Recent Advances in the Discovery of Deubiquitinating Enzyme Inhibitors (Q38725385)

5 September 2017

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title

Recent Advances in the Discovery of Deubiquitinating Enzyme Inhibitors (English)

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5 September 2017

Mark Kemp

1

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26852935%20AND%20SRC:MED&resulttype=core&format=json

12 June 2020

publication date

12 January 2016

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26852935

Progress in medicinal chemistry

5 September 2017

published in

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26852935%20AND%20SRC:MED&resulttype=core&format=json

12 June 2020

volume

55

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26852935%20AND%20SRC:MED&resulttype=core&format=json

12 June 2020

page(s)

149-192

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26852935%20AND%20SRC:MED&resulttype=core&format=json

A general chemical ligation approach towards isopeptide-linked ubiquitin and ubiquitin-like assay reagents

12 June 2020

cites work

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12 December 2020

Regulation of deubiquitinase proteolytic activity

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12 December 2020

Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening

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12 December 2020

Crystal structure of a UBP-family deubiquitinating enzyme in isolation and in complex with ubiquitin aldehyde

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12 December 2020

Small-Molecule Inhibitors and Probes for Ubiquitin- and Ubiquitin-Like-Specific Proteases

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12 December 2020

New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays

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12 December 2020

Will the Ubiquitin System Furnish as Many Drug Targets as Protein Kinases?

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12 December 2020

Structure-activity relationship, kinetic mechanism, and selectivity for a new class of ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitors

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12 December 2020

The JAMM motif of human deubiquitinase Poh1 is essential for cell viability

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12 December 2020

Severe Acute Respiratory Syndrome Coronavirus Papain-like Novel Protease Inhibitors: Design, Synthesis, Protein−Ligand X-ray Structure and Biological Evaluation

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12 December 2020

An optimal ubiquitin-proteasome pathway in the nervous system: the role of deubiquitinating enzymes

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12 December 2020

Polyubiquitin chains: polymeric protein signals

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12 December 2020

USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis

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12 December 2020

Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes

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12 December 2020

Spongiacidin C, a pyrrole alkaloid from the marine sponge Stylissa massa, functions as a USP7 inhibitor

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12 December 2020

Inhibiting the deubiquitinating enzymes (DUBs).

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12 December 2020

High incidence of ubiquitin-like domains in human ubiquitin-specific proteases

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12 December 2020

Macromolecular juggling by ubiquitylation enzymes

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12 December 2020

Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer

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12 December 2020

Pharmacological targets in the ubiquitin system offer new ways of treating cancer, neurodegenerative disorders and infectious diseases

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12 December 2020

Future of anticathepsin K drugs: dual therapy for skeletal disease and atherosclerosis?

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12 December 2020

Strategies for the identification of novel inhibitors of deubiquitinating enzymes

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12 December 2020

Structure-based design, synthesis, and biological evaluation of a series of novel and reversible inhibitors for the severe acute respiratory syndrome-coronavirus papain-like protease

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12 December 2020

A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases

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12 December 2020

Prolonged and tunable residence time using reversible covalent kinase inhibitors

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12 December 2020

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 suppression

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12 December 2020

Identification Of Small Molecule TRABID Deubiquitinase Inhibitors By Computation-Based Virtual Screen.

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12 December 2020

Emerging trends in metalloprotein inhibition

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12 December 2020

Crystal Structure of USP7 Ubiquitin-like Domains with an ICP0 Peptide Reveals a Novel Mechanism Used by Viral and Cellular Proteins to Target USP7

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12 December 2020

Amino-terminal dimerization, NRDP1-rhodanese interaction, and inhibited catalytic domain conformation of the ubiquitin-specific protease 8 (USP8)

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12 December 2020

Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells

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12 December 2020

Screening of DUB activity and specificity by MALDI-TOF mass spectrometry

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12 December 2020

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12 December 2020

Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists

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12 December 2020

Emerging potential of therapeutic targeting of ubiquitin-specific proteases in the treatment of cancer.

