Literature for peptidase C01.072: rhodesain
(Topics flags: S Structure, T Target, P Specificity, I Inhibitor, V Review. To select only the references relevant to a single topic, click the link above. See explanation.)
- Sheu-Idrees,R., Marques,G.V.L., Santana,P.A.L., Diniz,L.A., Resende,D.M., Odoma,S., Olorunshola,O., Ferreira,R.S., Murta,S.M.F., Maltarollo,V.G. and de Oliveira,R.B.<br>Investigation of the activity of 4-aminoquinolines as cysteine protease inhibitors with application in the treatment of Chagas disease<br>Mem Inst Oswaldo Cruz (2025) 120, e240161-e240161. PubMed Europe PubMed DOI PMC EPMC I
- Di Chio,C., Starvaggi,J., Totaro,N., Previti,S., Natale,B., Cosconati,S., Bogacz,M., Schirmeister,T., Legac,J., Rosenthal,P.J., Zappala,M. and Ettari,R.<br>Development of Novel Peptidyl Nitriles Targeting Rhodesain and Falcipain-2 for the Treatment of Sleeping Sickness and Malaria<br>Int J Mol Sci (2024) 25 PubMed Europe PubMed DOI PMC EPMC I
- Nunes,J.A., Santos-Junior,P.F.D.S., Gomes,M.C., Ferreira,L.A.S., Padilha,E.K.A., Teixeira,T.R., Stanger,E.J., Kaur,Y., Silva,E.B.D., Costa,C.A.C.B., Freitas,J.D., Araujo-Junior,J.X., Mendonca-Junior,F.J.B., Giardini,M.A., Siqueira-Neto,J.L., Caffrey,C.R., Zhan,P., Cardoso,S.H. and Silva-Junior,E.F.D.<br>Nanomolar activity of coumarin-3-thiosemicarbazones targeting Trypanosoma cruzi cruzain and the T. brucei cathepsin L-like protease<br>Eur J Med Chem (2024) 283, 117109-117109. PubMed Europe PubMed DOI I
- Ettari,R.<br>Cysteine Proteases as Validated Targets for the Treatment of Neglected and Poverty-Related Parasitic Diseases<br>Int J Mol Sci (2023) 24 PubMed Europe PubMed DOI PMC EPMC
- Di Chio,C., Previti,S., Amendola,G., Ravichandran,R., Wagner,A., Cosconati,S., Hellmich,U.A., Schirmeister,T., Zappala,M. and Ettari,R.<br>Development of novel dipeptide nitriles as inhibitors of rhodesain of Trypanosoma brucei rhodesiense<br>Eur J Med Chem (2022) 236, 114328-114328. PubMed Europe PubMed DOI
- Elrufaie,H.A., Mohamed,L.M., Hamd,A.Y., Bala,N.A., Elbadawi,F.A., Ghaboosh,H. and Alzain,A.A.<br>Discovery of novel natural products as rhodesain inhibitors for human African trypanosomiasis using in silico techniques<br>J Biomol Struct Dyn (2022) , 1-13. PubMed Europe PubMed DOI
- Arafet,K., Gonzalez,F.V. and Moliner,V.<br>Elucidating the dual mode of action of dipeptidyl enoates in the inhibition of rhodesain cysteine proteases<br>Chemistry (2021) PubMed Europe PubMed DOI
- Barbosa da Silva,E., Rocha,D.A., Fortes,I.S., Yang,W., Monti,L., Siqueira-Neto,J.L., Caffrey,C.R., McKerrow,J., Andrade,S.F. and Ferreira,R.S.<br>Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors<br>J Med Chem (2021) 64, 13054-13071. PubMed Europe PubMed DOI I
- Di Chio,C., Previti,S., De Luca,F., Allegra,A., Zappala,M. and Ettari,R.<br>Drug combination studies of PS-1 and quercetin against rhodesain of Trypanosoma brucei rhodesiense<br>Nat Prod Res (2021) , 1-5. PubMed Europe PubMed DOI I
- Johe,P., Jaenicke,E., Neuweiler,H., Schirmeister,T., Kersten,C. and Hellmich,U.A.<br>Structure, interdomain dynamics and pH-dependent autoactivation of pro-rhodesain, the main lysosomal cysteine protease from African trypanosomes<br>J Biol Chem (2021) , 100565-100565. PubMed Europe PubMed DOI
