How chemoproteomics can enable drug discovery and development (Q34143272)

31 July 2017

title

How chemoproteomics can enable drug discovery and development (English)

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31 July 2017

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Benjamin F Cravatt

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31 July 2017

Raymond E Moellering

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31 July 2017

publication date

1 January 2012

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31 July 2017

published in

Chemistry and Biology

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31 July 2017

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31 July 2017

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31 July 2017

page(s)

11-22

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Comprehensive analysis of kinase inhibitor selectivity

31 July 2017

cites work

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How were new medicines discovered?

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5 July 2018

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5 July 2018

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The end game of chemical genetics: target identification

5 July 2018

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Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1.

5 July 2018

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Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors

5 July 2018

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5 July 2018

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Nonproteasomal targets of the proteasome inhibitors bortezomib and carfilzomib: a link to clinical adverse events

5 July 2018

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5 July 2018

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Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

5 July 2018

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Photoreactive stapled BH3 peptides to dissect the BCL-2 family interactome.

5 July 2018

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Quantitative reactivity profiling predicts functional cysteines in proteomes

5 July 2018

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Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening

5 July 2018

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Evidence for an alternative glycolytic pathway in rapidly proliferating cells

5 July 2018

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Pharmacological Inhibition of BMK1 Suppresses Tumor Growth through Promyelocytic Leukemia Protein

5 July 2018

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5 July 2018

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5 July 2018

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Acylating drugs: redesigning natural covalent inhibitors

5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

5 July 2018

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Direct inhibition of the NOTCH transcription factor complex

5 July 2018

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A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog

5 July 2018

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Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

5 July 2018

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Inhibition of a viral enzyme by a small-molecule dimer disruptor

5 July 2018

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A suite of activity-based probes for human cytochrome P450 enzymes

5 July 2018

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Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes

5 July 2018

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Identifying the proteins to which small-molecule probes and drugs bind in cells

5 July 2018

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Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2

5 July 2018

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Targeting cancer with small molecule kinase inhibitors

5 July 2018

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Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects

5 July 2018

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Peptidase substrates via global peptide profiling

5 July 2018

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Contemporary strategies for the stabilization of peptides in the alpha-helical conformation

5 July 2018

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An integrated genomic analysis of human glioblastoma multiforme

5 July 2018

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Identification of RIP1 kinase as a specific cellular target of necrostatins

5 July 2018

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High-throughput kinase profiling as a platform for drug discovery

5 July 2018

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Activity-based protein profiling: from enzyme chemistry to proteomic chemistry

5 July 2018

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The M2 splice isoform of pyruvate kinase is important for cancer metabolism and tumour growth

5 July 2018

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Identification of proteases that regulate erythrocyte rupture by the malaria parasite Plasmodium falciparum

5 July 2018

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5 July 2018

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Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo

5 July 2018

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5 July 2018

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Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer

5 July 2018

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RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels

5 July 2018

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An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms

5 July 2018

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Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

5 July 2018

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A clickable inhibitor reveals context-dependent autoactivation of p90 RSK

5 July 2018

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Activity-based probes for proteomic profiling of histone deacetylase complexes

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3312051

Functional interrogation of the kinome using nucleotide acyl phosphates

5 July 2018

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How many drug targets are there?

5 July 2018

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Self-renewal of embryonic stem cells by a small molecule

5 July 2018

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An enzyme that regulates ether lipid signaling pathways in cancer annotated by multidimensional profiling

5 July 2018

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A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling

5 July 2018

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The druggable genome: an update

5 July 2018

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The use of orlistat in the treatment of obesity, dyslipidaemia and Type 2 diabetes

5 July 2018

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5 July 2018

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Structural bioinformatics-based design of selective, irreversible kinase inhibitors

5 July 2018

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A small molecule-kinase interaction map for clinical kinase inhibitors

5 July 2018

1 reference

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Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix

5 July 2018

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A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]

5 July 2018

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Acetylcholinesterase inhibitors: novel activities of old molecules.

5 July 2018

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Discovering potent and selective reversible inhibitors of enzymes in complex proteomes

5 July 2018

1 reference

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A role for the protease falcipain 1 in host cell invasion by the human malaria parasite

5 July 2018

1 reference

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Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts

5 July 2018

1 reference

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Activity-based protein profiling: the serine hydrolases

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3312051

Cytosolic isocitrate dehydrogenase in humans, mice, and voles and phylogenetic analysis of the enzyme family

5 July 2018

1 reference

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Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3312051

A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p

5 July 2018

1 reference

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A receptor for the immunosuppressant FK506 is a cis-trans peptidyl-prolyl isomerase

5 July 2018

1 reference

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A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes

5 July 2018

1 reference

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High throughput drug profiling

5 July 2018

1 reference

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A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases

28 October 2018

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Getting pharmaceutical R&D back on target

28 October 2018

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Identification and isolation of a membrane protein necessary for leukotriene production

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12 December 2020

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How to revive breakthrough innovation in the pharmaceutical industry

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10.1016/J.CHEMBIOL.2012.01.001

Identifiers

DOI

1 reference

31 July 2017

1 reference

31 July 2017

1 reference