Calpain inhibitors: a survey of compounds reported in the patent and scientific literature

scientific article published on 24 March 2011

Calpain inhibitors: a survey of compounds reported in the patent and scientific literature is …
instance of (P31):
scholarly articleQ13442814
review articleQ7318358

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P356DOI10.1517/13543776.2011.568480
P698PubMed publication ID21434837

P2093author name stringIsaac O Donkor
P2860cites workAmelioration of retinal degeneration and proteolysis in acute ocular hypertensive rats by calpain inhibitor ((1S)-1-((((1S)-1-benzyl-3-cyclopropylamino-2,3-di-oxopropyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester.Q54592052
Novel dual inhibitors of calpain and lipid peroxidation with enhanced cellular activity.Q55470694
Synthesis of a 24-Membered Cyclic Peptide-Biphenyl HybridQ58035473
Isolation and structure elucidation of two new calpain inhibitors from Streptomyces griseusQ71991558
A Ca(2+) switch aligns the active site of calpainQ27638321
Development of calpain-specific inactivators by screening of positional scanning epoxide librariesQ27643516
Cocrystal Structures of Primed Side-Extending α-Ketoamide Inhibitors Reveal Novel Calpain-Inhibitor Aromatic Interactions #Q27651571
Calcium-bound structure of calpain and its mechanism of inhibition by calpastatinQ27652954
Calpains and muscular dystrophiesQ28144209
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailabilityQ28207370
The novel calpain inhibitor SJA6017 improves functional outcome after delayed administration in a mouse model of diffuse brain injuryQ28207556
Proteases universally recognize beta strands in their active sitesQ28238770
Structure, activation, and biology of calpainQ28241296
Determination of peptide substrate specificity for mu-calpain by a peptide library-based approach: the importance of primed side interactionsQ28276503
Molecular mode of action of a covalently inhibiting peptidomimetic on the human calpain protease coreQ28596594
Comprehensive behavioral phenotyping of calpastatin-knockout miceQ30483897
Novel 6-hydroxy-3-morpholinones as cornea permeable calpain inhibitorsQ30884886
Exploration of orally available calpain inhibitors: peptidyl alpha-ketoamides containing an amphiphile at P3 siteQ30990832
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 positionQ31585865
Exploration of cornea permeable calpain inhibitors as anticataract agentsQ33186330
Synthesis of a small library of diketopiperazines as potential inhibitors of calpain.Q33215176
Identification of a novel calpain inhibitor using phage displayQ33217943
Design and synthesis of 4-aryl-4-oxobutanoic acid amides as calpain inhibitorsQ33388021
Evaluation of a novel calpain inhibitor as a treatment for cataractQ33417055
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activityQ33439900
Neuroprotection with delayed calpain inhibition after transient forebrain ischemiaQ33839760
A survey of calpain inhibitorsQ34060656
Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitorsQ34194374
Investigation into the P3 binding domain of m-calpain using photoswitchable diazo- and triazene-dipeptide aldehydes: new anticataract agentsQ34627750
Calpains as potential anti-cancer targetsQ34793288
Calpains and diseaseQ36156260
Calpain inhibition: a therapeutic strategy targeting multiple disease states.Q36393620
Novel dual inhibitors of calpain and lipid peroxidationQ44941185
Crystal structures of calpain-E64 and -leupeptin inhibitor complexes reveal mobile loops gating the active siteQ45112642
Reduction of myocardial infarction by calpain inhibitors A-705239 and A-705253 in isolated perfused rabbit heartsQ45171362
Ritonavir does not inhibit calpain in vitroQ45209533
Synthesis and evaluation of eight-membered cyclic pseudo-dipeptidesQ45209605
Human immunodeficiency virus (HIV)-induced neurotoxicity: roles for the NMDA receptor subtypes.Q45420727
Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors.Q46161964
Solid-phase combinatorial synthesis of peptide-biphenyl hybrids as calpain inhibitorsQ46208927
A new epicatechin gallate and calpain inhibitory activity from Orostachys japonicusQ46269852
Calpain inhibition and insulin action in cultured human muscle cellsQ46464191
Synthesis and biological evaluation of chromone carboxamides as calpain inhibitorsQ46505388
Synthesis, biological evaluation and molecular modelling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors.Q46525630
Chlortetracycline and demeclocycline inhibit calpains and protect mouse neurons against glutamate toxicity and cerebral ischemiaQ46642858
Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophyQ46721993
Design and synthesis of 4-quinolinone 2-carboxamides as calpain inhibitorsQ46892708
Calpain inhibitor MDL-28170 reduces the functional and structural deterioration of corpus callosum following fluid percussion injuryQ48121937
Calpastatin levels affect calpain activation and calpain proteolytic activity in APP transgenic mouse model of Alzheimer's diseaseQ48162315