- Johe,P., Jung,S., Endres,E., Kersten,C., Zimmer,C., Ye,W., Sonnichsen,C., Hellmich,U.A., Sotriffer,C., Schirmeister,T. and Neuweiler,H.<br>Warhead Reactivity Limits the Speed of Inhibition of the Cysteine Protease Rhodesain<br>ACS Chem Biol (2021) 16, 661-670. PubMed Europe PubMed DOI
- Nakamura,Y., Hayashida,K., Delesalle,V., Qiu,Y., Omori,R., Simuunza,M., Sugimoto,C., Namangala,B. and Yamagishi,J.<br>Genetic Diversity of African Trypanosomes in Tsetse Flies and Cattle From the Kafue Ecosystem<br>Front Vet Sci (2021) 8, 599815-599815. PubMed Europe PubMed DOI PMC EPMC
- Santos Nascimento,I.J.D., de Aquino,T.M. and da Silva-Junior,E.F.<br>Cruzain and Rhodesain Inhibitors: Last Decade of Advances in Seeking for New Compounds Against American and African Trypanosomiases<br>Curr Top Med Chem (2021) PubMed Europe PubMed DOI V
- Alvarez,V.E., Iribarren,P.A., Niemirowicz,G.T. and Cazzulo,J.J.<br>Update on relevant trypanosome peptidases: Validated targets and future challenges<br>Biochim Biophys Acta Proteins Proteom (2020) 1869, 140577-140577. PubMed Europe PubMed DOI
- Arafet,K., Gonzalez,F.V. and Moliner,V.<br>Quantum mechanics/molecular mechanics studies of the mechanism of cysteine proteases inhibition by dipeptidyl nitroalkenes<br>Chemistry (2020) 26, 2002-2012. PubMed Europe PubMed DOI I
- da Costa,C.H.S., Bonatto,V., Dos Santos,A.M., Lameira,J., Leitao,A. and Montanari,C.A.<br>Evaluating QM/MM free energy surfaces for ranking cysteine protease covalent inhibitors<br>J Chem Inf Model (2020) 60, 880-889. PubMed Europe PubMed DOI I
- Di Chio,C., Previti,S., Amendola,G., Cosconati,S., Schirmeister,T., Zappala,M. and Ettari,R.<br>Development of novel benzodiazepine-based peptidomimetics as inhibitors of rhodesain from Trypanosoma brucei rhodesiense<br>ChemMedChem (2020) 15, 995-1001. PubMed Europe PubMed DOI I
- Ettari,R., Previti,S., Di Chio,C., Maiorana,S., Allegra,A., Schirmeister,T. and Zappala,M.<br>Drug synergism: studies of combination of RK-52 and curcumin against rhodesain of Trypanosoma brucei rhodesiense<br>ACS Med Chem Lett (2020) 11, 806-810. PubMed Europe PubMed DOI PMC EPMC I
- Klein,P., Johe,P., Wagner,A., Jung,S., Kuhlborn,J., Barthels,F., Tenzer,S., Distler,U., Waigel,W., Engels,B., Hellmich,U.A., Opatz,T. and Schirmeister,T.<br>New cysteine protease inhibitors: electrophilic (het)arenes and unexpected prodrug identification for the Trypanosoma protease rhodesain<br>Molecules (2020) 25 PubMed Europe PubMed DOI I
- Klein,P., Barthels,F., Johe,P., Wagner,A., Tenzer,S., Distler,U., Le,T.A., Schmid,P., Engel,V., Engels,B., Hellmich,U.A., Opatz,T. and Schirmeister,T.<br>Naphthoquinones as covalent reversible inhibitors of cysteine proteases: studies on inhibition mechanism and kineticsNaphthoquinones as Covalent Reversible Inhibitors of Cysteine Proteases: Studies on Inhibition Mechanism and Kinetics<br>Molecules (2020) 25 PubMed Europe PubMed DOI I
- Cianni,L., Feldmann,C.W., Gilberg,E., Gutschow,M., Juliano,L., Leitao,A., Bajorath,J. and Montanari,C.A.<br>Can cysteine protease cross-class inhibitors achieve selectivity?<br>J Med Chem (2019) 62, 10497-10525. PubMed Europe PubMed DOI I