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12 December 2020

The role of UBL domains in ubiquitin-specific proteases

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12 December 2020

Ubiquitin vinyl methyl ester binding orients the misaligned active site of the ubiquitin hydrolase UCHL1 into productive conformation

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12 December 2020

X-ray Structural and Biological Evaluation of a Series of Potent and Highly Selective Inhibitors of Human Coronavirus Papain-like Proteases

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12 December 2020

Breaking the chains: structure and function of the deubiquitinases

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12 December 2020

A dynamic role of HAUSP in the p53-Mdm2 pathway

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12 December 2020

Profiling the NIH Small Molecule Repository for compounds that generate H2O2 by redox cycling in reducing environments

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12 December 2020

DUBs and cancer: the role of deubiquitinating enzymes as oncogenes, non-oncogenes and tumor suppressors

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12 December 2020

A heat-stable polypeptide component of an ATP-dependent proteolytic system from reticulocytes

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12 December 2020

Structure and mechanisms of the proteasome-associated deubiquitinating enzyme USP14

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12 December 2020

The 19S Deubiquitinase inhibitor b-AP15 is enriched in cells and elicits rapid commitment to cell death.

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12 December 2020

Molecular pathways: translational potential of deubiquitinases as drug targets

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12 December 2020

Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells

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12 December 2020

Toward understanding ubiquitin-modifying enzymes: from pharmacological targeting to proteomics

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12 December 2020

The co-crystal structure of ubiquitin carboxy-terminal hydrolase L1 (UCHL1) with a tripeptide fluoromethyl ketone (Z-VAE(OMe)-FMK)

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12 December 2020

Comparison of SARS and NL63 papain-like protease binding sites and binding site dynamics: inhibitor design implications

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12 December 2020

Kinetic and mechanistic studies on the hydrolysis of ubiquitin C-terminal 7-amido-4-methylcoumarin by deubiquitinating enzymes

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12 December 2020

Identification of a novel chemical potentiator and inhibitors of UCH-L1 by in silico drug screening

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12 December 2020

A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.

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12 December 2020

Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells.

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12 December 2020

Enhancement of proteasome activity by a small-molecule inhibitor of USP14

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12 December 2020

Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignancies

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12 December 2020

A genomic and functional inventory of deubiquitinating enzymes

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12 December 2020

USP8 is a novel target for overcoming gefitinib resistance in lung cancer

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12 December 2020

Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes

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12 December 2020

Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors

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12 December 2020

Deubiquitinases (DUBs) and DUB inhibitors: a patent review

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12 December 2020

Inhibition of proteasome deubiquitinating activity as a new cancer therapy

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12 December 2020

Curcusone D, a novel ubiquitin-proteasome pathway inhibitor via ROS-induced DUB inhibition, is synergistic with bortezomib against multiple myeloma cell growth

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12 December 2020

Ubiquitin-specific protease 4 is inhibited by its ubiquitin-like domain

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12 December 2020

Kinetic studies of isopeptidase T: modulation of peptidase activity by ubiquitin

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12 December 2020

Ubiquitin C-terminal hydrolase l1 in tumorigenesis

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12 December 2020

Deubiquitylases from genes to organism

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12 December 2020

Monitoring Target Engagement of Deubiquitylating Enzymes Using Activity Probes: Past, Present, and Future

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12 December 2020

Development of inhibitors in the ubiquitination cascade

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12 December 2020

Protein partners of deubiquitinating enzymes

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12 December 2020

A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance

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12 December 2020

Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis.

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12 December 2020

A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination

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12 December 2020

Structure and Catalytic Regulatory Function of Ubiquitin Specific Protease 11 N-Terminal and Ubiquitin-like Domains

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12 December 2020

Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13

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12 December 2020

Deubiquitylating enzymes and DNA damage response pathways

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12 December 2020

The demonstration of new human brain-specific proteins by high-resolution two-dimensional polyacrylamide gel electrophoresis

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12 December 2020

Proteasome inhibitors: an expanding army attacking a unique target

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12 December 2020

Antiviral activity of a small molecule deubiquitinase inhibitor occurs via induction of the unfolded protein response

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12 December 2020

Discovery of specific inhibitors of human USP7/HAUSP deubiquitinating enzyme

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12 December 2020

Deubiquitinases in cancer: new functions and therapeutic options.

