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Vinyl Sulfones as Mechanism-Based Cysteine Protease Inhibitors
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Rhodesain inhibitors on the edge of reversibility-irreversibility
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1,2,4-Thiadiazole: A novel Cathepsin B inhibitor
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Ring substituent effects on biological activity of vinyl sulfones as inhibitors of HIV-1
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In vivo programming of endogenous antibodies via oral administration of adaptor ligands
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Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
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Highly tunable thiosulfonates as a novel class of cysteine protease inhibitors with anti-parasitic activity against Schistosoma mansoni
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3,4-Disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P3 elements for potency and selectivity
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Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors
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The Bsmoc group as a novel scaffold for the design of irreversible inhibitors of cysteine proteases
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Dipeptide vinyl sultams: Synthesis via the Wittig–Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum
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Dipeptidyl α-fluorovinyl Michael acceptors: Synthesis and activity against cysteine proteases
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Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes
inferred← citeshttps://doi.org/10.1016/j.bmcl.2008.06.012openalex-snapshot
Synthesis of macrocyclic trypanosomal cysteine protease inhibitors
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Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: Design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition
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The co-crystal structure of ubiquitin carboxy-terminal hydrolase L1 (UCHL1) with a tripeptide fluoromethyl ketone (Z-VAE(OMe)-FMK)
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Synthesis of proline analogues as potent and selective cathepsin S inhibitors
inferred← citeshttps://doi.org/10.1016/j.bmcl.2018.05.005openalex-snapshot
Synthesis and kinetic evaluation of ethyl acrylate and vinyl sulfone derived inhibitors for human cysteine cathepsins
inferred← citeshttps://doi.org/10.1016/j.bmcl.2018.11.019openalex-snapshot
Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments
inferred← citeshttps://doi.org/10.1016/j.cbpa.2008.06.033openalex-snapshot
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inferred← citeshttps://doi.org/10.1016/j.cbpa.2014.08.011openalex-snapshot
Endo-lysosomal proteases in antigen presentation
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Assembly of 3-sulfonated 2H-pyrrol-2-ones through the insertion of sulfur dioxide with allenoic amides
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Proteasome Inhibitors: An Expanding Army Attacking a Unique Target
inferred← citeshttps://doi.org/10.1016/j.ejmech.2008.09.044openalex-snapshot
Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities
inferred← citeshttps://doi.org/10.1016/j.ejmech.2010.05.039openalex-snapshot
Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure–activity study
inferred← citeshttps://doi.org/10.1016/j.ejmech.2018.08.074openalex-snapshot
Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities
inferred← citeshttps://doi.org/10.1016/j.ejmech.2018.08.079openalex-snapshot
Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors
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Covalent small-molecule inhibitors of SARS-CoV-2 Mpro: Insights into their design, classification, biological activity, and binding interactions
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Inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice
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Macrophage-mediated controlled release of cysteine protease inhibitor from PLGA-PEG/hydroxyapatite microspheres for targeting cathepsin S in Alzheimer’s disease
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Leishmania tropica: cysteine proteases are essential for growth and pathogenicity
