The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28117205 |
13 |
Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L. |
Baylor University |
10617079 |
3 |
Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis. |
The University Of Tokyo |
27994740 |
41 |
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain. |
Universitat Jaume I |
27214508 |
43 |
Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S. |
Cnrs |
27690432 |
75 |
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). |
Charles River Discovery Research Services |
26985310 |
8 |
Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome. |
Whitman College |
26985300 |
110 |
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry. |
University Of Bonn |
26462052 |
29 |
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L. |
Baylor University |
25865131 |
40 |
Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity. |
Hebei University Of Science & Technology |
24913985 |
73 |
SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H. |
Kurukshetra University |
25571794 |
40 |
Structure-based design and optimization of potent inhibitors of the adenoviral protease. |
Novartis Institute For Biomedical Research |
25411915 |
54 |
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors. |
Array Biopharma |
25375026 |
14 |
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis. |
Universidade Federal De S£O Carlos |
25365789 |
83 |
The discovery of potent, selective, and reversible inhibitors of the house dust mite peptidase allergen Der p 1: an innovative approach to the treatment of allergic asthma. |
Domainex |
25313316 |
20 |
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins. |
University Of Bonn |
24915003 |
34 |
Probing of primed and unprimed sites of calpains: Design, synthesis and evaluation of epoxysuccinyl-peptide derivatives as selective inhibitors. |
E£Tv£S Lor£Nd University (Elte) |
24592859 |
59 |
Cathepsin C inhibitors: property optimization and identification of a clinical candidate. |
Astrazeneca |
24524217 |
65 |
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates. |
Hokkaido University |
24642566 |
17 |
Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H. |
Kurukshetra University |
23252745 |
86 |
Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives. |
University Of Ljubljana |
24900293 |
78 |
Discovery of novel cyanamide-based inhibitors of cathepsin C. |
TBA |
19616430 |
120 |
Design of selective Cathepsin inhibitors. |
Astrazeneca |
16546382 |
100 |
Keto-1,3,4-oxadiazoles as cathepsin K inhibitors. |
Celera Genomics |
23122525 |
9 |
Fluorescent nitrile-based inhibitors of cysteine cathepsins. |
University Of Bonn |
21413808 |
170 |
Synopsis of some recent tactical application of bioisosteres in drug design. |
Bristol-Myers Squibb Pharmaceutical Research And Development |
24900408 |
4 |
Nonpeptidic lysosomal modulators derived from z-phe-ala-diazomethylketone for treating protein accumulation diseases. |
TBA |
22984809 |
111 |
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors. |
Astrazeneca |
22742641 |
113 |
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis. |
Astrazeneca |
22686657 |
60 |
Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F. |
University Of Bonn |
22950366 |
6 |
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta. |
Hokkaido University |
22858142 |
121 |
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition. |
Astrazeneca |
24900494 |
72 |
Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L. |
TBA |
22236250 |
16 |
Exploring activity cliffs in medicinal chemistry. |
Rheinische Friedrich-Wilhelms-Universit£T |
21128614 |
76 |
Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors. |
University Of Bonn |
20598553 |
38 |
Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors. |
Universit£ |
19709887 |
25 |
Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors. |
Universit£ |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University Of Florida |
18995931 |
16 |
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases. |
Federal University Of Alfenas |
19419206 |
77 |
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity. |
Ewha Womans University |
17535802 |
91 |
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. |
Merck Research Laboratories |
18420405 |
26 |
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB. |
University Of California |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
18289850 |
4 |
Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain. |
Pukyong National University |
18232656 |
30 |
Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors. |
University Of Messina |
18226527 |
80 |
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
Merck Frosst Centre For Therapeutic Research |
16185867 |
5 |
Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy. |
Santhera Pharmaceuticals |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University Of Queensland |
9784105 |
68 |
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption. |
Takeda Chemical Industries |
9667954 |
47 |
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I. |
Cephalon |
14980679 |
30 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid. |
Maxim Pharmaceuticals |
11055335 |
27 |
Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
| 11 |
Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L |
TBA |
22019466 |
13 |
Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors. |
National Chemical Laboratory (Csir-Ncl) |
21420760 |
8 |
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors. |
University Of Messina |
21849222 |
50 |
Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as inhibitors of cathepsin B. |
University Of Ljubljana |
20823284 |
9 |
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease. |
Boehringer Ingelheim (Canada) |
21227690 |
68 |
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka. |
Merck Research Laboratories |
21041084 |
102 |
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease. |
Merck Research Laboratories |
21030256 |
61 |
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors. |
Merck Research Laboratories |
20933415 |
50 |
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L. |
Baylor University |
20843687 |
60 |
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG. |
Merck Research Laboratories |
20690647 |
33 |
Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
Georgia Institute Of Technology |
19841155 |
29 |
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
Merck Research Laboratories |
20692829 |
21 |
Allicin and derivates are cysteine protease inhibitors with antiparasitic activity. |
University Of WüRzburg |
20594841 |
123 |
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors. |
Merck Research Laboratories |
19715342 |
19 |
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences. |
University Of Duisburg-Essen |
20153187 |
32 |
Dioxo-triazines as a novel series of cathepsin K inhibitors. |
Schering-Plough |
20149657 |
53 |
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. |
Schering-Plough |
19665376 |
48 |
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C. |
Merck Frosst Canada |
20089402 |
72 |
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors. |
Baylor University |
19769357 |
93 |
Structure-guided development of selective TbcatB inhibitors. |
University Of California |
| 10 |
