Recent Advances in the Discovery of Deubiquitinating Enzyme Inhibitors

scientific article published on 12 January 2016

Recent Advances in the Discovery of Deubiquitinating Enzyme Inhibitors is …
instance of (P31):
review articleQ7318358
scholarly articleQ13442814

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P356DOI10.1016/BS.PMCH.2015.10.002
P932PMC publication ID7112275
P698PubMed publication ID26852935

P2093author name stringMark Kemp
P2860cites workEnzymatic characterisation of USP7 deubiquitinating activity and inhibitionQ39563641
Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis.Q39636568
Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47.Q39730830
Will the Ubiquitin System Furnish as Many Drug Targets as Protein Kinases?Q39812916
Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cellsQ39813804
Structure-activity relationship, kinetic mechanism, and selectivity for a new class of ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitorsQ40142929
A general chemical ligation approach towards isopeptide-linked ubiquitin and ubiquitin-like assay reagentsQ41515742
Ubiquitin-specific protease 4 is inhibited by its ubiquitin-like domainQ41861997
The DUSP-Ubl domain of USP4 enhances its catalytic efficiency by promoting ubiquitin exchangeQ42028148
Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymesQ43148533
Identification of a novel chemical potentiator and inhibitors of UCH-L1 by in silico drug screeningQ43834622
Thiopurine analogues inhibit papain-like protease of severe acute respiratory syndrome coronavirus.Q44594725
Delta12-Prostaglandin J2 inhibits the ubiquitin hydrolase UCH-L1 and elicits ubiquitin-protein aggregation without proteasome inhibitionQ44934471
Harnessing the oxidation susceptibility of deubiquitinases for inhibition with small moleculesQ46823938
Small-Molecule Inhibitors and Probes for Ubiquitin- and Ubiquitin-Like-Specific ProteasesQ58214454
The demonstration of new human brain-specific proteins by high-resolution two-dimensional polyacrylamide gel electrophoresisQ70732451
Kinetic studies of isopeptidase T: modulation of peptidase activity by ubiquitinQ71715465
Kinetic and mechanistic studies on the hydrolysis of ubiquitin C-terminal 7-amido-4-methylcoumarin by deubiquitinating enzymesQ74252080
High incidence of ubiquitin-like domains in human ubiquitin-specific proteasesQ80539443
Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologistsQ81620167
Deubiquitination of p53 by HAUSP is an important pathway for p53 stabilizationQ24292930
The mitochondrial deubiquitinase USP30 opposes parkin-mediated mitophagyQ24298748
USP30 and parkin homeostatically regulate atypical ubiquitin chains on mitochondriaQ24316174
UAF1 is a subunit of multiple deubiquitinating enzyme complexesQ24329003
Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13Q24338972
Structure and mechanisms of the proteasome-associated deubiquitinating enzyme USP14Q24537053
Deubiquitinating enzymes in cellular signaling and disease regulationQ26801232
Advances in the development of SUMO specific protease (SENP) inhibitorsQ26864235
Crystal structure of a UBP-family deubiquitinating enzyme in isolation and in complex with ubiquitin aldehydeQ27640257
Dipeptidyl nitrile inhibitors of Cathepsin LQ27655858
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitorsQ27659746
Ubiquitin vinyl methyl ester binding orients the misaligned active site of the ubiquitin hydrolase UCHL1 into productive conformationQ27661287
Severe Acute Respiratory Syndrome Coronavirus Papain-like Novel Protease Inhibitors: Design, Synthesis, Protein−Ligand X-ray Structure and Biological EvaluationQ27662127
Length of the active-site crossover loop defines the substrate specificity of ubiquitin C-terminal hydrolases for ubiquitin chainsQ27671821
Mechanism of USP7/HAUSP activation by its C-terminal ubiquitin-like domain and allosteric regulation by GMP-synthetaseQ27674789
The co-crystal structure of ubiquitin carboxy-terminal hydrolase L1 (UCHL1) with a tripeptide fluoromethyl ketone (Z-VAE(OMe)-FMK)Q27679250
X-ray Structural and Biological Evaluation of a Series of Potent and Highly Selective Inhibitors of Human Coronavirus Papain-like ProteasesQ27681891
Structure and Catalytic Regulatory Function of Ubiquitin Specific Protease 11 N-Terminal and Ubiquitin-like DomainsQ27683231
Crystal structure of the papain-like protease of MERS coronavirus reveals unusual, potentially druggable active-site featuresQ27694423
Catching a DUB in the act: novel ubiquitin-based active site directed probesQ38280690
Monitoring Target Engagement of Deubiquitylating Enzymes Using Activity Probes: Past, Present, and FutureQ38822748
Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignanciesQ38894421
USP30 deubiquitylates mitochondrial Parkin substrates and restricts apoptotic cell deathQ38903534
The 19S Deubiquitinase inhibitor b-AP15 is enriched in cells and elicits rapid commitment to cell death.Q39006249
Curcusone D, a novel ubiquitin-proteasome pathway inhibitor via ROS-induced DUB inhibition, is synergistic with bortezomib against multiple myeloma cell growthQ39023236
Mitoxantrone targets human ubiquitin-specific peptidase 11 (USP11) and is a potent inhibitor of pancreatic cancer cell survivalQ39148897
Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymesQ39437160
Inhibition of proteasome deubiquitinating activity as a new cancer therapyQ39447379
The USP1/UAF1 complex promotes double-strand break repair through homologous recombinationQ39560571
The ubiquitin systemQ27860803
Breaking the chains: structure and function of the deubiquitinasesQ28131738
A dynamic role of HAUSP in the p53-Mdm2 pathwayQ28253645
The ubiquitin codeQ28265104
The role of UBL domains in ubiquitin-specific proteasesQ28267230
Amino-terminal dimerization, NRDP1-rhodanese interaction, and inhibited catalytic domain conformation of the ubiquitin-specific protease 8 (USP8)Q28268036
