A Review of Small Molecule Inhibitors and Functional Probes of Human Cathepsin L (Q89634052)

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7 April 2020

review article

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title

A Review of Small Molecule Inhibitors and Functional Probes of Human Cathepsin L (English)

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7 April 2020

2

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7 April 2020

author name string

Dibyendu Dana

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1

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7 April 2020

publication date

6 February 2020

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7 April 2020

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7 April 2020

volume

25

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7 April 2020

issue

3

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Creative Commons Attribution 4.0 International

7 April 2020

copyright license

start time

6 February 2020

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April 2022 Public Data File from Crossref

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cites work

Transformation-dependent secretion of a low molecular weight protein by murine fibroblasts

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12 December 2020

Cysteine protease inhibition by azapeptide esters

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12 December 2020

Inhibition of cysteine proteinases in lysosomes and whole cells

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12 December 2020

Tight-binding inhibition of cathepsin S by cystatins

1 reference

12 December 2020

The identification of active forms of cysteine proteinases in Kirsten-virus-transformed mouse fibroblasts by use of a specific radiolabelled inhibitor

1 reference

12 December 2020

Reactions between dipeptidyl peptidase IV and diacyl hydroxylamines: mechanistic investigations

1 reference

12 December 2020

Potent and selective inactivation of cysteine proteinases with N-peptidyl-O-acyl hydroxylamines

1 reference

12 December 2020

Lysosomal acid phosphatase is transported to lysosomes via the cell surface

1 reference

12 December 2020

The use of benzyloxycarbonyl[125I]iodotyrosylalanyldiazomethane as a probe for active cysteine proteinases in human tissues

1 reference

12 December 2020

Evidence that aspartic proteinase is involved in the proteolytic processing event of procathepsin L in lysosomes

1 reference

12 December 2020

Potent and selective inactivation of proteinases with N-peptidyl-O-acylhydroxylamines

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12 December 2020

The design of peptidyldiazomethane inhibitors to distinguish between the cysteine proteinases calpain II, cathepsin L and cathepsin B

1 reference

12 December 2020

Dipeptidylpeptidase IV--inactivation with N-peptidyl-O-aroyl hydroxylamines

1 reference

12 December 2020

Human low-Mr kininogen contains three copies of a cystatin sequence that are divergent in structure and in inhibitory activity for cysteine proteinases

1 reference

12 December 2020

Lysosomal enzyme phosphorylation. Recognition of a protein-dependent determinant allows specific phosphorylation of oligosaccharides present on lysosomal enzymes

1 reference

12 December 2020

The place of human gamma-trace (cystatin C) amongst the cysteine proteinase inhibitors

1 reference

12 December 2020

1 reference

12 December 2020

Identification of a 31,500 molecular weight islet cell protease as cathepsin B

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12 December 2020

N,O-diacylhydroxylamines as enzyme-activated inhibitors for serine proteases

1 reference

12 December 2020

Cystatin-like cysteine proteinase inhibitors from human liver

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12 December 2020

L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L

1 reference

12 December 2020

Aziridine analogs of [[trans-(epoxysuccinyl)-L-leucyl]amino]-4-guanidinobutane (E-64) as inhibitors of cysteine proteases

1 reference

12 December 2020

Vinyl sulfones as mechanism-based cysteine protease inhibitors

1 reference

12 December 2020

Peptidyl (acyloxy)methanes as quiescent affinity labels for cysteine proteinases

1 reference

12 December 2020

Structural and functional characterization of two allelic variants of human cystatin D sharing a characteristic inhibition spectrum against mammalian cysteine proteinases

1 reference

12 December 2020

E64 [trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane] analogues as inhibitors of cysteine proteinases: investigation of S2 subsite interactions

1 reference

12 December 2020

Novel N-peptidyl-O-acyl hydroxamates: selective inhibitors of cysteine proteinases

1 reference

12 December 2020

In vitro activation of pro-cathepsin B by three serine proteinases: leucocyte elastase, cathepsin G, and the urokinase-type plasminogen activator

1 reference

12 December 2020

N-peptidyl-O-carbamoyl amino acid hydroxamates: irreversible inhibitors for the study of the S2' specificity of cysteine proteinases.