- Ettari,R., Previti,S., Maiorana,S., Allegra,A., Schirmeister,T., Grasso,S. and Zappala,M.<br>Drug combination studies of curcumin and genistein against rhodesain of Trypanosoma brucei rhodesiense<br>Nat Prod Res (2019) 33, 3577-3581. PubMed Europe PubMed DOI I
- Santos,L.H., Waldner,B.J., Fuchs,J.E., Pereira,G.A.N., Liedl,K.R., Caffarena,E.R. and Ferreira,R.S.<br>Understanding structure-activity relationships for trypanosomal cysteine protease inhibitors by simulations and free energy calculations<br>J Chem Inf Model (2019) 59, 137-148. PubMed Europe PubMed DOI I
- Steverding,D.<br>On the reversible and irreversible inhibition of rhodesain by curcumin<br>Molecules (2019) 25 PubMed Europe PubMed DOI I
- Eyssen,L.E., Vather,P., Jackson,L., Ximba,P., Biteau,N., Baltz,T., Boulange,A., Buscher,P. and Coetzer,T.H.T.<br>Recombinant and native TviCATL from Trypanosoma vivax: enzymatic characterisation and evaluation as a diagnostic target for animal African trypanosomosis<br>Mol Biochem Parasitol (2018) 223, 50-54. PubMed Europe PubMed DOI
- Giroud,M., Kuhn,B., Saint-Auret,S., Kuratli,C., Martin,R.E., Schuler,F., Diederich,F., Kaiser,M., Brun,R., Schirmeister,T. and Haap,W.<br>2 H-1,2,3-Triazole-based dipeptidyl nitriles: potent, selective, and trypanocidal rhodesain inhibitors by structure-based design<br>J Med Chem (2018) 61, 3370-3388. PubMed Europe PubMed DOI I
- Giroud,M., Dietzel,U., Anselm,L., Banner,D., Kuglstatter,A., Benz,J., Blanc,J.B., Gaufreteau,D., Liu,H., Lin,X., Stich,A., Kuhn,B., Schuler,F., Kaiser,M., Brun,R., Schirmeister,T., Kisker,C., Diederich,F. and Haap,W.<br>Repurposing a library of human cathepsin L ligands: identification of macrocyclic lactams as potent rhodesain and Trypanosoma brucei inhibitors<br>J Med Chem (2018) 61, 3350-3369. PubMed Europe PubMed DOI S I
- Macedo Koeller,C. and Bangs,J.D.<br>Processing and targeting of cathepsin L (TbCatL) to the lysosome in Trypanosoma brucei<br>Cell Microbiol (2018) , e12980-e12980. PubMed Europe PubMed DOI
- Rocha,D.A., Silva,E.B., Fortes,I.S., Lopes,M.S., Ferreira,R.S. and Andrade,S.F.<br>Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors<br>Eur J Med Chem (2018) 157, 1426-1459. PubMed Europe PubMed DOI I
- Royo,S., Schirmeister,T., Kaiser,M., Jung,S., Rodriguez,S., Bautista,J.M. and Gonzalez,F.V.<br>Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates<br>Bioorg Med Chem (2018) 26, 4624-4634. PubMed Europe PubMed DOI I
- Ferreira,L.G. and Andricopulo,A.D.<br>Targeting cysteine proteases in trypanosomatid disease drug discovery<br>Pharmacol Ther (2017) 180, 49-61. PubMed Europe PubMed DOI T
- Giroud,M., Ivkovic,J., Martignoni,M., Fleuti,M., Trapp,N., Haap,W., Kuglstatter,A., Benz,J., Kuhn,B., Schirmeister,T. and Diederich,F.<br>Inhibition of the cysteine protease human cathepsin L by triazine nitriles: amide???heteroarene pi-stacking interactions and chalcogen bonding in the S3 pocket<br>ChemMedChem (2017) 12, 257-270. PubMed Europe PubMed DOI I
