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Emerging principles in protease-based drug discovery
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1 of the 128 references listed on this page is in the Retraction Watch database as retracted (export 2026-10-28): 10.1074/jbc.m000464200 (notice 2007-09-28).
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What this work says
Outgoing claims: the papers this work cites, builds on, or argues with.
inferredcites →https://doi.org/10.1002/elps.200800698openalex-snapshot“Reverse degradomics”, monitoring of proteolytic trimming by multi‐CE and confocal detection of fluorescent substrates and reaction products
inferredcites →https://doi.org/10.1006/jmbi.2001.5394openalex-snapshotThe Methyl Group of Nα(Me)Arg-containing Peptides Disturbs the Active-site Geometry of Thrombin, Impairing Efficient Cleavage
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inferredcites →https://doi.org/10.1021/ac048631popenalex-snapshotSimulation of Evolution-Selected Propeptide by High-Throughput Selection of a Peptidomimetic Inhibitor on a Capillary DNA Sequencer Platform
inferredcites →https://doi.org/10.1021/bi052252oopenalex-snapshotMMP-20 Is Predominately a Tooth-Specific Enzyme with a Deep Catalytic Pocket that Hydrolyzes Type V Collagen
inferredcites →https://doi.org/10.1021/bi9003638openalex-snapshotThe M17 Leucine Aminopeptidase of the Malaria Parasite Plasmodium falciparum: Importance of Active Site Metal Ions in the Binding of Substrates and Inhibitors
inferredcites →https://doi.org/10.1021/ja0547230openalex-snapshotSubstrate Activity Screening: A Fragment-Based Method for the Rapid Identification of Nonpeptidic Protease Inhibitors
inferredcites →https://doi.org/10.1021/jm0493156openalex-snapshot(2 R )-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3- a ]pyrazin- 7(8 H )-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
inferredcites →https://doi.org/10.1021/jm070111+openalex-snapshotCharacterization and Optimization of Selective, Nonpeptidic Inhibitors of Cathepsin S with an Unprecedented Binding Mode
inferredcites →https://doi.org/10.1021/jm070330vopenalex-snapshotDiscovery of Potent and Selective Dipeptidyl Peptidase IV Inhibitors Derived from β-Aminoamides Bearing Subsituted Triazolopiperazines
inferredcites →https://doi.org/10.1021/jm070733vopenalex-snapshotIdentification of Phosphinate Dipeptide Analog Inhibitors Directed against the Plasmodium falciparum M17 Leucine Aminopeptidase as Lead Antimalarial Compounds
inferredcites →https://doi.org/10.1023/b:thro.0000037670.42776.cdopenalex-snapshotThe Occasional Venous Thromboses Seen in Patients with Severe (Homozygous) FXII Deficiency are Probably Due to Associated Risk Factors: A Study of Prevalence in 21 Patients and Review of the Literature
inferredcites →https://doi.org/10.1038/72642openalex-snapshotSynthesis of positional-scanning libraries of fluorogenic peptide substrates to define the extended substrate specificity of plasmin and thrombin
inferredcites →https://doi.org/10.1038/90273openalex-snapshotDetermination of protease cleavage site motifs using mixture-based oriented peptide libraries
inferredcites →https://doi.org/10.1038/nm782openalex-snapshotReal-time in vivo imaging of platelets, tissue factor and fibrin during arterial thrombus formation in the mouse
inferredcites →https://doi.org/10.1042/bj20070940openalex-snapshotActivity profiling of human deSUMOylating enzymes (SENPs) with synthetic substrates suggests an unexpected specificity of two newly characterized members of the family
inferredcites →https://doi.org/10.1042/bj20080779openalex-snapshotPositional-scanning fluorigenic substrate libraries reveal unexpected specificity determinants of DUBs (deubiquitinating enzymes)
inferredcites →https://doi.org/10.1074/jbc.m000464200openalex-snapshotThrombin-mediated Feedback Activation of Factor XI on the Activated Platelet Surface Is Preferred over Contact Activation by Factor XIIa or Factor XIa
inferredcites →https://doi.org/10.1074/jbc.m500588200openalex-snapshotFunctional Profiling of Recombinant NS3 Proteases from All Four Serotypes of Dengue Virus Using Tetrapeptide and Octapeptide Substrate Libraries
inferredcites →https://doi.org/10.1074/jbc.m505933200openalex-snapshotA Urokinase-type Plasminogen Activator-inhibiting Cyclic Peptide with an Unusual P2 Residue and an Extended Protease Binding Surface Demonstrates New Modalities for Enzyme Inhibition
inferredcites →https://doi.org/10.1074/jbc.m513331200openalex-snapshotSubstrate Profiling of Cysteine Proteases Using a Combinatorial Peptide Library Identifies Functionally Unique Specificities
inferredcites →https://doi.org/10.1128/aac.01327-07openalex-snapshotChemical Target Validation Studies of Aminopeptidase in Malaria Parasites Using α-Aminoalkylphosphonate and Phosphonopeptide Inhibitors
inferredcites →https://doi.org/10.1182/blood-2002-12-3791openalex-snapshotAmoeboid shape change and contact guidance: T-lymphocyte crawling through fibrillar collagen is independent of matrix remodeling by MMPs and other proteases
inferredcites →https://doi.org/10.1182/blood.v14.11.1230.1230openalex-snapshotUse of the Plasma Thrombin Time to Assess the Adequacy of in Vivo Neutralization of Heparin: Comparative Studies Following Operations Employing Extracorporeal Circulation
inferredcites →https://doi.org/10.1185/03007990903152045openalex-snapshotACE inhibitors, angiotensin receptor blockers and direct renin inhibitors in combination: a review of their role after the ONTARGET trial
inferredcites →https://doi.org/10.1515/bc.2004.129openalex-snapshotActivation of the kallikrein-kinin system and release of new kinins through alternative cleavage of kininogens by microbial and human cell proteinases
inferredcites →https://doi.org/10.2147/vhrm.s3364openalex-snapshotRenin inhibition with aliskiren in hypertension: focus on aliskiren/hydrochlorothiazide combination therapy
inferredcites →https://doi.org/10.7270/q2z31wxkopenalex-snapshotBindingDB Entry 2158: Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.
