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Publikationer i urvalet

31 träffar

Bibliografisk träff 2024-06-04

Structural Modifications of Covalent Cathepsin S Inhibitors: Impact on Affinity, Selectivity, and Permeability.

Meta M, Zimmer C, Fuchs N, Zecher MJ, Lahu A, Schirmeister T.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.4c00050

Bibliografisk träff 2023-03-01

Antitarget, Anti-SARS-CoV-2 Leads, Drugs, and the Drug Discovery-Genetics Alliance Perspective.

Pozzi C, Vanet A, Francesconi V, Tagliazucchi L, Tassone G, Venturelli A, Spyrakis F, Mazzorana M, Costi MP, Tonelli M.

J Med Chem · review-article; review; journal article · DOI 10.1021/acs.jmedchem.2c01229

Bibliografisk träff 2022-06-30

Development of Urea-Bond-Containing Michael Acceptors as Antitrypanosomal Agents Targeting Rhodesain.

Previti S, Ettari R, Calcaterra E, Di Chio C, Ravichandran R, Zimmer C, Hammerschmidt S, Wagner A, Bogacz M, Cosconati S, Schirmeister T, Zappalà M.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.2c00084

Bibliografisk träff 2022-05-14

New peptidomimetic rhodesain inhibitors with improved selectivity towards human cathepsins.

Jung S, Fuchs N, Grathwol C, Hellmich UA, Wagner A, Diehl E, Willmes T, Sotriffer C, Schirmeister T.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114460

Bibliografisk träff 2022-03-08

Recent applications of vinyl sulfone motif in drug design and discovery.

Ahmadi R, Emami S.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114255

Bibliografisk träff 2021-08-11

Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and In Vivo Studies.

Jung S, Fuchs N, Johe P, Wagner A, Diehl E, Yuliani T, Zimmer C, Barthels F, Zimmermann RA, Klein P, Waigel W, Meyr J, Opatz T, Tenzer S, Distler U, Räder HJ, Kersten C, Engels B, Hellmich UA, Klein J, Schirmeister T.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c01002

Bibliografisk träff 2021-07-21

Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.

Li L, Chenna BC, Yang KS, Cole TR, Goodall ZT, Giardini M, Moghadamchargari Z, Hernandez EA, Gomez J, Calvet CM, Bernatchez JA, Bernatchez JA, Mellott DM, Zhu J, Rademacher A, Thomas D, Blankenship LR, Drelich A, Laganowsky A, Tseng CK, Liu WR, Wand AJ, Cruz-Reyes J, Siqueira-Neto JL, Meek TD.

J Med Chem · research-article; journal article · DOI 10.1021/acs.jmedchem.1c00628

Bibliografisk träff 2021-01-12

The race to treat COVID-19: Potential therapeutic agents for the prevention and treatment of SARS-CoV-2.

Shagufta, Ahmad I.

Eur J Med Chem · review-article; review; journal article · DOI 10.1016/j.ejmech.2021.113157

Bibliografisk träff 2020-09-11

Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).

Choudhry N, Zhao X, Xu D, Zanin M, Chen W, Yang Z, Chen J.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.0c00626

Bibliografisk träff 2020-06-26

COVID-19: Drug Targets and Potential Treatments.

Gil C, Ginex T, Maestro I, Nozal V, Barrado-Gil L, Cuesta-Geijo MÁ, Urquiza J, Ramírez D, Alonso C, Campillo NE, Martinez A.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.0c00606

Bibliografisk träff 2020-06-25

Inhibitors of SARS-CoV-2 Entry: Current and Future Opportunities.

Xiu S, Dick A, Ju H, Mirzaie S, Abdi F, Cocklin S, Zhan P, Liu X.

J Med Chem · research support, non-u.s. gov't; research-article; review; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.0c00502

Bibliografisk träff 2020-03-17

Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.

Chenna BC, Li L, Mellott DM, Zhai X, Siqueira-Neto JL, Calvet Alvarez C, Bernatchez JA, Bernatchez JA, Desormeaux E, Alvarez Hernandez E, Gomez J, McKerrow JH, Cruz-Reyes J, Meek TD.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.9b02078

Bibliografisk träff 2019-08-15

Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?

