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

scientific article published on 06 February 2020

A Review of Small Molecule Inhibitors and Functional Probes of Human Cathepsin L is …
instance of (P31):
review articleQ7318358
scholarly articleQ13442814

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P356DOI10.3390/MOLECULES25030698
P932PMC publication ID7038230
P698PubMed publication ID32041276

P50authorSanjai KumarQ55838184
P2093author name stringDibyendu Dana
P2860cites workStructural basis for the recognition and cleavage of histone H3 by cathepsin LQ24293301
The place of human gamma-trace (cystatin C) amongst the cysteine proteinase inhibitorsQ24300962
The proteome of lysosomesQ24303943
Cystatin F is a glycosylated human low molecular weight cysteine proteinase inhibitorQ24312357
Structural and functional characterization of two allelic variants of human cystatin D sharing a characteristic inhibition spectrum against mammalian cysteine proteinasesQ24319696
L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and LQ24531160
Structure of human procathepsin L reveals the molecular basis of inhibition by the prosegmentQ24561952
Secreted cathepsin L generates endostatin from collagen XVIIIQ24599981
Major histocompatibility complex class II-associated p41 invariant chain fragment is a strong inhibitor of lysosomal cathepsin LQ24678337
Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitorsQ26771736
Cysteine cathepsins: their role in tumor progression and recent trends in the development of imaging probesQ26827307
Cysteine cathepsins: from structure, function and regulation to new frontiersQ26860406
Inhibition mechanism of cathepsin L-specific inhibitors based on the crystal structure of papain-CLIK148 complexQ27620728
Azepanone-based inhibitors of human and rat cathepsin KQ27631249
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptidesQ27639963
Crystal structure of the parasite protease inhibitor chagasin in complex with a host target cysteine proteaseQ27645572
Exploring inhibitor binding at the S' subsites of cathepsin LQ27649866
Crystal structure and silica condensing activities of silicatein α–cathepsin L chimerasQ27650199
Dipeptidyl nitrile inhibitors of Cathepsin LQ27655858
A combined crystallographic and molecular dynamics study of cathepsin L retrobinding inhibitorsQ27657460
Structural basis for reversible and irreversible inhibition of human cathepsin L by their respective dipeptidyl glyoxal and diazomethylketone inhibitorsQ27664560
Systematic investigation of halogen bonding in protein-ligand interactionsQ27666413
Halogen bonding at the active sites of human cathepsin L and MEK1 kinase: efficient interactions in different environmentsQ27673373
Optimization of triazine nitriles as rhodesain inhibitors: structure-activity relationships, bioisosteric imidazopyridine nitriles, and X-ray crystal structure analysis with human cathepsin LQ27684569
Caught in the act: the crystal structure of cleaved cathepsin L bound to the active site of Cathepsin LQ27704273
CystatinsQ28180897
The crystal structure of human cathepsin L complexed with E-64Q28237390
The identification of active forms of cysteine proteinases in Kirsten-virus-transformed mouse fibroblasts by use of a specific radiolabelled inhibitorQ28342303
The use of benzyloxycarbonyl[125I]iodotyrosylalanyldiazomethane as a probe for active cysteine proteinases in human tissuesQ28354320
The design of peptidyldiazomethane inhibitors to distinguish between the cysteine proteinases calpain II, cathepsin L and cathepsin BQ28359859
Clinical significance of cathepsin L and cathepsin B in dilated cardiomyopathy.Q50959078
Inhibition of the Cysteine Protease Human Cathepsin L by Triazine Nitriles: Amide⋅⋅⋅Heteroarene π-Stacking Interactions and Chalcogen Bonding in the S3 Pocket.Q51251348
Preclinical Evaluation of Cathepsin-Based Fluorescent Imaging System for Cytoreductive Surgery.Q52950183
Cathepsin-L contributes to cardiac repair and remodelling post-infarction.Q54627475
Selective imaging of cathepsin L in breast cancer by fluorescent activity-based probes.Q55023666
Lysosomal, cytoskeletal, and metabolic alterations in cardiomyopathy of cathepsin L knockout miceQ56993719
pH-induced conformational transitions of the propeptide of human cathepsin L. A role for a molten globule state in zymogen activationQ57220930
UniProt: a worldwide hub of protein knowledgeQ58611634
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei InhibitorsQ58842291
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 BondsQ61066401
Aziridide-Based Inhibitors of Cathepsin L: Synthesis, Inhibition Activity, and Docking StudiesQ61066429
Rational Design of Aziridine-Containing Cysteine Protease Inhibitors with Improved Potency: Studies on Inhibition MechanismQ61066430
