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Subnanomolar Cathepsin S Inhibitors with High Selectivity: Optimizing Covalent Reversible α‐Fluorovinylsulfones and α‐Sulfonates as Potential Immunomodulators in Cancer

https://doi.org/10.1002/cmdc.202300160

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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

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Reversible Covalent Inhibition of a Protein Target

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CD8+ cytotoxic T lymphocytes in cancer immunotherapy: A review

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Insights from molecular modeling into the selective inhibition of cathepsin S by its inhibitor

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Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

inferredcites →https://doi.org/10.1016/j.bbamcr.2020.118781openalex-snapshot

Leading the invasion: The role of Cathepsin S in the tumour microenvironment

inferredcites →https://doi.org/10.1016/j.biocel.2016.08.030openalex-snapshot

Differential cathepsin responses to inhibitor-induced feedback: E-64 and cystatin C elevate active cathepsin S and suppress active cathepsin L in breast cancer cells

inferredcites →https://doi.org/10.1016/j.biochi.2011.08.017openalex-snapshot

Inhibition of Cathepsin S by Fsn0503 enhances the efficacy of chemotherapy in colorectal carcinomas

inferredcites →https://doi.org/10.1016/j.bmcl.2006.07.033openalex-snapshot

Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers

inferredcites →https://doi.org/10.1016/j.bmcl.2007.06.023openalex-snapshot

The identification of potent, selective, and bioavailable cathepsin S inhibitors

inferredcites →https://doi.org/10.1016/j.bmcl.2010.10.012openalex-snapshot

Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors

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Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent

inferredcites →https://doi.org/10.1016/j.ccell.2020.03.016openalex-snapshot

Cathepsin S Regulates Antigen Processing and T Cell Activity in Non-Hodgkin Lymphoma

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Cathepsin S Alterations Induce a Tumor-Promoting Immune Microenvironment in Follicular Lymphoma

inferredcites →https://doi.org/10.1016/j.drudis.2015.05.005openalex-snapshot

Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies

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Cathepsin S inhibition changes regulatory T-cell activity in regulating bladder cancer and immune cell proliferation and apoptosis

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Human cathepsin S: chromosomal localization, gene structure, and tissue distribution

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Cathepsin S Required for Normal MHC Class II Peptide Loading and Germinal Center Development

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Essential Role for Cathepsin S in MHC Class II–Associated Invariant Chain Processing and Peptide Loading

inferredcites →https://doi.org/10.1021/acs.jmedchem.1c01002openalex-snapshot

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

inferredcites →https://doi.org/10.1021/bi000951popenalex-snapshot

Crystal Structure of Human Cathepsin V,

inferredcites →https://doi.org/10.1021/bi027308iopenalex-snapshot

Specificity Determinants of Human Cathepsin S Revealed by Crystal Structures of Complexes ,

inferredcites →https://doi.org/10.1021/cr950025uopenalex-snapshot

Cysteine Proteases and Their Inhibitors

inferredcites →https://doi.org/10.1021/jacs.6b03052openalex-snapshot

Quantum Chemical-Based Protocol for the Rational Design of Covalent Inhibitors

inferredcites →https://doi.org/10.1021/jm020209iopenalex-snapshot

Design and Synthesis of Dipeptide Nitriles as Reversible and Potent Cathepsin S Inhibitors

inferredcites →https://doi.org/10.1021/jm401528kopenalex-snapshot

Identification of Potent and Selective Cathepsin S Inhibitors Containing Different Central Cyclic Scaffolds

inferredcites →https://doi.org/10.1021/ml500283gopenalex-snapshot

Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm

inferredcites →https://doi.org/10.1021/pr100492xopenalex-snapshot

Cathepsin S Mediates Gastric Cancer Cell Migration and Invasion via a Putative Network of Metastasis-Associated Proteins

inferredcites →https://doi.org/10.1038/nchembio.1817openalex-snapshot

Prolonged and tunable residence time using reversible covalent kinase inhibitors

inferredcites →https://doi.org/10.1038/nrd2082openalex-snapshot

Drug–target residence time and its implications for lead optimization

inferredcites →https://doi.org/10.1042/bj2640467openalex-snapshot

Cathepsin S from bovine spleen. Purification, distribution, intracellular localization and action on proteins