Cianni L, Feldmann CW, Gilberg E, Gütschow M, Juliano L, Leitão A, Bajorath J, Montanari CA.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.9b00683

Bibliografisk träff 2019-05-13

Highly tunable thiosulfonates as a novel class of cysteine protease inhibitors with anti-parasitic activity against Schistosoma mansoni.

Ward DJ, Van de Langemheen H, Koehne E, Kreidenweiss A, Liskamp RMJ.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2019.05.014

Bibliografisk träff 2018-08-31

Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors.

Rocha DA, Silva EB, Fortes IS, Lopes MS, Ferreira RS, Andrade SF.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2018.08.079

Bibliografisk träff 2017-07-01

Bistacrines as potential antitrypanosomal agents.

Schmidt I, Göllner S, Fuß A, Stich A, Kucharski A, Schirmeister T, Katzowitsch E, Bruhn H, Miliu A, Krauth-Siegel RL, Holzgrabe U.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2017.06.051

Bibliografisk träff 2016-09-21

Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.

Latorre A, Schirmeister T, Kesselring J, Jung S, Johé P, Hellmich UA, Heilos A, Engels B, Krauth-Siegel RL, Dirdjaja N, Bou-Iserte L, Rodríguez S, González FV.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.6b00276

Bibliografisk träff 2015-12-15

Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain.

Jones BD, Tochowicz A, Tang Y, Cameron MD, McCall LI, Hirata K, Siqueira-Neto JL, Reed SL, McKerrow JH, Roush WR.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.5b00336

Bibliografisk träff 2014-11-25

Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.

Vieira DF, Choi JY, Calvet CM, Siqueira-Neto JL, Johnston JB, Kellar D, Gut J, Cameron MD, McKerrow JH, Roush WR, Podust LM.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/jm501568b

Bibliografisk träff 2013-09-03

Vinyl sulfone-based peptidomimetics as anti-trypanosomal agents: design, synthesis, biological and computational evaluation.

Dunny E, Doherty W, Evans P, Malthouse JP, Nolan D, Knox AJ.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm400294w

Bibliografisk träff 2013-05-07

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.

Ettari R, Tamborini L, Angelo IC, Micale N, Pinto A, De Micheli C, Conti P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm301424d

Bibliografisk träff 2010-06-14

Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.

Engel JC, Ang KK, Chen S, Arkin MR, McKerrow JH, Doyle PS.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; evaluation study; journal article; research support, n.i.h., extramural · DOI 10.1128/aac.01777-09

Bibliografisk träff 2010-04-12

A nonazole CYP51 inhibitor cures Chagas' disease in a mouse model of acute infection.

Doyle PS, Chen CK, Johnston JB, Hopkins SD, Leung SS, Jacobson MP, Engel JC, McKerrow JH, Podust LM.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1128/aac.00281-10

Bibliografisk träff 2009-09-03

Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.

Bryant C, Kerr ID, Debnath M, Ang KK, Ratnam J, Ferreira RS, Jaishankar P, Zhao D, Arkin MR, McKerrow JH, Brinen LS, Renslo AR.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2009.08.098

Bibliografisk träff 2008-06-10

Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.

Chen YT, Lira R, Hansell E, McKerrow JH, Roush WR.

Bioorg Med Chem Lett · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2008.06.012

Bibliografisk träff 2007-11-22

Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes.

Jaishankar P, Hansell E, Zhao DM, Doyle PS, McKerrow JH, Renslo AR.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2007.11.070

Bibliografisk träff 2007-10-22

Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain.

González FV, Izquierdo J, Rodríguez S, McKerrow JH, Hansell E.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2007.10.056

Bibliografisk träff 2007-08-13

A cysteine protease inhibitor cures Chagas' disease in an immunodeficient-mouse model of infection.

Doyle PS, Zhou YM, Engel JC, McKerrow JH.

Antimicrob Agents Chemother · research-article; journal article; research support, n.i.h., extramural · DOI 10.1128/aac.00436-07

Bibliografisk träff 2006-12-04

Cysteine protease inhibitors block Toxoplasma gondii microneme secretion and cell invasion.

Teo CF, Zhou XW, Bogyo M, Carruthers VB.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1128/aac.01059-06

Bibliografisk träff 2005-10-01

Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.

Fontana E, Dansette PM, Poli SM.

Curr Drug Metab · systematic review; journal article · DOI 10.2174/138920005774330639