Inhibition of calpain-mediated cell death by a novel peptide inhibitorQ48427996
VE-cadherin-derived cell-penetrating peptide, pVEC, with carrier functionsQ48779585
A novel dual inhibitor of calpains and lipid peroxidation (BN82270) rescues the cochlea from sound trauma.Q50457945
Implication of calpain in neuronal apoptosis. A possible regulation of Alzheimer's diseaseQ36554860
Involvement of calpain activation in neurodegenerative processes.Q36588397
The therapeutic potential of the calpain family: new aspects.Q36601917
The calpains: modular designs and functional diversityQ36672357
Calpains and their multiple roles in diabetes mellitusQ36675894
Calpain activity in retinal degeneration.Q36685247
Calpain-mediated regulation of platelet signaling pathwaysQ36783478
Mechanistic role of calpains in postischemic neurodegenerationQ37029897
The role of calcium-activated protease calpain in experimental retinal pathologyQ37113015
Calpain as a potential therapeutic target in Parkinson's diseaseQ37232901
Calpain-mediated signaling mechanisms in neuronal injury and neurodegenerationQ37237452
Calpain as a therapeutic target in traumatic brain injuryQ37686765
Calpains: attractive targets for the development of synthetic inhibitorsQ37694672
Regulation of calpain-2 in neurons: implications for synaptic plasticityQ37798196
The role of calpain in diabetes-associated platelet hyperactivation.Q37798968
Expanding members and roles of the calpain superfamily and their genetically modified animalsQ37804653
Evidence for calpain-mediated androgen receptor cleavage as a mechanism for androgen independenceQ40073673
A new cell-permeable calpain inhibitor.Q40223788
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamidesQ40242934
Calpain inhibitors and antioxidants act synergistically to prevent cell necrosis: effects of the novel dual inhibitors (cysteine protease inhibitor and antioxidant) BN 82204 and its pro-drug BN 82270.Q40245964
Exploration of orally available calpain inhibitors 2: peptidyl hemiacetal derivativesQ40264619
Treatment of rats with calpain inhibitors prevents sepsis-induced muscle proteolysis independent of atrogin-1/MAFbx and MuRF1 expressionQ40321294
1,2-Benzothiazine 1,1-dioxide alpha-ketoamide analogues as potent calpain I inhibitorsQ40580239
Calpastatin exon 1B-derived peptide, a selective inhibitor of calpain: enhancing cell permeability by conjugation with penetratin.Q40652159
Calpain is involved in the HIV replication from the latently infected OM10.1 cellsQ40659344
Cellular uptake of an alpha-helical amphipathic model peptide with the potential to deliver polar compounds into the cell interior non-endocyticallyQ40996709
HIV-1 Tat C-terminus is cleaved by calpain 1: implication for Tat-mediated neurotoxicityQ41765004
Direct effect of human immunodeficiency virus protease inhibitors on neutrophil function and apoptosis via calpain inhibitionQ41829112
Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 positionQ41846613
Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacidsQ41940642
A novel series of urea-based peptidomimetic calpain inhibitors.Q42166244
Calpain inhibition by alpha-ketoamide and cyclic hemiacetal inhibitors revealed by X-ray crystallography.Q42688028
Molecular modeling studies of peptide inhibitors highlight the importance of conformational prearrangement for inhibition of calpainQ43054948
The novel calpain inhibitor A-705253 potently inhibits oligomeric beta-amyloid-induced dynamin 1 and tau cleavage in hippocampal neurons.Q43213857
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitorsQ43507699
Calpain inhibitor, SJA6017, reduces the rate of formation of selenite cataract in ratsQ43681124
Synthesis of a reported calpain inhibitor isolated from Streptomyces griseus.Q43733834
1,2-Benzothiazine 1,1-dioxide P(2)-P(3) peptide mimetic aldehyde calpain I inhibitorsQ43755661
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitorsQ43981452
Ritonavir inhibition of calcium-activated neutral proteasesQ43984010
Exploration of peptidyl hydrazones as water-soluble calpain inhibitorsQ44011778
Structural determinants of the calpain inhibitory activity of calpastatin peptide B27-WT.Q44261564
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitorQ44320330
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimeticsQ44345391
Poly-arginine-fused calpastatin peptide, a living cell membrane-permeable and specific inhibitor for calpainQ44563746
Calpain inhibitors, a treatment for Alzheimer's disease: position paperQ44591036
Design, synthesis, molecular modeling studies, and calpain inhibitory activity of novel alpha-ketoamides incorporating polar residues at the P1'-positionQ44706434
Studies on aromatic compounds: inhibition of calpain I by biphenyl derivatives and peptide-biphenyl hybrids.Q44882624
P433issue5
P407language of work or nameEnglishQ1860
P921main subjectscientific literatureQ12042160
P304page(s)601-636
P577publication date2011-03-24
P1433published inExpert Opinion on Therapeutic PatentsQ5421213
P1476titleCalpain inhibitors: a survey of compounds reported in the patent and scientific literature
P478volume21