inferredcites →https://doi.org/10.1074/jbc.m109.014340openalex-snapshot

Vinyl Sulfones as Antiparasitic Agents and a Structural Basis for Drug Design

inferredcites →https://doi.org/10.1084/jem.186.4.549openalex-snapshot

Degradation of Mouse Invariant Chain: Roles of Cathepsins S and D and the Influence of Major Histocompatibility Complex Polymorphism

inferredcites →https://doi.org/10.1093/nar/28.1.235openalex-snapshot

The Protein Data Bank

inferredcites →https://doi.org/10.1108/rr.2000.14.2.21.73openalex-snapshot

The Cambridge Guide to Women’s Writing in English

inferredcites →https://doi.org/10.1111/j.0105-2896.2005.00310.xopenalex-snapshot

The lysosomal cysteine proteases in MHC class II antigen presentation

inferredcites →https://doi.org/10.1111/j.1432-1033.1996.00558.xopenalex-snapshot

Folding and Activation of Human Procathepsin S from Inclusion Bodies Produced in Escherichia coli

inferredcites →https://doi.org/10.1158/1078-0432.ccr-09-1262openalex-snapshot

Antibody-Mediated Inhibition of Cathepsin S Blocks Colorectal Tumor Invasion and Angiogenesis

inferredcites →https://doi.org/10.1172/jci1158openalex-snapshot

Cathepsin S activity regulates antigen presentation and immunity.

inferredcites →https://doi.org/10.1186/s12943-016-0513-7openalex-snapshot

A bioavailable cathepsin S nitrile inhibitor abrogates tumor development

inferredcites →https://doi.org/10.1517/13543776.14.3.301openalex-snapshot

Cathepsin S inhibitors

inferredcites →https://doi.org/10.1517/13543776.2011.553800openalex-snapshot

Cathepsin S inhibitors: 2004 – 2010

inferredcites →https://doi.org/10.1517/17460441.2012.688744openalex-snapshot

Drug discovery for a new generation of covalent drugs

inferredcites →https://doi.org/10.18632/oncotarget.8582openalex-snapshot

Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer

inferredcites →https://doi.org/10.2174/156802610791113432openalex-snapshot

Recent Advances in the Design of Cathepsin S Inhibitors

inferredcites →https://doi.org/10.3389/fimmu.2018.03059openalex-snapshot

Dendritic Cells and CD8 T Cell Immunity in Tumor Microenvironment

inferredcites →https://doi.org/10.3389/fimmu.2019.02037openalex-snapshot

Cysteine Cathepsins in Tumor-Associated Immune Cells

inferredcites →https://doi.org/10.3389/fonc.2020.01290openalex-snapshot

Mechanisms of Cancer Resistance to Immunotherapy

inferredcites →https://doi.org/10.3390/cells8070747openalex-snapshot

Macrophage-Mediated Subversion of Anti-Tumour Immunity

inferredcites →https://doi.org/10.3390/cells9092021openalex-snapshot

Novel Opportunities for Cathepsin S Inhibitors in Cancer Immunotherapy by Nanocarrier-Mediated Delivery

inferredcites →https://doi.org/10.4049/jimmunol.174.3.1205openalex-snapshot

Cathepsin S Controls MHC Class II-Mediated Antigen Presentation by Epithelial Cells In Vivo

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

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Novel Insights Into the Dynamic Conformational Transitions and Active Site Plasticity of Human Immunoregulatory Cathepsin S

inferred← citeshttps://doi.org/10.1016/j.bioorg.2024.107830openalex-snapshot

Rhodesain inhibitors on the edge of reversibility-irreversibility

inferred← citeshttps://doi.org/10.1016/j.intimp.2025.114622openalex-snapshot

Cathepsin S: A key drug target and signalling hub in immune system diseases

inferred← citeshttps://doi.org/10.1021/acsmedchemlett.4c00050openalex-snapshot

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

inferred← citeshttps://doi.org/10.1101/2025.04.13.648563openalex-snapshot

Sustained Antigen Stimulation to Evoke and Study Negative feedback Systems responsible for Self-Tolerance/Tumor Immune Escape and transition to the M2 macrophage

inferred← citeshttps://doi.org/10.1186/s41181-026-00493-5openalex-snapshot

Development and preclinical evaluation of selective vinyl sulfone-based probes for PET imaging of tumor-associated cathepsins

inferred← citeshttps://doi.org/10.3390/ph18101462openalex-snapshot

A Second Opportunity for the Peptide-Based Analogues with γ-Lactam at the P1 Position: Human Cathepsin S Inhibition

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