New Peptidic Cysteine Protease Inhibitors Derived from the Electrophilic α-Amino Acid Aziridine-2,3-dicarboxylic AcidQ61066437
Crystallization and preliminary X-ray diffraction studies of human procathepsin LQ64038879
Cathepsin L deficiency reduces diet-induced atherosclerosis in low-density lipoprotein receptor-knockout mice.Q64885339
Reactions between dipeptidyl peptidase IV and diacyl hydroxylamines: mechanistic investigationsQ69370125
Evidence that aspartic proteinase is involved in the proteolytic processing event of procathepsin L in lysosomesQ69505828
Characterization of human cathepsin L promoter and identification of binding sites for NF-Y, Sp1 and Sp3 that are essential for its activityQ28366301
Acquisition of T regulatory function in cathepsin L-inhibited T cells by eye-derived CTLA-2alpha during inflammatory conditionsQ28505057
Lysosomal enzyme phosphorylation. Recognition of a protein-dependent determinant allows specific phosphorylation of oligosaccharides present on lysosomal enzymesQ28573945
A cathepsin L isoform that is devoid of a signal peptide localizes to the nucleus in S phase and processes the CDP/Cux transcription factorQ28592058
Acceleration of polycystic kidney disease progression in cpk mice carrying a deletion in the homeodomain protein Cux1Q28594958
Cathepsin L: critical role in Ii degradation and CD4 T cell selection in the thymusQ28613227
N-peptidyl-O-carbamoyl amino acid hydroxamates: irreversible inhibitors for the study of the S2' specificity of cysteine proteinases.Q30321430
Tight-binding inhibition of cathepsin S by cystatinsQ30321471
Podocyte biology and pathogenesis of kidney diseaseQ30424169
In situ hybridization screen in zebrafish for the selection of genes encoding secreted proteins.Q30781073
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.Q31805262
Substrate profiling of cysteine proteases using a combinatorial peptide library identifies functionally unique specificitiesQ33235638
Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin LQ33327656
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitorsQ33525418
Novel peptidyl aryl vinyl sulfones as highly potent and selective inhibitors of cathepsins L and B.Q33638719
Roles for cathepsins S, L, and B in insulitis and diabetes in the NOD mouseQ33653550
Finding enzymes that are actively involved in cancerQ33664242
Cathepsin L and B as Potential Markers for Liver Fibrosis: Insights From Patients and Experimental Models.Q33920338
The actin cytoskeleton of kidney podocytes is a direct target of the antiproteinuric effect of cyclosporine A.Q33943247
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.Q34009651
Cathepsin L is essential for onset of autoimmune diabetes in NOD miceQ34014524
Strategies for discovering and derisking covalent, irreversible enzyme inhibitorsQ34023143
Dilated cardiomyopathy in mice deficient for the lysosomal cysteine peptidase cathepsin L.Q34028619
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.Q34051627
Functional imaging of proteases: recent advances in the design and application of substrate-based and activity-based probesQ34078522
The resurgence of covalent drugsQ34174891
Activity-based probes for protein tyrosine phosphatasesQ34330552
The lysosome turns fiftyQ34447595
Distinct roles for cysteine cathepsin genes in multistage tumorigenesisQ34471105
Cysteine cathepsins and the cutting edge of cancer invasionQ34605340
Biogenesis and proteolytic processing of lysosomal DNase IIQ34630331
Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?Q34657266
Cathepsin inhibition-induced lysosomal dysfunction enhances pancreatic beta-cell apoptosis in high glucoseQ35019204
Potent and selective inactivation of proteinases with N-peptidyl-O-acylhydroxylaminesQ69510216
Dipeptidylpeptidase IV--inactivation with N-peptidyl-O-aroyl hydroxylaminesQ69931019
Cathepsin B-related proteases in the insulin secretory granuleQ70213567
N,O-diacylhydroxylamines as enzyme-activated inhibitors for serine proteasesQ70265656
Novel N-peptidyl-O-acyl hydroxamates: selective inhibitors of cysteine proteinasesQ70481053
In vitro activation of pro-cathepsin B by three serine proteinases: leucocyte elastase, cathepsin G, and the urokinase-type plasminogen activatorQ70494598
Potency and selectivity of the cathepsin L propeptide as an inhibitor of cysteine proteasesQ71185919
Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivoQ71348149
Aziridine Analogs of [[trans-(Epoxysuccinyl)-L-leucyl]amino]-4-guanidinobutane (E-64) as Inhibitors of Cysteine ProteasesQ71963258
Structure based development of novel specific inhibitors for cathepsin L and cathepsin S in vitro and in vivoQ73077056
Relative rates of Michael reactions of 2'-(phenethyl)thiol with vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides relevant to vinyl sulfonyl cysteine protease inhibitorsQ73428095
