in mice of orally administered peptidyl cysteine protease inhibitors.  Bioorg Med Chem. 1999 Apr;7(4):633-8.

Rosenthal PJ.  Proteases of protozoan parasites.  Adv Parasitol. 1999;43:105-59. Review.

Scheidt KA, Roush WR, McKerrow JH, Selzer PM, Hansell E, Rosenthal PJ.  Structure-based design, synthesis and evaluation of conformationally constrained cysteine protease inhibitors.  Bioorg Med Chem. 1998 Dec;6(12):2477-94.

Rosenthal PJ, Semenov A, Ploplis VA, Plow EF.  Plasminogen activators are not required in the erythrocytic life cycle of malaria parasites.  Mol Biochem Parasitol. 1998 Nov 30;97(1-2):253-7.

Lobel HO, Coyne PE, Rosenthal PJ.  Drug overdoses with antimalarial agents: prescribing and dispensing errors.  JAMA. 1998 Nov 4;280(17):1483.

Semenov A, Olson JE, Rosenthal PJ.  Antimalarial synergy of cysteine and aspartic protease inhibitors.  Antimicrob Agents Chemother. 1998 Sep;42(9):2254-8.

Gor DO, Rosenthal PJ.  Humoral immune responses of Africans to cysteine protease-related antigens of Plasmodium falciparum.  J Infect Dis. 1998 Jul;178(1):285-8.

Gor DO, Li AC, Rosenthal PJ.  Protective immune responses against protease-like antigens of the murine malaria parasite Plasmodium vinckei.  Vaccine. 1998 Jul;16(11-12):1193-202.

Rosenthal PJ.  Proteases of malaria parasites: new targets for chemotherapy.  Emerg Infect Dis. 1998 Jan-Mar;4(1):49-57. Review.

Rosenthal PJ, Meshnick SR.  Hemoglobin catabolism and iron utilization by malaria parasites.  Mol Biochem Parasitol. 1996 Dec 20;83(2):131-9. Review.

Rosenthal PJ, Petersen C, Geertsma FR, Kohl S.  Availability of intravenous quinidine for falciparum malaria.  N Engl J Med. 1996 Jul 11;335(2):138.

Rosenthal PJ, Olson JE, Lee GK, Palmer JT, Klaus JL, Rasnick D.  Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors.  Antimicrob Agents Chemother. 1996 Jul;40(7):1600-3.

Gamboa de Dominguez ND, Rosenthal PJ.  Cysteine proteinase inhibitors block early steps in hemoglobin degradation by cultured malaria parasites.  Blood. 1996 May 15;87(10):4448-54.

Salas F, Fichmann J, Lee GK, Scott MD, Rosenthal PJ.  Functional expression of falcipain, a Plasmodium falciparum cysteine proteinase, supports its role as a malarial hemoglobinase.  Infect Immun. 1995 Jun;63(6):2120-5.

Rosenthal PJ.  Plasmodium falciparum: effects of proteinase inhibitors on globin hydrolysis by cultured malaria parasites.  Exp Parasitol. 1995 Mar;80(2):272-81.

Li Z, Chen X, Davidson E, Zwang O, Mendis C, Ring CS, Roush WR, Fegley G, Li R, Rosenthal PJ, et al.  Anti-malarial drug development using models of enzyme structure.  Chem Biol. 1994 Sep;1(1):31-7.

Rosenthal PJ, Ring CS, Chen X, Cohen FE.  Characterization of a Plasmodium vivax cysteine proteinase gene identifies uniquely conserved amino acids that may mediate the substrate specificity of malarial hemoglobinases.  J Mol Biol. 1994 Aug 12;241(2):312-6.

Rosenthal PJ.  A Plasmodium vinckei cysteine proteinase shares unique features with its Plasmodium falciparum analogue.  Biochim Biophys Acta. 1993 Apr 29;1173(1):91-3.

Ring CS, Sun E, McKerrow JH, Lee GK, Rosenthal PJ, Kuntz ID, Cohen FE.  Structure-based inhibitor design by using protein models for the development of antiparasitic agents.  Proc Natl Acad Sci U S A. 1993 Apr 15;90(8):3583-7.

Rosenthal PJ, Lee GK, Smith RE.  Inhibition of a Plasmodium vinckei cysteine proteinase cures murine malaria.  J Clin Invest. 1993 Mar;91(3):1052-6.

McKerrow JH, Sun E, Rosenthal PJ, Bouvier J.  The proteases and pathogenicity of parasitic protozoa.  Annu Rev Microbiol. 1993;47:821-53. Review.

Rosenthal PJ, Wollish WS, Palmer JT, Rasnick D.  Antimalarial effects of peptide inhibitors of a Plasmodium falciparum cysteine proteinase.  J Clin Invest. 1991 Nov;88(5):1467-72.

Rosenthal PJ, McKerrow JH, Aikawa M, Nagasawa H, Leech JH.  A malarial cysteine proteinase is necessary for hemoglobin degradation by Plasmodium falciparum.  J Clin Invest. 1988 Nov;82(5):1560-6.

Rosenthal PJ, Kim K, McKerrow JH, Leech JH.  Identification of three stage-specific proteinases of Plasmodium falciparum.  J Exp Med. 1987 Sep 1;166(3):816-21.