The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28287264 |
38 |
Prospective Evaluation of Free Energy Calculations for the Prioritization of Cathepsin L Inhibitors. |
Roche Pharmaceutical Research and Early Development (Pred) |
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 |
27890381 |
2 |
Evaluation of dipeptide nitriles as inhibitors of rhodesain, a major cysteine protease of Trypanosoma brucei. |
Johannes Gutenberg University |
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 |
26881908 |
13 |
De Novo Design at the Edge of Chaos. |
Swiss Federal Institute of Technology (Eth) |
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 |
26280490 |
17 |
Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors. |
National Institute of Chemistry |
25571794 |
40 |
Structure-based design and optimization of potent inhibitors of the adenoviral protease. |
Novartis Institute For Biomedical Research |
25375026 |
14 |
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis. |
Universidade Federal De S£O Carlos |
25313327 |
11 |
Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
Eli Lilly |
25313316 |
20 |
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins. |
University of Bonn |
24592859 |
59 |
Cathepsin C inhibitors: property optimization and identification of a clinical candidate. |
Astrazeneca |
23145854 |
9 |
Principles and applications of halogen bonding in medicinal chemistry and chemical biology. |
Eberhard-Karls 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 |
23084902 |
116 |
Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement. |
Boehringer Ingelheim Pharmaceuticals |
23167554 |
28 |
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice. |
Universidade Federal De Pernambuco |
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 |
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 |
22591648 |
78 |
Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and V. |
Universidade Federal De S£O Carlos |
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£ |
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 |
18499453 |
8 |
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype. |
University of Pennsylvania |
18375120 |
45 |
New chemotypes for cathepsin K inhibitors. |
Novartis Institutes For Biomedical Research |
18060772 |
5 |
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor. |
University of Pennsylvania |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
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 |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
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 |
21420760 |
8 |
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors. |
University of Messina |
21733692 |
56 |
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent. |
Glaxosmithkline |
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 |
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 |
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 |
| 22 |
Inhibition of human erythrocyte calpain I by novel quinolinecarboxamides |
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 |
19124252 |
141 |
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity. |
Medivir |
18783943 |
35 |
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2. |
Novartis Institutes For Biomedical Research |
18707091 |
14 |
Effect of cathepsin K inhibitors on bone resorption. |
Novartis Institutes For Biomedical Research |
18701300 |
55 |
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides. |
University of Leipzig |
18662880 |
56 |
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors. |
Novartis Institutes For Biomedical Research |
18572405 |
85 |
Discovery of selective and nonpeptidic cathepsin S inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
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 |
16750630 |
28 |
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K. |
Celera Genomics |
16647256 |
16 |
Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors. |
Arpida |
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 |
16216498 |
2 |
Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor. |
University of WüRzburg |
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 |
15537340 |
27 |
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K. |
Novartis Institutes For Biomedical Research |
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 |
12781182 |
81 |
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents. |
Novartis Pharma |
12467634 |
67 |
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors. |
Currently Naeja Pharmaceutical |
12431059 |
27 |
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides. |
National Research Council of Canada |
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 |
12036343 |
24 |
Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors. |
TBA |
11992771 |
19 |
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors. |
Abbott |
11814800 |
14 |
Design and synthesis of dual inhibitors for matrix metalloproteinase and cathepsin. |
Organon K.K. |
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 |
32631567 |
13 |
Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors. |
Federal University of S£O Carlos |
32336669 |
6 |
Cytotoxicity of 4-substituted quinoline derivatives: Anticancer and antileishmanial potential. |
Universidade De Mogi Das Cruzes (Umc) |
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 |
10937745 |
7 |
Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B. |
Queen'S University Belfast |
31145622 |
91 |
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors. |
National Institute of Biological Sciences (Nibs) |
29400967 |
136 |
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
Bristol-Myers Squibb |
30773420 |
16 |
Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes. |
Jilin University |
32125159 |
60 |
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity. |
Texas A&M University |
31158752 |
6 |
Enhanced tumor retention of NTSR1-targeted agents by employing a hydrophilic cysteine cathepsin inhibitor. |
University of Nebraska Medical Center |
9733481 |
31 |
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K. |
Smithkline Beecham Pharmaceuticals |
31714776 |
30 |
Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis. |
University of Messina |
31539239 |
33 |
Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and |
The University of Jordan |
31361135 |
17 |
Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity? |
University of S£O Paulo |
30455147 |
7 |
Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments. |
University of Houston |
31561938 |
64 |
Synthesis and structure-activity relationship of nitrile-based cruzain inhibitors incorporating a trifluoroethylamine-based P2 amide replacement. |
Universidade De S£O Paulo |
24364476 |
9 |
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L. |
University of California |
23608763 |
38 |
Chalcones, inhibitors for topoisomerase I and cathepsin B and L, as potential anti-cancer agents. |
Cha University |
23562595 |
98 |
Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors? |
National Institute of Biology |
23540644 |
59 |
Small-molecule inhibitors of cathepsin L incorporating functionalized ring-fused molecular frameworks. |
Baylor University |
7650671 |
15 |
Vinyl sulfones as mechanism-based cysteine protease inhibitors. |
Khepri Pharmaceuticals |
30029081 |
31 |
New aziridine-based inhibitors of cathepsin L-like cysteine proteases with selectivity for the Leishmania cysteine protease LmCPB2.8. |
Johannes Gutenberg-Universit£T Mainz |
29272750 |
15 |
Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S. |
Cnrs Upr 4301 |
30049585 |
73 |
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs. |
Universit£ |
30037754 |
64 |
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates. |
Universitat Jaume I |
29615344 |
101 |
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins. |
Irbm Science Park |
29503024 |
138 |
Cathepsin B inhibitors: Further exploration of the nitroxoline core. |
University of Ljubljana |
29650289 |
54 |
Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability. |
University of Michigan |
29590751 |
80 |
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design. |
Eth Zurich |
29590750 |
58 |
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors. |
Eth Zurich |
28720327 |
17 |
Asymmetric synthesis and evaluation of epoxy-?-acyloxycarboxamides as selective inhibitors of cathepsin L. |
Federal University of S£O Carlos |
28763614 |
48 |
Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs). |
University of Messina |
22397393 |
5 |
Synthesis of a-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase. |
Institute For Advanced Studies In Basic Sciences (Iasbs) |
21635213 |
8 |
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II. |
Balikesir University |
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 |
10455251 |
10 |
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. |
Roche Bioscience |
1397049 |
24 |
NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists. |
Novo Nordisk |
15734651 |
135 |
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists. |
National Institutes of Health |