- Previti,S., Ettari,R., Cosconati,S., Amendola,G., Chouchene,K., Wagner,A., Hellmich,U.A., Ulrich,K., Krauth-Siegel,R.L., Wich,P.R., Schmid,I., Schirmeister,T., Gut,J., Rosenthal,P.J., Grasso,S. and Zappala,M.<br>Development of novel peptide-based Michael acceptors targeting rhodesain and falcipain-2 for the treatment of neglected tropical diseases (NTDs)<br>J Med Chem (2017) 60, 6911-6923. PubMed Europe PubMed DOI I
- Schirmeister,T., Schmitz,J., Jung,S., Schmenger,T., Krauth-Siegel,R.L. and Gutschow,M.<br>Evaluation of dipeptide nitriles as inhibitors of rhodesain, a major cysteine protease of Trypanosoma brucei<br>Bioorg Med Chem Lett (2017) 27, 45-50. PubMed Europe PubMed DOI I
- Ettari,R., Previti,S., Cosconati,S., Kesselring,J., Schirmeister,T., Grasso,S. and Zappala,M.<br>Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors<br>J Enzyme Inhib Med Chem (2016) 31, 1184-1191. PubMed Europe PubMed DOI I
- Ettari,R., Previti,S., Tamborini,L., Cullia,G., Grasso,S. and Zappala,M.<br>The inhibition of cysteine proteases rhodesain and TbCatB: a valuable approach to treat human African trypanosomiasis<br>Mini Rev Med Chem (2016) 16, 1374-1391. PubMed Europe PubMed DOI V I
- Latorre,A., Schirmeister,T., Kesselring,J., Jung,S., Johe,P., Hellmich,U.A., Heilos,A., Engels,B., Krauth-Siegel,R.L., Dirdjaja,N., Bou-Iserte,L., Rodriguez,S. and Gonzalez,F.V.<br>Dipeptidyl nitroalkenes as potent reversible inhibitors of cysteine proteases rhodesain and cruzain<br>ACS Med Chem Lett (2016) 7, 1073-1076. PubMed Europe PubMed DOI PMC EPMC I
- Ettari,R., Pinto,A., Previti,S., Tamborini,L., Angelo,I.C., La Pietra,V., Marinelli,L., Novellino,E., Schirmeister,T., Zappala,M., Grasso,S., De Micheli,C. and Conti,P.<br>Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation<br>Bioorg Med Chem (2015) 23, 7053-7060. PubMed Europe PubMed DOI I
- Fonseca,N.C., da Cruz,L.F., da Silva Villela,F., do Nascimento Pereira,G.A., de Siqueira-Neto,J.L., Kellar,D., Suzuki,B.M., Ray,D., de Souza,T.B., Alves,R.J., Junior,P.A., Romanha,A.J., Murta,S.M., McKerrow,J.H., Caffrey,C.R., de Oliveira,R.B. and Ferreira,R.S.<br>Synthesis of a sugar-based thiosemicarbazone series and structure-activity relationship versus the parasite cysteine proteases rhodesain, cruzain, and Schistosoma mansoni cathepsin B1<br>Antimicrob Agents Chemother (2015) 59, 2666-2677. PubMed Europe PubMed DOI I
- McShan,D., Kathman,S., Lowe,B., Xu,Z., Zhan,J., Statsyuk,A. and Ogungbe,I.V.<br>Identification of non-peptidic cysteine reactive fragments as inhibitors of cysteine protease rhodesain<br>Bioorg Med Chem Lett (2015) 25, 4509-4512. PubMed Europe PubMed DOI I
- Royo,S., Rodriguez,S., Schirmeister,T., Kesselring,J., Kaiser,M. and Gonzalez,F.V.<br>Dipeptidyl enoates as potent rhodesain inhibitors that display a dual mode of action<br>ChemMedChem (2015) 10, 1484-1487. PubMed Europe PubMed DOI I
- Alsford,S., Currier,R.B., Guerra-Assuncao,J.A., Clark,T.G. and Horn,D.<br>Cathepsin-L can resist lysis by human serum in Trypanosoma brucei brucei<br>PLoS Pathog (2014) 10, e1004130-e1004130. PubMed Europe PubMed DOI PMC EPMC