1 reference

12 December 2020

Major histocompatibility complex class II-associated p41 invariant chain fragment is a strong inhibitor of lysosomal cathepsin L

1 reference

12 December 2020

Peptidyl vinyl sulphones: a new class of potent and selective cysteine protease inhibitors: S2P2 specificity of human cathepsin O2 in comparison with cathepsins S and L.

1 reference

12 December 2020

Potency and selectivity of the cathepsin L propeptide as an inhibitor of cysteine proteases

1 reference

12 December 2020

Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo

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12 December 2020

Crystallization and preliminary X-ray diffraction studies of human procathepsin L

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12 December 2020

Structure of human procathepsin L reveals the molecular basis of inhibition by the prosegment

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12 December 2020

The crystal structure of human cathepsin L complexed with E-64

1 reference

12 December 2020

Cathepsin L: critical role in Ii degradation and CD4 T cell selection in the thymus

1 reference

12 December 2020

pH-induced conformational transitions of the propeptide of human cathepsin L. A role for a molten globule state in zymogen activation

1 reference

12 December 2020

Quantification of cathepsins B and L in cells

1 reference

12 December 2020

Cystatin F is a glycosylated human low molecular weight cysteine proteinase inhibitor

1 reference

12 December 2020

Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption

1 reference

12 December 2020

New Peptidic Cysteine Protease Inhibitors Derived from the Electrophilic α-Amino Acid Aziridine-2,3-dicarboxylic Acid

1 reference

12 December 2020

Structure based development of novel specific inhibitors for cathepsin L and cathepsin S in vitro and in vivo

1 reference

12 December 2020

Inhibition mechanism of cathepsin L-specific inhibitors based on the crystal structure of papain-CLIK148 complex

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12 December 2020

Secreted cathepsin L generates endostatin from collagen XVIII

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12 December 2020

Distinct roles of cathepsin K and cathepsin L in osteoclastic bone resorption

1 reference

12 December 2020

Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B

1 reference

12 December 2020

Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.

1 reference

12 December 2020

Azepanone-based inhibitors of human and rat cathepsin K

1 reference

12 December 2020

Characterization of human cathepsin L promoter and identification of binding sites for NF-Y, Sp1 and Sp3 that are essential for its activity

1 reference

12 December 2020

In situ hybridization screen in zebrafish for the selection of genes encoding secreted proteins.

1 reference

12 December 2020

Splice variants of human cathepsin L mRNA show different expression rates

1 reference

12 December 2020

Dilated cardiomyopathy in mice deficient for the lysosomal cysteine peptidase cathepsin L.

1 reference

12 December 2020

Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides

1 reference

12 December 2020

Lysosomal cysteine proteases (cathepsins): promising drug targets.

1 reference

12 December 2020

Relative rates of Michael reactions of 2'-(phenethyl)thiol with vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides relevant to vinyl sulfonyl cysteine protease inhibitors

1 reference

12 December 2020

Cathepsin L in secretory vesicles functions as a prohormone-processing enzyme for production of the enkephalin peptide neurotransmitter.

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12 December 2020

Impaired cathepsin L gene expression in skeletal muscle is associated with type 2 diabetes

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12 December 2020

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12 December 2020

A cathepsin L isoform that is devoid of a signal peptide localizes to the nucleus in S phase and processes the CDP/Cux transcription factor

1 reference

12 December 2020

Cathepsin L is crucial for a Th1-type immune response during Leishmania major infection.

1 reference

12 December 2020

Activity-based probes for protein tyrosine phosphatases

1 reference

12 December 2020

Cathepsin L-deficient mice exhibit abnormal skin and bone development and show increased resistance to osteoporosis following ovariectomy

1 reference

12 December 2020

Comprehensive search for cysteine cathepsins in the human genome

1 reference

12 December 2020

Synthesis and antiplasmodial activity of a cysteine protease-inhibiting biotinylated aziridine-2,3-dicarboxylate

1 reference

12 December 2020

Podocyte migration during nephrotic syndrome requires a coordinated interplay between cathepsin L and alpha3 integrin

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12 December 2020

Complete and limited proteolysis in cell cycle progression.

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12 December 2020

Multiple roles for cysteine cathepsins in cancer

1 reference

12 December 2020

The lysosome turns fifty

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12 December 2020

Cathepsin L is essential for onset of autoimmune diabetes in NOD mice

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12 December 2020

Zebrafish KLF4 is essential for anterior mesendoderm/pre-polster differentiation and hatching

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12 December 2020

Azepanone-based inhibitors of human cathepsin L.