Nonpeptidic inhibitors of recombinant human calpain I |
TBA |
| 2 |
Oligopresentation of protease inhibitors with β-cyclodextrin as template |
TBA |
| 22 |
Inhibition of human erythrocyte calpain I by novel quinolinecarboxamides |
TBA |
| 4 |
Design of a new selective cysteine protease inactivator and its mechanistic implications |
TBA |
19296600 |
14 |
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors. |
University Of Messina |
19231183 |
44 |
5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors. |
Astrazeneca |
18951789 |
1 |
Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides. |
University Of Toyama |
18789705 |
6 |
Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition. |
Bar-Ilan University |
18694642 |
6 |
Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position. |
The University Of Tennessee Health Science Center |
18571402 |
24 |
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts. |
Korea Research Institute Of Chemical Technology |
18313933 |
18 |
Substrate optimization for monitoring cathepsin C activity in live cells. |
Genomics Institute Of The Novartis Research Foundation |
17845856 |
1 |
Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs. |
LinköPing University |
17656088 |
15 |
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays. |
University Of Pennsylvania |
17544269 |
30 |
Primary amides as selective inhibitors of cathepsin K. |
Merck Frosst Centre For Therapeutic Research |
17196818 |
90 |
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases. |
The Genomics Institute Of The Novartis Research Foundation |
17049233 |
82 |
Design of potent inhibitors of human beta-secretase. Part 2. |
Pfizer |
16913717 |
42 |
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides. |
The University Of Tennessee Health Science Center |
16750630 |
28 |
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K. |
Celera Genomics |
16686537 |
165 |
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors. |
Celera |
16647256 |
16 |
Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors. |
Arpida |
16412635 |
4 |
A novel series of urea-based peptidomimetic calpain inhibitors. |
The University Of Tennessee Health Science Center |
16302794 |
53 |
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. |
Celera Genomics |
16290936 |
69 |
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? |
Glaxosmithkline |
16250645 |
35 |
Azepanone-based inhibitors of human cathepsin L. |
Glaxosmithkline |
16154747 |
37 |
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K. |
Merck Frosst Centre For Therapeutic Research |
15982880 |
86 |
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
15896958 |
32 |
Acyclic cyanamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
15837295 |
55 |
A structural screening approach to ketoamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
15780613 |
28 |
Novel and potent cyclic cyanamide-based cathepsin K inhibitors. |
Glaxosmithkline |
15634028 |
5 |
Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors. |
Université |
15588093 |
3 |
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors. |
Boehringer Ingelheim (Canada) |
15380210 |
18 |
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I). |
University Of Southern California |
15341970 |
59 |
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors. |
Eli Lilly |
15341947 |
57 |
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions. |
Glaxosmithkline |
15261289 |
38 |
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors. |
Merck Frosst Centre For Therapeutic Research |
15177446 |
41 |
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors. |
Glaxosmithkline |
14684338 |
44 |
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors. |
Eli Lilly |
14684304 |
41 |
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors. |
Amgen |
14592520 |
41 |
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B. |
Novartis Institute Of Biomedical Research |
12781193 |
36 |
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity. |
Ligand Pharmaceuticals |
12773044 |
18 |
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability. |
Abbott |
12617890 |
9 |
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics. |
University Of Tennessee Health Science Center |
12593666 |
30 |
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. |
Senju Pharmaceutical |
12431059 |
27 |
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides. |
National Research Council Of Canada |
12419374 |
45 |
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S. |
Currently Naeja Pharmaceutical |
12419373 |
18 |
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors. |
Currently Naeja Pharmaceutical |
12270191 |
36 |
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain. |
University Of California |
12270170 |
42 |
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors. |
Celera |
12213061 |
23 |
Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. |
University Of Gda£?Sk |
11992771 |
19 |
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors. |
Abbott |
11806719 |
61 |
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis. |
University Of California |
11741472 |
45 |
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design. |
Novartis Pharmaceuticals |
11356112 |
175 |
Potent reversible inhibitors of the protein tyrosine phosphatase CD45. |
Astrazeneca Pharmaceuticals |
11311061 |
40 |
Azepanone-based inhibitors of human and rat cathepsin K. |
Glaxosmithkline |
11141092 |
85 |
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L. |
Merck Frosst Centre For Therapeutic Research |
11086714 |
10 |
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position. |
The University Of Tennessee Health Science Center |
11012026 |
18 |
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors. |
Knoll |
10508448 |
11 |
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites. |
Brown University |
9873610 |
48 |
Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease. |
Boehringer Ingelheim (Canada) |
9873596 |
18 |
P2-proline-derived inhibitors of calpain I. |
Cephalon |
9871780 |
85 |
Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams. |
Boehringer Ingelheim (Canada) |
9871680 |
5 |
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids. |
Proscript |
9733481 |
31 |
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K. |
Smithkline Beecham Pharmaceuticals |
9406601 |
109 |
Peptidomimetic inhibitors of the human cytomegalovirus protease. |
Boehringer Ingelheim |
8831774 |
261 |
Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases. |
Georgia Institute Of Technology |
7650671 |
15 |
Vinyl sulfones as mechanism-based cysteine protease inhibitors. |
Khepri Pharmaceuticals |
28122457 |
12 |
Idiopathic Pulmonary Fibrosis: Current Status, Recent Progress, and Emerging Targets. |
Taipei Medical University |
21635213 |
8 |
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II. |
Balikesir University |
| 16 |
Design, synthesis and evaluation of trisubstituted thiazoles targeting plasmodium falciparum cysteine proteases |
University, Mississippi |
15608078 |
35 |
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. |
Abbott Laboratories |
11805207 |
8 |
Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties. |
Abbott Laboratories |
10455251 |
10 |
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. |
Roche Bioscience |