- Ettari,R., Pinto,A., Tamborini,L., Angelo,I.C., Grasso,S., Zappala,M., Capodicasa,N., Yzeiraj,L., Gruber,E., Aminake,M.N., Pradel,G., Schirmeister,T., De Micheli,C. and Conti,P.<br>Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antiprotozoal agents<br>ChemMedChem (2014) 9, 1817-1825. PubMed Europe PubMed DOI I
- Ehmke,V., Winkler,E., Banner,D.W., Haap,W., Schweizer,W.B., Rottmann,M., Kaiser,M., Freymond,C., Schirmeister,T. and Diederich,F.<br>Optimization of triazine nitriles as rhodesain inhibitors: structure-activity relationships, bioisosteric imidazopyridine nitriles, and X-ray crystal structure analysis with human cathepsin L<br>ChemMedChem (2013) 8, 967-975. PubMed Europe PubMed DOI I
- Elliott,E.B., McCarroll,D., Hasumi,H., Welsh,C.E., Panissidi,A.A., Jones,N.G., Rossor,C.L., Tait,A., Smith,G.L., Mottram,J.C., Morrison,L.J. and Loughrey,C.M.<br>Trypanosoma brucei cathepsin-L increases arrhythmogenic sarcoplasmic reticulum-mediated calcium release in rat cardiomyocytes<br>Cardiovasc Res (2013) 100, 325-335. PubMed Europe PubMed DOI
- Ettari,R., Tamborini,L., Angelo,I.C., Grasso,S., Schirmeister,T., Lo Presti,L., De Micheli,C., Pinto,A. and Conti,P.<br>Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead<br>ChemMedChem (2013) 8, 2070-2076. PubMed Europe PubMed DOI I
- Ettari,R., Tamborini,L., Angelo,I.C., Micale,N., Pinto,A., De Micheli,C. and Conti,P.<br>Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis<br>J Med Chem (2013) 56, 5637-5658. PubMed Europe PubMed DOI I
- Costa,T.F., Reis,F.C. and Lima,A.P.<br>Substrate inhibition and allosteric regulation by heparan sulfate of Trypanosoma brucei cathepsin L<br>Biochim Biophys Acta (2012) 1824, 493-501. PubMed Europe PubMed DOI
- Ehmke,V., Quinsaat,J.E., Rivera-Fuentes,P., Heindl,C., Freymond,C., Rottmann,M., Brun,R., Schirmeister,T. and Diederich,F.<br>Tuning and predicting biological affinity: aryl nitriles as cysteine protease inhibitors<br>Org Biomol Chem (2012) 10, 5764-5768. PubMed Europe PubMed DOI I
- Steverding,D., Sexton,D.W., Wang,X., Gehrke,S.S., Wagner,G.K. and Caffrey,C.R.<br>Trypanosoma brucei: chemical evidence that cathepsin L is essential for survival and a relevant drug target<br>Int J Parasitol (2012) 42, 481-488. PubMed Europe PubMed DOI I
- Yang,P.Y., Wang,M., Li,L., Wu,H., He,C.Y. and Yao,S.Q.<br>Design, synthesis and biological evaluation of potent azadipeptide nitrile inhibitors and activity-based probes as promising anti-Trypanosoma brucei agents<br>Chemistry (2012) 18, 6528-6541. PubMed Europe PubMed DOI I
- Caffrey,C.R., Lima,A.P. and Steverding,D.<br>Cysteine peptidases of kinetoplastid parasites<br>Adv Exp Med Biol (2011) 712, 84-99. PubMed Europe PubMed DOI V
- Ehmke,V., Heindl,C., Rottmann,M., Freymond,C., Schweizer,W.B., Brun,R., Stich,A., Schirmeister,T. and Diederich,F.<br>Potent and selective inhibition of cysteine proteases from Plasmodium falciparum and Trypanosoma brucei<br>ChemMedChem (2011) 6, 273-278. PubMed Europe PubMed DOI I
- Breuning,A., Degel,B., Schulz,F., Buchold,C., Stempka,M., Machon,U., Heppner,S., Gelhaus,C., Leippe,M., Leyh,M., Kisker,C., Rath,J., Stich,A., Gut,J., Rosenthal,P.J., Schmuck,C. and Schirmeister,T.<br>Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids<br>J Med Chem (2010) 53, 1951-1963. PubMed Europe PubMed DOI I