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12 December 2020

Activity-based probes that target diverse cysteine protease families

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12 December 2020

Dynamic imaging of protease activity with fluorescently quenched activity-based probes.

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12 December 2020

Distinct roles for cysteine cathepsin genes in multistage tumorigenesis

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12 December 2020

Substrate profiling of cysteine proteases using a combinatorial peptide library identifies functionally unique specificities

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12 December 2020

Lysosomal, cytoskeletal, and metabolic alterations in cardiomyopathy of cathepsin L knockout mice

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12 December 2020

Antiinflammatory and immunosuppressive activity of sialostatin L, a salivary cystatin from the tick Ixodes scapularis.

1 reference

12 December 2020

Global analysis of protein tyrosine phosphatase activity with ultra-sensitive fluorescent probes.

1 reference

12 December 2020

Rational Design of Aziridine-Containing Cysteine Protease Inhibitors with Improved Potency: Studies on Inhibition Mechanism

1 reference

12 December 2020

Aziridide-Based Inhibitors of Cathepsin L: Synthesis, Inhibition Activity, and Docking Studies

1 reference

12 December 2020

Osteoclastic bone degradation and the role of different cysteine proteinases and matrix metalloproteinases: differences between calvaria and long bone

1 reference

12 December 2020

Cysteine cathepsins: multifunctional enzymes in cancer

1 reference

12 December 2020

Cysteine cathepsins and the cutting edge of cancer invasion

1 reference

12 December 2020

Cathepsin L deficiency reduces diet-induced atherosclerosis in low-density lipoprotein receptor-knockout mice.

1 reference

12 December 2020

Crystal structure of the parasite protease inhibitor chagasin in complex with a host target cysteine protease

1 reference

12 December 2020

Proteolytic processing of dynamin by cytoplasmic cathepsin L is a mechanism for proteinuric kidney disease

1 reference

12 December 2020

Noninvasive optical imaging of cysteine protease activity using fluorescently quenched activity-based probes.

1 reference

12 December 2020

Increased expression and activity of nuclear cathepsin L in cancer cells suggests a novel mechanism of cell transformation.

1 reference

12 December 2020

Cell type-specific functions of the lysosomal protease cathepsin L in the heart

1 reference

12 December 2020

Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor

1 reference

12 December 2020

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

1 reference

12 December 2020

Exploring inhibitor binding at the S' subsites of cathepsin L

1 reference

12 December 2020

Homing and engraftment of progenitor cells: a prerequisite for cell therapy

1 reference

12 December 2020

Activity-based protein profiling: from enzyme chemistry to proteomic chemistry

1 reference

12 December 2020

Cathepsin L expression is up-regulated by hypoxia in human melanoma cells: role of its 5'-untranslated region.

1 reference

12 December 2020

Crystal structure and silica condensing activities of silicatein α–cathepsin L chimeras

1 reference

12 December 2020

Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L

1 reference

12 December 2020

Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB

1 reference

12 December 2020

Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype

1 reference

12 December 2020

Molecular docking of cathepsin L inhibitors in the binding site of papain

1 reference

12 December 2020

High glucose reduces cathepsin L activity and impairs invasion of circulating progenitor cells

1 reference

12 December 2020

The actin cytoskeleton of kidney podocytes is a direct target of the antiproteinuric effect of cyclosporine A.

1 reference

12 December 2020

Acceleration of polycystic kidney disease progression in cpk mice carrying a deletion in the homeodomain protein Cux1

1 reference

12 December 2020

Lysosomal cysteine peptidase cathepsin L protects against cardiac hypertrophy through blocking AKT/GSK3beta signaling

1 reference

12 December 2020

Autophagic neuron death.

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12 December 2020

Regulation of cell proliferation and differentiation in the kidney.

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12 December 2020

Dipeptidyl nitrile inhibitors of Cathepsin L

1 reference

12 December 2020

A cathepsin L-specific inhibitor preferentially inhibits degradation of autophagosomal LC3 and GABARAP in HeLa and Huh-7 cells.