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12 December 2020

The DUSP-Ubl domain of USP4 enhances its catalytic efficiency by promoting ubiquitin exchange

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12 December 2020

USP30 deubiquitylates mitochondrial Parkin substrates and restricts apoptotic cell death

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12 December 2020

Catching a DUB in the act: novel ubiquitin-based active site directed probes

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12 December 2020

Advances in the development of SUMO specific protease (SENP) inhibitors

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12 December 2020

The mitochondrial deubiquitinase USP30 opposes parkin-mediated mitophagy

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12 December 2020

Thiopurine analogues inhibit papain-like protease of severe acute respiratory syndrome coronavirus.

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12 December 2020

A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication

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12 December 2020

The USP1/UAF1 complex promotes double-strand break repair through homologous recombination

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12 December 2020

Thiopurine analogs and mycophenolic acid synergistically inhibit the papain-like protease of Middle East respiratory syndrome coronavirus

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12 December 2020

Mechanism of USP7/HAUSP activation by its C-terminal ubiquitin-like domain and allosteric regulation by GMP-synthetase

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12 December 2020

Enzymatic characterisation of USP7 deubiquitinating activity and inhibition

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12 December 2020

Harnessing the oxidation susceptibility of deubiquitinases for inhibition with small molecules

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12 December 2020

UAF1 is a subunit of multiple deubiquitinating enzyme complexes

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12 December 2020

Targeting deubiquitinases enabled by chemical synthesis of proteins.

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12 December 2020

A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance

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12 December 2020

Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47.

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12 December 2020

Dipeptidyl nitrile inhibitors of Cathepsin L

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12 December 2020

USP30 and parkin homeostatically regulate atypical ubiquitin chains on mitochondria

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12 December 2020

Delta12-Prostaglandin J2 inhibits the ubiquitin hydrolase UCH-L1 and elicits ubiquitin-protein aggregation without proteasome inhibition

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12 December 2020

Crystal structure of the papain-like protease of MERS coronavirus reveals unusual, potentially druggable active-site features

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12 December 2020

Deubiquitination of p53 by HAUSP is an important pathway for p53 stabilization

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12 December 2020

Length of the active-site crossover loop defines the substrate specificity of ubiquitin C-terminal hydrolases for ubiquitin chains

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12 December 2020

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 cancer

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12 December 2020

Families of cysteine peptidases.

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12 December 2020

Structural basis for conformational plasticity of the Parkinson's disease-associated ubiquitin hydrolase UCH-L1

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12 December 2020

Deubiquitinating enzymes in cellular signaling and disease regulation

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12 December 2020

Discovery of Inhibitors that Elucidate the Role of UCH-L1 Activity in the H1299 Lung Cancer Cell Line

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12 December 2020

Emerging roles of deubiquitinases in cancer-associated pathways

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12 December 2020

Mitoxantrone targets human ubiquitin-specific peptidase 11 (USP11) and is a potent inhibitor of pancreatic cancer cell survival

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12 December 2020

Covalent Inhibition of Ubc13 Affects Ubiquitin Signaling and Reveals Active Site Elements Important for Targeting

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12 December 2020

Peptidomimetic inhibitors of cathepsin K.

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12 December 2020

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12 December 2020

Coronavirus papain-like proteases negatively regulate antiviral innate immune response through disruption of STING-mediated signaling

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12 December 2020

A small natural molecule promotes mitochondrial fusion through inhibition of the deubiquitinase USP30

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12 December 2020

Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15

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12 December 2020

Loss of mTOR repressors Tsc1 or Pten has divergent effects on excitatory and inhibitory synaptic transmission in single hippocampal neuron cultures

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12 December 2020

10.1016/BS.PMCH.2015.10.002

Identifiers

DOI

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26852935%20AND%20SRC:MED&resulttype=core&format=json

12 June 2020

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26852935%20AND%20SRC:MED&resulttype=core&format=json

12 June 2020

26852935

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