- Ettari,R., Zappala,M., Micale,N., Schirmeister,T., Gelhaus,C., Leippe,M., Evers,A. and Grasso,S.<br>Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain<br>Eur J Med Chem (2010) 45, 3228-3233. PubMed Europe PubMed DOI I
- Kerr,I.D., Wu,P., Marion-Tsukamaki,R., Mackey,Z.B. and Brinen,L.S.<br>Crystal structures of TbCatB and rhodesain, potential chemotherapeutic targets and major cysteine proteases of Trypanosoma brucei<br>PLoS Negl Trop Dis (2010) 4, e701-e701. PubMed Europe PubMed DOI PMC EPMC S
- Mott,B.T., Ferreira,R.S., Simeonov,A., Jadhav,A., Ang,K.K., Leister,W., Shen,M., Silveira,J.T., Doyle,P.S., Arkin,M.R., McKerrow,J.H., Inglese,J., Austin,C.P., Thomas,C.J., Shoichet,B.K. and Maloney,D.J.<br>Identification and optimization of inhibitors of trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB<br>J Med Chem (2010) 53, 52-60. PubMed Europe PubMed DOI S I
- Waag,T., Gelhaus,C., Rath,J., Stich,A., Leippe,M. and Schirmeister,T.<br>Allicin and derivates are cysteine protease inhibitors with antiparasitic activity<br>Bioorg Med Chem Lett (2010) 20, 5541-5543. PubMed Europe PubMed DOI I
- Caffrey,C.R. and Steverding,D.<br>Kinetoplastid papain-like cysteine peptidases<br>Mol Biochem Parasitol (2009) 167, 12-19. PubMed Europe PubMed DOI I
- Cortez,A.P., Rodrigues,A.C., Garcia,H.A., Neves,L., Batista,J.S., Bengaly,Z., Paiva,F. and Teixeira,M.M.<br>Cathepsin L-like genes of Trypanosoma vivax from Africa and South America - characterization, relationships and diagnostic implications<br>Mol Cell Probes (2009) 23, 44-51. PubMed Europe PubMed DOI
- Kerr,I.D., Lee,J.H., Farady,C.J., Marion,R., Rickert,M., Sajid,M., Pandey,K.C., Caffrey,C.R., Legac,J., Hansell,E., McKerrow,J.H., Craik,C.S., Rosenthal,P.J. and Brinen,L.S.<br>Vinyl sulfones as antiparasitic agents and a structural basis for drug design<br>J Biol Chem (2009) 284, 25697-25703. PubMed Europe PubMed DOI PMC EPMC S I
- Steverding,D., Wang,X. and Sexton,D.W.<br>The trypanocidal effect of NO-releasing agents is not due to inhibition of the major cysteine proteinase in Trypanosoma brucei<br>Parasitol Res (2009) 105, 1333-1338. PubMed Europe PubMed DOI
- Abdulla,M.H., O'Brien,T., Mackey,Z.B., Sajid,M., Grab,D.J. and McKerrow,J.H.<br>RNA interference of Trypanosoma brucei cathepsin B and L affects disease progression in a mouse model<br>PLoS Negl Trop Dis (2008) 2, e298-e298. PubMed Europe PubMed DOI PMC EPMC
- Jaishankar,P., Hansell,E., Zhao,D.M., Doyle,P.S., McKerrow,J.H. and Renslo,A.R.<br>Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes<br>Bioorg Med Chem Lett (2008) 18, 624-628. PubMed Europe PubMed DOI I
- Mallari,J.P., Shelat,A., Kosinski,A., Caffrey,C.R., Connelly,M., Zhu,F., McKerrow,J.H. and Guy,R.K.<br>Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB<br>Bioorg Med Chem Lett (2008) 18, 2883-2885. PubMed Europe PubMed DOI PMC EPMC I
- Gonzalez,F.V., Izquierdo,J., Rodriguez,S., McKerrow,J.H. and Hansell,E.<br>Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain<br>Bioorg Med Chem Lett (2007) 17, 6697-6700. PubMed Europe PubMed DOI I