What points at this work
Incoming claims: where this work appears in other papers’ reference lists and arguments.
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inferred← citeshttps://doi.org/10.1002/ange.202110027openalex-snapshotInhibition Mechanism of SARS‐CoV‐2 Main Protease with Ketone‐Based Inhibitors Unveiled by Multiscale Simulations: Insights for Improved Designs**
inferred← citeshttps://doi.org/10.1002/ange.202507241openalex-snapshotA Versatile DNAzyme‐Amplified Protease‐Sensing Platform for Accurate Diagnosis of SARS‐CoV‐2 and Reliable Classification of Colorectal Cancer
inferred← citeshttps://doi.org/10.1002/ange.8169928openalex-snapshotSpatially Controlled Imaging of Proteases in Acidic Extracellular Milieu of Lesions Using DNA‐Peptide‐PNA Hybrid Probes
inferred← citeshttps://doi.org/10.1002/anie.202110027openalex-snapshotInhibition Mechanism of SARS‐CoV‐2 Main Protease with Ketone‐Based Inhibitors Unveiled by Multiscale Simulations: Insights for Improved Designs**
inferred← citeshttps://doi.org/10.1002/anie.202507241openalex-snapshotA Versatile DNAzyme‐Amplified Protease‐Sensing Platform for Accurate Diagnosis of SARS‐CoV‐2 and Reliable Classification of Colorectal Cancer
inferred← citeshttps://doi.org/10.1002/anie.8169928openalex-snapshotSpatially Controlled Imaging of Proteases in Acidic Extracellular Milieu of Lesions Using DNA‐Peptide‐PNA Hybrid Probes
inferred← citeshttps://doi.org/10.1002/biof.2001openalex-snapshotAdvances in screening, synthesis, modification, and biomedical applications of peptides and peptide aptamers
inferred← citeshttps://doi.org/10.1002/bip.22231openalex-snapshotMechanism‐based selection of a potent kallikrein‐related peptidase 7 inhibitor from a versatile library based on the sunflower trypsin inhibitor SFTI‐1
inferred← citeshttps://doi.org/10.1002/bit.27519openalex-snapshotGeneration of highly selective monoclonal antibodies inhibiting a recalcitrant protease using decoy designs
inferred← citeshttps://doi.org/10.1002/chem.201904513openalex-snapshotQuantum Mechanics/Molecular Mechanics Studies of the Mechanism of Cysteine Proteases Inhibition by Dipeptidyl Nitroalkenes
inferred← citeshttps://doi.org/10.1002/chem.202301855openalex-snapshotNext Generation of Fluorometric Protease Assays: 7‐Nitrobenz‐2‐oxa‐1,3‐diazol‐4‐yl‐amides (NBD‐Amides) as Class‐Spanning Protease Substrates
inferred← citeshttps://doi.org/10.1002/cmdc.201300112openalex-snapshotOptimization of Triazine Nitriles as Rhodesain Inhibitors: Structure–Activity Relationships, Bioisosteric Imidazopyridine Nitriles, and X‐ray Crystal Structure Analysis with Human Cathepsin L
inferred← citeshttps://doi.org/10.1002/jrs.4995openalex-snapshotAmino‐methyl coumarin as a potential SERS@Ag probe for the evaluation of protease activity and inhibition
inferred← citeshttps://doi.org/10.1002/pep2.24377openalex-snapshotIn Silico Analysis of Conformational Dynamics and Energetic Landscapes of Putative Insulinase PF11_0189 From the Plasmodium falciparum Genome With Insulin‐Derived Peptides: Approach to Rationale Design of Insulin Peptide‐Based Inhibitors
inferred← citeshttps://doi.org/10.1002/slct.202507173openalex-snapshotUnveiling the Novel Multitarget Antidepressant Mechanisms of Ligustilide in Postpartum Depression: An Integrative Network Pharmacology and Molecular Simulation Study
inferred← citeshttps://doi.org/10.1007/978-94-007-6214-5_21openalex-snapshotThe Bitter Fruit with Sweet Health Benefits: A Comprehensive Synopsis of Recent Research Progress on Medicinal Properties of Momordica Charantia
inferred← citeshttps://doi.org/10.1007/s00216-018-1292-3openalex-snapshotA fluorometric sensing method for sensitive detection of trypsin and its inhibitor based on gold nanoclusters and gold nanoparticles
inferred← citeshttps://doi.org/10.1007/s11030-020-10166-3openalex-snapshotFirst structure–activity relationship analysis of SARS-CoV-2 virus main protease (Mpro) inhibitors: an endeavor on COVID-19 drug discovery
inferred← citeshttps://doi.org/10.1016/j.ab.2013.09.022openalex-snapshotCleavage of pro-tumor necrosis factor alpha by ADAM metallopeptidase domain 17: A fluorescence-based protease assay cleaves its natural protein substrate