Distinct roles of cathepsin K and cathepsin L in osteoclastic bone resorptionQ74095795
Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin BQ74151522
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorptionQ77449793
Osteoclastic bone degradation and the role of different cysteine proteinases and matrix metalloproteinases: differences between calvaria and long boneQ80182629
Parkinson's disease involves autophagy and abnormal distribution of cathepsin LQ82753888
Decreased arthritis severity in cathepsin L-deficient mice is attributed to an impaired T helper cell compartmentQ84312844
Microarray-guided discovery of two-photon (2P) small molecule probes for live-cell imaging of cysteinyl cathepsin activitiesQ84404193
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituentQ84512759
A novel photoaffinity-based probe for selective detection of cathepsin L active formQ85356487
Expression of a zebrafish Cathepsin L gene in anterior mesendoderm and hatching glandQ88564623
Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and Trypanosoma cruzi CruzainQ90189749
Cysteine Cathepsins in Tumor-Associated Immune CellsQ90290679
Clinical and translational pharmacology of the cathepsin K inhibitor odanacatib studied for osteoporosisQ91134523
Cell penetrable, clickable and tagless activity-based probe of human cathepsin LQ91893901
Selective cancer targeting with prodrugs activated by histone deacetylases and a tumour-associated proteaseQ39066800
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatBQ39412077
Real-time monitoring of drug releaseQ39753844
Cathepsin L expression is up-regulated by hypoxia in human melanoma cells: role of its 5'-untranslated region.Q39998490
Increased expression and activity of nuclear cathepsin L in cancer cells suggests a novel mechanism of cell transformation.Q40080774
Toolbox of Fluorescent Probes for Parallel Imaging Reveals Uneven Location of Serine Proteases in Neutrophils.Q40149159
Global analysis of protein tyrosine phosphatase activity with ultra-sensitive fluorescent probes.Q40247455
Antiinflammatory and immunosuppressive activity of sialostatin L, a salivary cystatin from the tick Ixodes scapularis.Q40268385
Activity-based probes that target diverse cysteine protease familiesQ40330849
Podocyte migration during nephrotic syndrome requires a coordinated interplay between cathepsin L and alpha3 integrinQ40545315
Lysosomal acid phosphatase is transported to lysosomes via the cell surfaceQ40822199
Antimicrobial Peptide LL-37 Is Both a Substrate of Cathepsins S and K and a Selective Inhibitor of Cathepsin L.Q41056650
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotypeQ41265835
Inhibition of cysteine proteinases in lysosomes and whole cellsQ41613431
Cystatin-like cysteine proteinase inhibitors from human liverQ41868134
Molecular docking of cathepsin L inhibitors in the binding site of papainQ41889166
E64 [trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane] analogues as inhibitors of cysteine proteinases: investigation of S2 subsite interactionsQ42084932
Cathepsin L inactivates human trypsinogen, whereas cathepsin L-deletion reduces the severity of pancreatitis in mice.Q42273053
Multiple Cathepsins Promote Pro-IL-1β Synthesis and NLRP3-Mediated IL-1β ActivationQ42428279
Quantification of cathepsins B and L in cellsQ42537421
Potent and selective inactivation of cysteine proteinases with N-peptidyl-O-acyl hydroxylaminesQ42804251
Dynamic imaging of protease activity with fluorescently quenched activity-based probes.Q42806191
Human low-Mr kininogen contains three copies of a cystatin sequence that are divergent in structure and in inhibitory activity for cysteine proteinasesQ42852932
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.Q42864053
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.Q42981725
Cysteine protease inhibition by azapeptide estersQ43428037
Splice variants of human cathepsin L mRNA show different expression ratesQ43840167
Impaired cathepsin L gene expression in skeletal muscle is associated with type 2 diabetesQ44564070
Cathepsin L is crucial for a Th1-type immune response during Leishmania major infection.Q44862470
Cathepsin L-deficient mice exhibit abnormal skin and bone development and show increased resistance to osteoporosis following ovariectomyQ44904231
Comprehensive search for cysteine cathepsins in the human genomeQ44935351
Synthesis and antiplasmodial activity of a cysteine protease-inhibiting biotinylated aziridine-2,3-dicarboxylateQ44935373
Peptidyl (acyloxy)methanes as quiescent affinity labels for cysteine proteinasesQ45304042
Optimization of a Protease Activated Probe for Optical Surgical Navigation.Q45933355
A cathepsin L-specific inhibitor preferentially inhibits degradation of autophagosomal LC3 and GABARAP in HeLa and Huh-7 cells.Q45964739
