98 articles for thisTarget
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Design, synthesis and biological evaluation of novel non-peptide boronic acid derivatives as proteasome inhibitors.
China Pharmaceutical University
Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors.
Hangzhou Xixi Hospital
Terminal functionalized thiourea-containing dipeptides as multidrug-resistance reversers that target 20S proteasome and cell proliferation.
Guangxi Normal University
Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit.
Kezar Life Sciences
Design, synthesis and biological evaluation of novel non-covalent piperidine-containing peptidyl proteasome inhibitors.
Hangzhou Xixi Hospital
Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual screening.
University of Naples Federico Ii
Development of novel proteasome inhibitors based on phthalazinone scaffold.
Peking University Health Science Center
3D-QSAR-aided design, synthesis, in vitro and in vivo evaluation of dipeptidyl boronic acid proteasome inhibitors and mechanism studies.
Nanjing Forestry University
Design, synthesis and docking studies of novel dipeptidyl boronic acid proteasome inhibitors constructed fromaa- andaß-amino acids.
China Pharmaceutical University
Structure-activity relationship study of syringolin A as a potential anticancer agent.
Hokkaido University
Substrate-guided optimization of the syringolins yields potent proteasome inhibitors with activity against leukemia cell lines.
Brown University
Cystargolides, 20S Proteasome Inhibitors Isolated from Kitasatospora cystarginea.
University of Prince Edward Island
Discovery of novel non-covalent inhibitors selective to theß5-subunit of the human 20S proteasome.
Peking Union Medical College
Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.
University of Messina
Identification of a new series of amides as non-covalent proteasome inhibitors.
University of Messina
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.
Hokkaido University
A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor.
Institute of Bio-Science and Technology
(S)-4-Trimethylsilyl-3-butyn-2-ol as an auxiliary for stereocontrolled synthesis of salinosporamide analogs with modifications at positions C2 and C5.
The Pennsylvania State University
Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors.
Moffitt Cancer Center
Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action.
Hokkaido University
Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.
University Paris 6
Further characterization of a putative serine protease contributing to the¿-secretase cleavage ofß-amyloid precursor protein.
University of Montpellier
Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites.
Leiden Institute of Chemistry and Netherlands Proteomics Centre
Molecular mechanisms of acquired proteasome inhibitor resistance.
University of California San Diego
P3 and P4 position analysis of vinyl ester pseudopeptide proteasome inhibitors.
University of Ferrara
Incorporation of fluorinated phenylalanine generates highly specific inhibitor of proteasome's chymotrypsin-like sites.
Gorlaeus Laboratories
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
Non-peptidic immunoproteasome β5i-selective inhibitor as potential treatment for idiopathic pulmonary fibrosis: Virtual screening, hit evolution and lead identification.
Chinese Academy of Medical Sciences & Peking Union Medical College
Recent advance of small-molecule drugs for clinical treatment of multiple myeloma.
Jilin University
Optimization of α-amido boronic acids via cryo-electron microscopy analysis: Discovery of a novel highly selective immunoproteasome subunit LMP7 (β5i)/LMP2 (β1i) dual inhibitor.
Mitsubishi Tanabe Pharma Corporation
Histone deacetylase (HDAC) inhibitor specificity determinants are preserved in a class of dual HDAC/non-covalent proteasome inhibitors.
University of Maryland
Combination Therapy and Dual-Target Inhibitors Based on LSD1: New Emerging Tools in Cancer Therapy.
Zhengzhou University
Peptidic Boronic Acid Plasmodium falciparum SUB1 Inhibitors with Improved Selectivity over Human Proteasome.
The Francis Crick Institute
Discovery of Highly Selective Inhibitors of the Human Constitutive Proteasome β5c Chymotryptic Subunit.
Weill Cornell Medicine
Identification of a new class of proteasome inhibitors based on a naphthyl-azotricyclic-urea-phenyl scaffold.
