The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27777011 |
92 |
Variation of the aryl substituent on the piperazine ring within the 4-(piperazin-1-yl)-2,6-di(pyrrolidin-1-yl)pyrimidine scaffold unveils potent, non-competitive inhibitors of the inflammatory caspases. |
Depaul University |
26422006 |
13 |
Inhibiting the Inflammasome: A Chemical Perspective. |
The University of Manchester |
26641525 |
6 |
Azaphilones from an Acid Mine Extremophile Strain of a Pleurostomophora sp. |
Memorial Sloan-Kettering Cancer Center |
25418070 |
2 |
Electrophilic warhead-based design of compounds preventing NLRP3 inflammasome-dependent pyroptosis. |
Universit£ |
25358116 |
84 |
Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis. |
Westf£Lische Wilhelms-Universit£T M£Nster |
23411396 |
60 |
Synthesis of new fluorinated, 2-substituted 5-pyrrolidinylsulfonyl isatin derivatives as caspase-3 and caspase-7 inhibitors: nonradioactive counterparts of putative PET-compatible apoptosis imaging agents. |
Westf£Lische Wilhelms-Universit£T M£Nster |
24900651 |
50 |
Irreversible inhibitors of cysteine proteases. |
Dart Neuroscience |
22276851 |
4 |
Caspase-1 and -3 inhibiting drimane sesquiterpenoids from the extremophilic fungus Penicillium solitum. |
University of Montana |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
16870441 |
30 |
Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors. |
Procter and Gamble Pharmaceuticals |
16046125 |
18 |
Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis. |
Procter & Gamble Pharmaceuticals |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
14980679 |
30 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid. |
Maxim Pharmaceuticals |
9873373 |
20 |
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases). |
Institute For Drug Research |
21441025 |
147 |
Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay. |
Washington University |
20674352 |
50 |
Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones. |
Pfizer |
20656488 |
61 |
Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
Pfizer |
20170165 |
13 |
Noncovalent tripeptidyl benzyl- and cyclohexyl-amine inhibitors of the cysteine protease caspase-1. |
The University of Queensland |
19908842 |
84 |
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. |
National Human Genome Research Institute |
| 25 |
3-chloro-4-carboxamido-6-arylpyridazines as a non-peptide class of interleukin-1β converting enzyme inhibitor |
TBA |
| 13 |
Structure-based design of non-peptidic pyridone aldehydes as inhibitors of interleukin-1β converting enzyme |
TBA |
| 32 |
PYRIDONE-BASED PEPTIDOMIMETIC INHIBITORS OF INTERLEUKIN-1β-CONVERTING ENZYME (ICE) |
TBA |
| 2 |
Structural and stereochemical requirements of time-dependent inactivators of the interleukin-1β converting enzyme |
TBA |
| 24 |
Inhibition of interleukin-1β converting enzyme by N-acyl-aspartyl aryloxymethyl ketones |
TBA |
| 16 |
Inhibition of interleukin-1β converting enzyme by N-Acyl-aspartic acid ketones |
TBA |
| 17 |
The synthesis and evaluation of peptidyl aspartyl aldehydes as inhibitors of ice. |
TBA |
| 8 |
Activated ketones as potent reversible inhibitors of interleukin-Iβ converting enzyme |
TBA |
| 2 |
Synthesis of a peptidyl 2,2-difluoro-4-phenylbutyl ketone and its evaluation as an inhibitor of interleukin-1β converting enzyme. |
TBA |
| 10 |
Phenylalkyl ketones as potent reversible inhibitors of interleukin-1β converting enzyme |
TBA |
| 1 |
Synthesis of a potent, reversible inhibitor of interleukin-1β converting enzyme |
TBA |
19445513 |
82 |
Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis. |
Westfalische Wilhelms-Universitat |
19049429 |
70 |
Design, synthesis, and biological characterization of a caspase 3/7 selective isatin labeled with 2-[18F]fluoroethylazide. |
Imperial College |
18457385 |
41 |
Recent developments in fragment-based drug discovery. |
Astex Therapeutics |
18330993 |
4 |
The berkeleyamides, amides from the acid lake fungus Penicillum rubrum. |
Montana Tech of The University of Montana |
17889532 |
23 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids. |
Epicept |
17585855 |
65 |
Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors. |
Washington University |
17251019 |
30 |
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones. |
Merck Frosst Centre For Therapeutic Research |
17181147 |
10 |
Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo. |
University of Edinburgh |
17154501 |
121 |
5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis. |
University Hospital of The WestfäLische Wilhelms-UniversitäT |
17127070 |
61 |
Synthesis and evaluation of unsaturated caprolactams as interleukin-1beta converting enzyme (ICE) inhibitors. |
Procter & Gamble Pharmaceuticals |
16891117 |
5 |
Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis. |
Washington University |
16782334 |
61 |
Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors. |
Procter & Gamble Pharmaceuticals |
16274992 |
29 |
Tethering identifies fragment that yields potent inhibitors of human caspase-1. |
Sunesis Pharmaceuticals |
16216507 |
87 |
Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors. |
Procter & Gamble Pharmaceuticals |
16046129 |
18 |
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme. |
Procter & Gamble Pharmaceuticals |
15686936 |
210 |
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors. |
Merck Frosst Centre For Therapeutic Research |
14741295 |
29 |
The design and synthesis of sulfonamides as caspase-1 inhibitors. |
Pfizer |
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 |
12270186 |
99 |
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization. |
Idun Pharmaceuticals |
12270185 |
257 |
Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization. |
Idun Pharmaceuticals |
11934593 |
1 |
A practical synthesis of (S) 3-tert-butoxycarbonylamino-2-oxo-2,3,4,5-tetrahydro-1,5-benzodiazepine-1-acetic acid methyl ester as a conformationally restricted dipeptido-mimetic for caspase-1 (ICE) inhibitors. |
Vertex Pharmaceuticals |
10978183 |
40 |
Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery. |
Basf Bioresearch |
9873533 |
11 |
Rapid optimization of an ICE inhibitor synthesis using multiple reaction conditions in a parallel array. |
Warner-Lambert |
9873452 |
1 |
Novel cytokine release inhibitors. Part I: Triterpenes. |
RhóNe-Poulenc Rorer Central Research |
9871520 |
30 |
Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE). |
Ferring Research Institute |
9207934 |
6 |
Pyridazinodiazepines as a high-affinity, P2-P3 peptidomimetic class of interleukin-1 beta-converting enzyme inhibitor. |
Sanofi Winthrop |
29157864 |
4 |
New Caspase-1 inhibitor by scaffold hopping into bio-inspired 3D-fragment space. |
Edelris |
29648825 |
47 |
Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne. |
Nestl� |
9108306 |
17 |
Molecular cloning and characterization of a new receptor for galanin. |
Merck Research Laboratories |
19473017 |
12 |
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
Purdue University |
19555126 |
38 |
Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. |
Burnham Institute For Medical Research |
18812261 |
8 |
The molecular interactions of buspirone analogues with the serotonin transporter. |
National Medicines Institute |
18307303 |
75 |
Discovery of selective aminothiazole aurora kinase inhibitors. |
Novartis |
18800762 |
61 |
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation. |
National Taiwan University |
18308563 |
39 |
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
Irbm/Merck Research Laboratories |
32272481 |
9 |
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors |
Shanghaitech University |
14698155 |
68 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3. |
Bristol-Myers Squibb |