Noninvasive optical imaging of cysteine protease activity using fluorescently quenched activity-based probes.Q46006433
Vinyl Sulfones as Mechanism-Based Cysteine Protease InhibitorsQ46097132
Lysosomal cysteine peptidase cathepsin L protects against cardiac hypertrophy through blocking AKT/GSK3beta signalingQ46190199
High glucose reduces cathepsin L activity and impairs invasion of circulating progenitor cellsQ46488605
Azepanone-based inhibitors of human cathepsin L.Q46775748
Cell type-specific functions of the lysosomal protease cathepsin L in the heartQ46945604
Zebrafish KLF4 is essential for anterior mesendoderm/pre-polster differentiation and hatchingQ47073901
The Multifaceted Role of the Lysosomal Protease Cathepsins in Kidney Disease.Q47171560
Prospective Evaluation of Free Energy Calculations for the Prioritization of Cathepsin L Inhibitors.Q48045269
Autophagic neuron deathQ48745538
Cysteine cathepsins in extracellular matrix remodeling: Extracellular matrix degradation and beyond.Q50057748
Lysosomal cysteine proteases (cathepsins): promising drug targets.Q35055535
Cathepsin L in secretory vesicles functions as a prohormone-processing enzyme for production of the enkephalin peptide neurotransmitter.Q35234967
Redundancy between Cysteine Cathepsins in Murine Experimental Autoimmune EncephalomyelitisQ35663877
Protease-activated drug developmentQ35811508
Complete and limited proteolysis in cell cycle progression.Q35836775
An Active 32-kDa Cathepsin L Is Secreted Directly from HT 1080 Fibrosarcoma Cells and Not via Lysosomal ExocytosisQ35870565
Proteolytic processing of dynamin by cytoplasmic cathepsin L is a mechanism for proteinuric kidney diseaseQ35916157
Multiple roles for cysteine cathepsins in cancerQ35946770
Loss of Cathepsin B and L Leads to Lysosomal Dysfunction, NPC-Like Cholesterol Sequestration and Accumulation of the Key Alzheimer's ProteinsQ36208265
Cathepsin L targeting in cancer treatment.Q36218199
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.Q36470838
Cysteine cathepsins: multifunctional enzymes in cancerQ36600996
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.Q36775345
Homing and engraftment of progenitor cells: a prerequisite for cell therapyQ37096297
Plasma levels of cathepsins L, K, and V and risks of abdominal aortic aneurysms: a randomized population-based study.Q37118040
Activity-based protein profiling: from enzyme chemistry to proteomic chemistryQ37119021
Dynamin rings: not just for fissionQ37315491
Regulation of cell proliferation and differentiation in the kidney.Q37359013
Transformation-dependent secretion of a low molecular weight protein by murine fibroblastsQ37588423
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.Q37598633
Identification of a 31,500 molecular weight islet cell protease as cathepsin BQ37613242
Cathepsin L, target in cancer treatment?Q37643875
Enhancing the outcome of cell therapy for cardiac repair: progress from bench to bedside and backQ37677400
Cathepsin L in tumor angiogenesis and its therapeutic intervention by the small molecule inhibitor KGP94.Q37735722
Homing of progenitor cells to ischemic tissuesQ37784827
Specialized roles for cysteine cathepsins in health and disease.Q37797839
Activity-based profiling of proteasesQ38218232
Cysteine cathepsin proteases: regulators of cancer progression and therapeutic responseQ38644547
The Future of Cysteine Cathepsins in Disease ManagementQ38664101
Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L.Q38766492
Development of a highly potent, selective, and cell-active inhibitor of cysteine cathepsin L-A hybrid design approach.Q38969005
Prodrug-inspired probes selective to cathepsin B over other cysteine cathepsinsQ38983504
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitorQ39035003
P275copyright licenseCreative Commons Attribution 4.0 InternationalQ20007257
P6216copyright statuscopyrightedQ50423863
P433issue3
P577publication date2020-02-06
P1433published inMoleculesQ151332
P1476titleA Review of Small Molecule Inhibitors and Functional Probes of Human Cathepsin L
P478volume25

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cites work (P2860)
Q108502694Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development
Q96017828Cathepsin L-selective inhibitors: A potentially promising treatment for COVID-19 patients
Q94672407Coumarin as a structural component of substrates and probes for serine and cysteine proteases
Q96352766Inhibitors of SARS-CoV-2 Entry: Current and Future Opportunities
Q99637358Potential clinical drugs as covalent inhibitors of the priming proteases of the spike protein of SARS-CoV-2
Q98389656SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells

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