1 reference

12 December 2020

Roles for cathepsins S, L, and B in insulitis and diabetes in the NOD mouse

1 reference

12 December 2020

A combined crystallographic and molecular dynamics study of cathepsin L retrobinding inhibitors

1 reference

12 December 2020

Acquisition of T regulatory function in cathepsin L-inhibited T cells by eye-derived CTLA-2alpha during inflammatory conditions

1 reference

12 December 2020

Cathepsin L inactivates human trypsinogen, whereas cathepsin L-deletion reduces the severity of pancreatitis in mice.

1 reference

12 December 2020

Cathepsin L, target in cancer treatment?

1 reference

12 December 2020

Real-time monitoring of drug release

1 reference

12 December 2020

Enhancing the outcome of cell therapy for cardiac repair: progress from bench to bedside and back

1 reference

12 December 2020

Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors

1 reference

12 December 2020

Finding enzymes that are actively involved in cancer

1 reference

12 December 2020

A small-molecule oxocarbazate inhibitor of human cathepsin L blocks severe acute respiratory syndrome and ebola pseudotype virus infection into human embryonic kidney 293T cells.

1 reference

12 December 2020

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

1 reference

12 December 2020

Novel peptidyl aryl vinyl sulfones as highly potent and selective inhibitors of cathepsins L and B.

1 reference

12 December 2020

Homing of progenitor cells to ischemic tissues

1 reference

12 December 2020

Structural basis for reversible and irreversible inhibition of human cathepsin L by their respective dipeptidyl glyoxal and diazomethylketone inhibitors

1 reference

12 December 2020

Specialized roles for cysteine cathepsins in health and disease.

1 reference

12 December 2020

Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.

1 reference

12 December 2020

The proteome of lysosomes

1 reference

12 December 2020

Parkinson's disease involves autophagy and abnormal distribution of cathepsin L

1 reference

12 December 2020

Cathepsin-L contributes to cardiac repair and remodelling post-infarction.

1 reference

12 December 2020

Systematic investigation of halogen bonding in protein-ligand interactions

1 reference

12 December 2020

Structural basis for the recognition and cleavage of histone H3 by cathepsin L

1 reference

12 December 2020

The resurgence of covalent drugs

1 reference

12 December 2020

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

1 reference

12 December 2020

Halogen bonding at the active sites of human cathepsin L and MEK1 kinase: efficient interactions in different environments

1 reference

12 December 2020

Cysteine cathepsins: from structure, function and regulation to new frontiers

1 reference

12 December 2020

Functional imaging of proteases: recent advances in the design and application of substrate-based and activity-based probes

1 reference

12 December 2020

The tick salivary protein sialostatin L inhibits the Th9-derived production of the asthma-promoting cytokine IL-9 and is effective in the prevention of experimental asthma.

1 reference

12 December 2020

Protease-activated drug development

1 reference

12 December 2020

Decreased arthritis severity in cathepsin L-deficient mice is attributed to an impaired T helper cell compartment

1 reference

12 December 2020

Microarray-guided discovery of two-photon (2P) small molecule probes for live-cell imaging of cysteinyl cathepsin activities

1 reference

12 December 2020

A novel photoaffinity-based probe for selective detection of cathepsin L active form

1 reference

12 December 2020

Podocyte biology and pathogenesis of kidney disease

1 reference

12 December 2020

Biogenesis and proteolytic processing of lysosomal DNase II

1 reference

12 December 2020

Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?

1 reference

12 December 2020

Optimization of triazine nitriles as rhodesain inhibitors: structure-activity relationships, bioisosteric imidazopyridine nitriles, and X-ray crystal structure analysis with human cathepsin L

1 reference

12 December 2020

Plasma levels of cathepsins L, K, and V and risks of abdominal aortic aneurysms: a randomized population-based study.

1 reference

12 December 2020

Dynamin rings: not just for fission

1 reference

12 December 2020

Selective cancer targeting with prodrugs activated by histone deacetylases and a tumour-associated protease

1 reference

12 December 2020

The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.

1 reference

12 December 2020

Activity-based profiling of proteases

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12 December 2020

Prodrug-inspired probes selective to cathepsin B over other cysteine cathepsins

1 reference

12 December 2020

Development of a highly potent, selective, and cell-active inhibitor of cysteine cathepsin L-A hybrid design approach.

1 reference

12 December 2020

Cathepsin inhibition-induced lysosomal dysfunction enhances pancreatic beta-cell apoptosis in high glucose

1 reference

12 December 2020

Antimicrobial Peptide LL-37 Is Both a Substrate of Cathepsins S and K and a Selective Inhibitor of Cathepsin L.

1 reference

12 December 2020

Redundancy between Cysteine Cathepsins in Murine Experimental Autoimmune Encephalomyelitis

1 reference

12 December 2020

Cysteine cathepsins: their role in tumor progression and recent trends in the development of imaging probes

1 reference

12 December 2020

Multiple Cathepsins Promote Pro-IL-1β Synthesis and NLRP3-Mediated IL-1β Activation

1 reference

12 December 2020

Cathepsin L targeting in cancer treatment.

1 reference

12 December 2020

Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.

1 reference

12 December 2020

Cysteine cathepsin proteases: regulators of cancer progression and therapeutic response

1 reference

12 December 2020

An Active 32-kDa Cathepsin L Is Secreted Directly from HT 1080 Fibrosarcoma Cells and Not via Lysosomal Exocytosis

1 reference

12 December 2020

Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors

1 reference

12 December 2020

Caught in the act: the crystal structure of cleaved cathepsin L bound to the active site of Cathepsin L

1 reference

12 December 2020

Cathepsin L in tumor angiogenesis and its therapeutic intervention by the small molecule inhibitor KGP94.

1 reference

12 December 2020

Fluorine Scan of Inhibitors of the Cysteine Protease Human Cathepsin L: Dipolar and Quadrupolar Effects in the π-Stacking of Fluorinated Phenyl Rings on Peptide Amide Bonds

1 reference

12 December 2020

Expression of a zebrafish Cathepsin L gene in anterior mesendoderm and hatching gland

1 reference

12 December 2020

Loss of Cathepsin B and L Leads to Lysosomal Dysfunction, NPC-Like Cholesterol Sequestration and Accumulation of the Key Alzheimer's Proteins

1 reference

12 December 2020

Preclinical Evaluation of Cathepsin-Based Fluorescent Imaging System for Cytoreductive Surgery.

1 reference

12 December 2020

Inhibition of the Cysteine Protease Human Cathepsin L by Triazine Nitriles: Amide⋅⋅⋅Heteroarene π-Stacking Interactions and Chalcogen Bonding in the S3 Pocket.

1 reference

12 December 2020

Clinical significance of cathepsin L and cathepsin B in dilated cardiomyopathy.

1 reference

12 December 2020

Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L.

1 reference

12 December 2020

Prospective Evaluation of Free Energy Calculations for the Prioritization of Cathepsin L Inhibitors.

1 reference

12 December 2020

Cathepsin L and B as Potential Markers for Liver Fibrosis: Insights From Patients and Experimental Models.

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12 December 2020

The Future of Cysteine Cathepsins in Disease Management

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12 December 2020

Toolbox of Fluorescent Probes for Parallel Imaging Reveals Uneven Location of Serine Proteases in Neutrophils.

1 reference

12 December 2020

Optimization of a Protease Activated Probe for Optical Surgical Navigation.

1 reference

12 December 2020

The Multifaceted Role of the Lysosomal Protease Cathepsins in Kidney Disease.

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12 December 2020

Cysteine cathepsins in extracellular matrix remodeling: Extracellular matrix degradation and beyond.

1 reference

12 December 2020

Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors

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12 December 2020

Selective imaging of cathepsin L in breast cancer by fluorescent activity-based probes.

1 reference

12 December 2020

UniProt: a worldwide hub of protein knowledge

1 reference

12 December 2020

Clinical and translational pharmacology of the cathepsin K inhibitor odanacatib studied for osteoporosis

1 reference

12 December 2020

Cell penetrable, clickable and tagless activity-based probe of human cathepsin L

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12 December 2020

Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and Trypanosoma cruzi Cruzain

1 reference

12 December 2020

Cysteine Cathepsins in Tumor-Associated Immune Cells

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12 December 2020

10.3390/MOLECULES25030698

Identifiers

DOI

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:32041276%20AND%20SRC:MED&resulttype=core&format=json

7 April 2020

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:32041276%20AND%20SRC:MED&resulttype=core&format=json

7 April 2020

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