The JAMM motif of human deubiquitinase Poh1 is essential for cell viabilityQ28284132
A genomic and functional inventory of deubiquitinating enzymesQ28284911
Polyubiquitin chains: polymeric protein signalsQ28294396
A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistanceQ28395203
Antiviral activity of a small molecule deubiquitinase inhibitor occurs via induction of the unfolded protein responseQ28481001
A small natural molecule promotes mitochondrial fusion through inhibition of the deubiquitinase USP30Q28504988
Crystal Structure of USP7 Ubiquitin-like Domains with an ICP0 Peptide Reveals a Novel Mechanism Used by Viral and Cellular Proteins to Target USP7Q28547943
Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15Q28834132
Deubiquitinases (DUBs) and DUB inhibitors: a patent reviewQ28834608
New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassaysQ29615588
Enhancement of proteasome activity by a small-molecule inhibitor of USP14Q29616735
Targeting deubiquitinases enabled by chemical synthesis of proteins.Q31046568
Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screeningQ33296122
A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replicationQ33375590
Structure-based design, synthesis, and biological evaluation of a series of novel and reversible inhibitors for the severe acute respiratory syndrome-coronavirus papain-like proteaseQ33488957
Profiling the NIH Small Molecule Repository for compounds that generate H2O2 by redox cycling in reducing environmentsQ33523595
Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells.Q33873915
A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitinationQ33998170
A heat-stable polypeptide component of an ATP-dependent proteolytic system from reticulocytesQ34056133
An optimal ubiquitin-proteasome pathway in the nervous system: the role of deubiquitinating enzymesQ34063163
A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.Q34089593
Coronavirus papain-like proteases negatively regulate antiviral innate immune response through disruption of STING-mediated signalingQ34152661
Discovery of specific inhibitors of human USP7/HAUSP deubiquitinating enzymeQ34240760
Discovery of Inhibitors that Elucidate the Role of UCH-L1 Activity in the H1299 Lung Cancer Cell LineQ34266771
Identification Of Small Molecule TRABID Deubiquitinase Inhibitors By Computation-Based Virtual Screen.Q34268517
Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancerQ34313778
Families of cysteine peptidases.Q34317817
Spongiacidin C, a pyrrole alkaloid from the marine sponge Stylissa massa, functions as a USP7 inhibitorQ34345359
Thiopurine analogs and mycophenolic acid synergistically inhibit the papain-like protease of Middle East respiratory syndrome coronavirusQ34455805
Structural basis for conformational plasticity of the Parkinson's disease-associated ubiquitin hydrolase UCH-L1Q34502063
Crystal structure of the Middle East respiratory syndrome coronavirus (MERS-CoV) papain-like protease bound to ubiquitin facilitates targeted disruption of deubiquitinating activity to demonstrate its role in innate immune suppressionQ34683256
Macromolecular juggling by ubiquitylation enzymesQ34782977
Development of inhibitors in the ubiquitination cascadeQ35044801
A fragment-based method to discover irreversible covalent inhibitors of cysteine proteasesQ35175346
Screening of DUB activity and specificity by MALDI-TOF mass spectrometryQ35232335
Inhibiting the deubiquitinating enzymes (DUBs).Q35386992
Pharmacological targets in the ubiquitin system offer new ways of treating cancer, neurodegenerative disorders and infectious diseasesQ35559055
Prolonged and tunable residence time using reversible covalent kinase inhibitorsQ35756228
Covalent Inhibition of Ubc13 Affects Ubiquitin Signaling and Reveals Active Site Elements Important for TargetingQ35864085
Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cellsQ35934305
Ubiquitin C-terminal hydrolase l1 in tumorigenesisQ36091119
Comparison of SARS and NL63 papain-like protease binding sites and binding site dynamics: inhibitor design implicationsQ36095703
A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistanceQ36338365
Emerging trends in metalloprotein inhibitionQ36956841
Protein partners of deubiquitinating enzymesQ37237774
Strategies for the identification of novel inhibitors of deubiquitinating enzymesQ37269483
Future of anticathepsin K drugs: dual therapy for skeletal disease and atherosclerosis?Q37428071
USP8 is a novel target for overcoming gefitinib resistance in lung cancerQ37476722
DUBs and cancer: the role of deubiquitinating enzymes as oncogenes, non-oncogenes and tumor suppressorsQ37485753
USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosisQ37577477
Loss of mTOR repressors Tsc1 or Pten has divergent effects on excitatory and inhibitory synaptic transmission in single hippocampal neuron culturesQ37579637
Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancerQ37660030
Emerging roles of deubiquitinases in cancer-associated pathwaysQ37674364
Peptidomimetic inhibitors of cathepsin K.Q37718837
Deubiquitinases in cancer: new functions and therapeutic options.Q37945451
Proteasome inhibitors: an expanding army attacking a unique targetQ37979388
Deubiquitylating enzymes and DNA damage response pathwaysQ38109871
Deubiquitylases from genes to organismQ38125278
Regulation of deubiquitinase proteolytic activityQ38130360
Toward understanding ubiquitin-modifying enzymes: from pharmacological targeting to proteomicsQ38203366
Molecular pathways: translational potential of deubiquitinases as drug targetsQ38236205
Emerging potential of therapeutic targeting of ubiquitin-specific proteases in the treatment of cancer.Q38244793
P304page(s)149-192
P577publication date2016-01-12
P1433published inProgress in medicinal chemistryQ27712806
P1476titleRecent Advances in the Discovery of Deubiquitinating Enzyme Inhibitors
P478volume55