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Targeting the active sites of malarial proteases for antimalarial drug discovery: approaches, progress and challenges
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Analysis of Kunitz inhibitors from plants for comprehensive structural and functional insights
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The Phosphoinositide Kinase PIKfyve Promotes Cathepsin-S-Mediated Major Histocompatibility Complex Class II Antigen Presentation
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Cathepsin S dominates autoantigen processing in human thymic dendritic cells
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Structure, interdomain dynamics, and pH-dependent autoactivation of pro-rhodesain, the main lysosomal cysteine protease from African trypanosomes
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Probing the potential of platinum(II) complexes for the inhibition of thiol-dependent enzymatic activity
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Photoredox Catalyzed Sulfonylation of Multisubstituted Allenes with Ru(bpy)3Cl2 or Rhodamine B
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Serum albumin as a probe for testing the selectivity of irreversible cysteine protease inhibitors: The case of vinyl sulfones
inferred← citeshttps://doi.org/10.1016/j.jscs.2024.101848openalex-snapshot
Selective C–C bond cleavage of cycloketoximes via iminyl radicals and distal carbon radicals through photocatalysis
inferred← citeshttps://doi.org/10.1016/j.mam.2022.101150openalex-snapshot
Cysteine cathepsins: A long and winding road towards clinics
inferred← citeshttps://doi.org/10.1016/j.molbiopara.2019.111246openalex-snapshot
Trypanosoma brucei: Inhibition of cathepsin L is sufficient to kill bloodstream forms
inferred← citeshttps://doi.org/10.1016/j.sjbs.2021.09.014openalex-snapshot
Exploring the role of cathepsin in rheumatoid arthritis
inferred← citeshttps://doi.org/10.1016/j.tet.2015.07.043openalex-snapshot
An efficient one-pot, three-component synthesis of vinyl sulfones via iodide-catalyzed radical alkenylation
inferred← citeshttps://doi.org/10.1016/j.tet.2016.01.042openalex-snapshot
Decarboxylative sulfonylation of arylpropiolic acids with sulfinic acids: synthesis of (E)-vinyl sulfones
inferred← citeshttps://doi.org/10.1016/j.tet.2021.132310openalex-snapshot
Synthesis of (E)-iodo vinylsulfones via oxidative addition of thiol into alkyne under metal free condition
inferred← citeshttps://doi.org/10.1016/j.tetlet.2005.12.101openalex-snapshot
A convenient semicarbazide resin for the solid-phase synthesis of peptide ketones and aldehydes
inferred← citeshttps://doi.org/10.1016/j.tetlet.2007.11.091openalex-snapshot
Formation of 2-arylindane-1,3-diones and 3-alkylphthalides from methyl o-[α-phenylsulfonyl]toluate
inferred← citeshttps://doi.org/10.1016/j.tetlet.2009.07.063openalex-snapshot
Radical-mediated thiodesulfonylation of the vinyl sulfones: access to (α-fluoro)vinyl sulfides
inferred← citeshttps://doi.org/10.1016/j.tetlet.2013.03.056openalex-snapshot
A base-controlled regioselective synthesis of allyl and vinyl phenyl sulfones
inferred← citeshttps://doi.org/10.1016/j.tetlet.2021.153203openalex-snapshot
Transition-metal-free NaI-mediated reaction of aryl sulfonyl chloride with alkynes: Synthesis of (E)-β-iodovinyl sulfones
inferred← citeshttps://doi.org/10.1016/j.trsl.2018.04.007openalex-snapshot
The proteasome as a target to combat malaria: hits and misses
inferred← citeshttps://doi.org/10.1016/j.ymeth.2003.10.003openalex-snapshot
Using peptide libraries to identify optimal cleavage motifs for proteolytic enzymes
inferred← citeshttps://doi.org/10.1016/s0002-9440(10)63068-4openalex-snapshot
Cathepsin K Is a Critical Protease in Synovial Fibroblast-Mediated Collagen Degradation
inferred← citeshttps://doi.org/10.1016/s0002-9440(10)63641-3openalex-snapshot
The Clinical Significance of Cathepsin S Expression in Human Astrocytomas
inferred← citeshttps://doi.org/10.1016/s0014-5793(01)03008-3openalex-snapshot
Reversible inhibition of cathepsin L‐like proteases by 4‐mer pseudopeptides
inferred← citeshttps://doi.org/10.1016/s0022-2836(02)00145-6openalex-snapshot
Crystal Structure of HslUV Complexed with a Vinyl Sulfone Inhibitor: Corroboration of a Proposed Mechanism of Allosteric Activation of HslV by HslU
inferred← citeshttps://doi.org/10.1016/s0022-2836(02)00780-5openalex-snapshot
The Crystal Structure of Human Cathepsin F and Its Implications for the Development of Novel Immunomodulators