- Reis,F.C., Costa,T.F., Sulea,T., Mezzetti,A., Scharfstein,J., Bromme,D., Menard,R. and Lima,A.P.<br>The propeptide of cruzipain - a potent selective inhibitor of the trypanosomal enzymes cruzipain and brucipain, and of the human enzyme cathepsin F<br>FEBS J (2007) 274, 1224-1234. PubMed Europe PubMed DOI
- [YEAR:6-3-2006]Choe,Y., Leonetti,F., Greenbaum,D.C., Lecaille,F., Bogyo,M., Bromme,D., Ellman,J.A. and Craik,C.S.<br>Substrate profiling of cysteine proteases using a combinatorial peptide library identifies functionally unique specificities<br>J Biol Chem (6-3-2006) 281, 12824-12832. PubMed Europe PubMed DOI P
- [YEAR:2-10-2006]Nikolskaia,O.V., de,A.L., Kim,Y.V., Lonsdale-Eccles,J.D., Fukuma,T., Scharfstein,J. and Grab,D.J.<br>Blood-brain barrier traversal by African trypanosomes requires calcium signaling induced by parasite cysteine protease<br>J Clin Invest (2-10-2006) 116, 2739-2747. PubMed Europe PubMed DOI I
- [YEAR:1-3-2006]Vicik,R., Hoerr,V., Glaser,M., Schultheis,M., Hansell,E., McKerrow,J.H., Holzgrabe,U., Caffrey,C.R., Ponte-Sucre,A., Moll,H., Stich,A. and Schirmeister,T.<br>Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents<br>Bioorg Med Chem Lett (1-3-2006) 16, 2753-2757. PubMed Europe PubMed DOI I
- [YEAR:3-1-2005]Fujii,N., Mallari,J.P., Hansell,E.J., Mackey,Z., Doyle,P., Zhou,Y.M., Gut,J., Rosenthal,P.J., McKerrow,J.H. and Guy,R.K.<br>Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain<br>Bioorg Med Chem Lett (3-1-2005) 15, 121-123. PubMed Europe PubMed DOI I
- [YEAR:10-2-2005]Gosalia,D.N., Salisbury,C.M., Ellman,J.A. and Diamond,S.L.<br>High throughput substrate specificity profiling of serine and cysteine proteases using solution-phase fluorogenic peptide microarrays<br>Mol Cell Proteomics (10-2-2005) 4, 626-636. PubMed Europe PubMed DOI
- [YEAR:20-10-2003]Chiyanzu,I., Hansell,E., Gut,J., Rosenthal,P.J., McKerrow,J.H. and Chibale,K.<br>Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain<br>Bioorg Med Chem Lett (20-10-2003) 13, 3527-3530. PubMed Europe PubMed DOI I
- Caffrey,C.R., Hansell,E., Lucas,K.D., Brinen,L.S., Hernandez,A.A., Cheng,J.N., Gwaltney,S.L., II, Roush,W.R., Stierhof,Y.D., Bogyo,M., Steverding,D. and McKerrow,J.H.<br>Active site mapping, biochemical properties and subcellular localization of rhodesain, the major cysteine protease of Trypanosoma brucei rhodesiense<br>Mol Biochem Parasitol (2001) 118, 61-73. PubMed Europe PubMed DOI
- Scory,S., Caffrey,C.R., Stierhof,Y.D., Ruppel,A. and Steverding,D.<br>Trypanosoma brucei: killing of bloodstream forms in vitro and in vivo by the cysteine proteinase inhibitor Z-Phe-Ala-CHN2<br>Exp Parasitol (1999) 91, 327-333. PubMed Europe PubMed DOI I
- Troeberg,L., Morty,R.E., Pike,R.N., Lonsdale-Eccles,J.D., Palmer,J.T., McKerrow,J.H. and Coetzer,T.H.<br>Cysteine proteinase inhibitors kill cultured bloodstream forms of Trypanosoma brucei brucei<br>Exp Parasitol (1999) 91, 349-355. PubMed Europe PubMed DOI I
- Pamer,E.G., Davis,C.E. and So,M.<br>Expression and deletion analysis of the Trypanosoma brucei rhodesiense cysteine protease in Escherichia coli<br>Infect Immun (1991) 59, 1074-1078. PubMed Europe PubMed PMC EPMC
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