inferred← citeshttps://doi.org/10.1016/j.abb.2025.110304openalex-snapshotUnveiling the cyclopropyl appended acyl thiourea derivatives as antimicrobial, α-amylase and proteinase K inhibitors: Design, synthesis, biological evaluation, molecular docking, DFT and ADMET studies
inferred← citeshttps://doi.org/10.1016/j.bcab.2015.11.007openalex-snapshotMagnesium dependent proteinaceous protease inhibitor with pesticidal potential from alkali-halotolerant Streptomyces spp.: Optimization of production using statistical tools
inferred← citeshttps://doi.org/10.1016/j.biochi.2011.10.014openalex-snapshotS1 pocket fingerprints of human and bacterial methionine aminopeptidases determined using fluorogenic libraries of substrates and phosphorus based inhibitors
inferred← citeshttps://doi.org/10.1016/j.biochi.2012.10.018openalex-snapshotAn integrated approach to the ligand binding specificity of Neisseria meningitidis M1 alanine aminopeptidase by fluorogenic substrate profiling, inhibitory studies and molecular modeling
inferred← citeshttps://doi.org/10.1016/j.biochi.2013.05.006openalex-snapshotToward very potent, non-covalent organophosphonate inhibitors of cathepsin C and related enzymes by 2-amino-1-hydroxy-alkanephosphonates dipeptides
inferred← citeshttps://doi.org/10.1016/j.bios.2025.117193openalex-snapshotMitigating dithiothreitol interference to gold/thiol interface in electrochemical detection of cathepsin B activity toward multiplex protease analysis
inferred← citeshttps://doi.org/10.1016/j.bmc.2020.115756openalex-snapshotAhp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7
inferred← citeshttps://doi.org/10.1016/j.bmc.2020.115860openalex-snapshotProtease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors
inferred← citeshttps://doi.org/10.1016/j.bmcl.2018.10.027openalex-snapshotCorrigendum to “Design, synthesis, biological evaluation, and molecular docking of chalcone derivatives as anti-inflammatory agents” [Bioorg. Med. Chem. Lett. 27 (3) (2017) 602–606]
inferred← citeshttps://doi.org/10.1016/j.csbj.2021.11.016openalex-snapshotNovel dynamic residue network analysis approaches to study allosteric modulation: SARS-CoV-2 M pro and its evolutionary mutations as a case study
inferred← citeshttps://doi.org/10.1016/j.ejmcr.2025.100311openalex-snapshotDiscovery of highly potent α-keto ester-based peptidomimetic inhibitors of the Hip1 protease for the treatment of Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116704openalex-snapshotCovalent small-molecule inhibitors of SARS-CoV-2 Mpro: Insights into their design, classification, biological activity, and binding interactions
inferred← citeshttps://doi.org/10.1016/j.ejmech.2025.118144openalex-snapshotMitigating SARS-CoV-2–exacerbated neuroinflammation and Alzheimer's pathology: Synthesis of quinoline-based dual inhibitors targeting cysteine and aspartyl proteases
inferred← citeshttps://doi.org/10.1016/j.febslet.2012.06.015openalex-snapshotComparative analysis of the substrate preferences of two post‐proline cleaving endopeptidases, prolyl oligopeptidase and fibroblast activation protein α
inferred← citeshttps://doi.org/10.1016/j.gene.2014.05.055openalex-snapshotCloning, characterization, expression analysis and inhibition studies of a novel gene encoding Bowman–Birk type protease inhibitor from rice bean
inferred← citeshttps://doi.org/10.1016/j.jmb.2015.08.005openalex-snapshotSelection of High-Affinity Peptidic Serine Protease Inhibitors with Increased Binding Entropy from a Back-Flip Library of Peptide–Protease Fusions
inferred← citeshttps://doi.org/10.1016/j.molstruc.2022.132652openalex-snapshotIn silico detection of potential inhibitors from vitamins and their derivatives compounds against SARS-CoV-2 main protease by using molecular docking, molecular dynamic simulation and ADMET profiling
inferred← citeshttps://doi.org/10.1016/j.peptides.2012.01.003openalex-snapshotIdentification and molecular cloning of a novel amphibian Bowman Birk-type trypsin inhibitor from the skin of the Hejiang Odorous Frog; Odorrana hejiangensis
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