inferred← citeshttps://doi.org/10.1016/s0022-3565(24)37785-7openalex-snapshot
Effects of Ketoconazole on the Intestinal Metabolism, Transport and Oral Bioavailability of K02, a Novel Vinylsulfone Peptidomimetic Cysteine Protease Inhibitor and a P450 3A, P-Glycoprotein Dual Substrate, in Male Sprague-Dawley Rats
inferred← citeshttps://doi.org/10.1016/s0040-4020(00)00882-6openalex-snapshot
Design, Synthesis and Evaluation of d-Homophenylalanyl Epoxysuccinate Inhibitors of the Trypanosomal Cysteine Protease Cruzain
inferred← citeshttps://doi.org/10.1016/s0040-4039(02)01805-1openalex-snapshot
Synthesis of Fmoc-protected amino ketones bearing tert-butyl based side-chain protecting groups
inferred← citeshttps://doi.org/10.1016/s0040-4039(99)00388-3openalex-snapshot
“One-pot” preparation of N-(Carbonylamino)amino acids and half-acid/half-ester urea dipeptides directly from α-amio acids
inferred← citeshttps://doi.org/10.1016/s0045-2068(02)00009-3openalex-snapshot
pH Dependence of inhibitors targeting the occluding loop of cathepsin B
inferred← citeshttps://doi.org/10.1016/s0065-2776(02)80013-xopenalex-snapshot
Proteolysis and antigen presentation by MHC class II molecules
inferred← citeshttps://doi.org/10.1016/s0065-7743(00)35029-1openalex-snapshot
Chapter 28. Inhibition of cysteine proteases
inferred← citeshttps://doi.org/10.1016/s0065-7743(04)39007-xopenalex-snapshot
Inhibition of the Cysteine Protease Cathepsin K (EC 3.4.22.38)
inferred← citeshttps://doi.org/10.1016/s0079-6468(04)42006-2openalex-snapshot
Cathepsin K Inhibitors: Their Potential as Anti-Osteoporosis Agents
inferred← citeshttps://doi.org/10.1016/s0079-6468(05)43006-4openalex-snapshot
Recent Advances in the Search for Newer Antimalarial Agents
inferred← citeshttps://doi.org/10.1016/s0162-3109(00)00267-8openalex-snapshot
Dipeptide vinyl sulfones suitable for intracellular inhibition of dipeptidyl peptidase I
inferred← citeshttps://doi.org/10.1016/s0165-5728(03)00093-6openalex-snapshot
Antigen processing and presentation in human muscle: cathepsin S is critical for MHC class II expression and upregulated in inflammatory myopathies
inferred← citeshttps://doi.org/10.1016/s0166-1280(03)00086-1openalex-snapshot
An approximation to the mechanism of inhibition of cystein proteases: nucleophilic sulphur addition to Michael acceptors type compounds
inferred← citeshttps://doi.org/10.1016/s0166-6851(98)00012-7openalex-snapshot
The role of proteolysis during differentiation of Trypanosoma brucei from the bloodstream to the procyclic form
inferred← citeshttps://doi.org/10.1016/s0167-5699(97)80021-7openalex-snapshot
Destruction of proteins as a creative force
inferred← citeshttps://doi.org/10.1016/s0168-3659(99)00034-6openalex-snapshot
Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery
inferred← citeshttps://doi.org/10.1016/s0223-5234(00)00118-5openalex-snapshot
Synthesis and activity of pyrrolidinyl- and thiazolidinyl-dipeptide derivatives as inhibitors of the Tc80 prolyl oligopeptidase from Trypanosoma cruzi
inferred← citeshttps://doi.org/10.1016/s0924-8579(03)00096-7openalex-snapshot
Improved trypanocidal activities of cathepsin L inhibitors
inferred← citeshttps://doi.org/10.1016/s0960-894x(00)00340-1openalex-snapshot
Development of peptidyl α-keto-β-aldehydes as new inhibitors of cathepsin L — comparisons of potency and selectivity profiles with cathepsin B
inferred← citeshttps://doi.org/10.1016/s0960-894x(00)00451-0openalex-snapshot
Calpain inhibitors based on the quiescent affinity label concept: high rates of calpain inactivation with leaving groups derived from N-hydroxy peptide coupling reagents
inferred← citeshttps://doi.org/10.1016/s0960-894x(01)00440-1openalex-snapshot
Vinyl sulfonium as novel proteolytic enzyme inhibitor
inferred← citeshttps://doi.org/10.1016/s0960-894x(01)00566-2openalex-snapshot
Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain
inferred← citeshttps://doi.org/10.1016/s0960-894x(02)00008-2openalex-snapshot
Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. Part 7: Structure–Activity Studies of Bicyclic 2-Pyridone-Containing Peptidomimetics
inferred← citeshttps://doi.org/10.1016/s0960-894x(02)00619-4openalex-snapshot
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain
inferred← citeshttps://doi.org/10.1016/s0960-894x(02)00765-5openalex-snapshot
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors
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