Middlesex University
Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells.
Wayne State University
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
Identification of N, C-capped di- and tripeptides as selective immunoproteasome inhibitors.
Peking Union Medical College
Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i).
Merck
Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors.
Weill Cornell Medicine
Development of isoquinolinone derivatives as immunoproteasome inhibitors.
University of Messina
Cell-based screening of extracts of natural sources to search for inhibitors of the ubiquitin-proteasome system and identification of proteasome inhibitors from the fungus Remotididymella sp.
Kumamoto University
Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.
Guangzhou Medical University
Development of peptide epoxyketones as selective immunoproteasome inhibitors.
Zhejiang University
Discovery of selective fragment-sized immunoproteasome inhibitors.
Hungarian Academy of Sciences
Design, synthesis and biological evaluation of novel naphthoquinone-4-aminobenzensulfonamide/carboxamide derivatives as proteasome inhibitors.
Ege University
Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.
Weill Cornell Medicine
Design and synthesis of tripeptidyl furylketones as selective inhibitors against the β5 subunit of human 20S proteasome.
Peking University Health Science Center
Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.
University of Melbourne
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.
Hangzhou Xixi Hospital
Design, synthesis and biological evaluation of triaryl compounds as novel 20S proteasome inhibitors.
Peking Union Medical College
LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease.
University of Kentucky
Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.
Leiden Institute of Chemistry
Another look at phenolic compounds in cancer therapy the effect of polyphenols on ubiquitin-proteasome system.
Institute of Agricultural and Food Biotechnology
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles.
Hangzhou Institute of Innovative Medicine
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.
Zhejiang University
Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide).
Kezar Life Sciences
Identification of neomacrophorins isolated from Trichoderma sp. 1212-03 as proteasome inhibitors.
Iwate University
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.
Hangzhou Xixi Hospital
Synthesis and Biological Activity of Peptide α-Ketoamide Derivatives as Proteasome Inhibitors.
University of Ferrara
Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors.
Nanjing Forestry University
Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib.
University of Kentucky
Proline- and Arginine-Rich Peptides as Flexible Allosteric Modulators of Human Proteasome Activity.
University of Gdansk
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.
Zhejiang University
Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits.
Leiden Institute of Chemistry and Netherlands Proteomics Centre
Boron in drug design: Recent advances in the development of new therapeutic agents.
S£O Paulo State University
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.
Zhejiang University
Tetradehydrohalicyclamine B, a new proteasome inhibitor from the marine sponge Acanthostrongylophora ingens.
Kumamoto University
Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities.
Sichuan University
Design, synthesis, and evaluation of cystargolide-based β-lactones as potent proteasome inhibitors.
New Mexico Institute of Mining and Technology
Structure-based design of human immuno- and constitutive proteasomes inhibitors.
University of Rennes 1
Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies.
Nanjing Forestry University
Synthesis and biological evaluation of curcumin derivatives modified with α-amino boronic acid as proteasome inhibitors.
Peking University
Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death.
Nagahama Institute of Bio-Science and Technology
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
Heinrich Heine University D£Sseldorf
Potent and Highly Selective Inhibitors of the Proteasome Trypsin-like Site by Incorporation of Basic Side Chain Containing Amino Acid Derived Sulfonyl Fluorides.
University of Glasgow
Discovery of novel 20S proteasome inhibitors by rational topology-based scaffold hopping of bortezomib.
Fudan University
Neomacrophorin X, a [4.4.3]Propellane-Type Meroterpenoid from Trichoderma sp. 1212-03.
Hirosaki University
Synthesis and biological activity of peptide proline-boronic acids as proteasome inhibitors.
Peking University
Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine.
Palack£
Urea-containing peptide boronic acids as potent proteasome inhibitors.
Peking University
Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity.
University of California
A strategy for dual inhibition of the proteasome and fatty acid synthase with belactosin C-orlistat hybrids.
Baylor University
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis