Determining target engagement in living systems (Q37732146)

22 August 2017

Determining target engagement in living systems (English)

1 reference

22 August 2017

3

Benjamin F Cravatt

1 reference

22 August 2017

Gabriel M Simon

1

1 reference

PMCID

4004587

22 August 2017

Micah J Niphakis

series ordinal

2

1 reference

22 August 2017

1 April 2013

1 reference

22 August 2017

Nature Chemical Biology

1 reference

22 August 2017

9

1 reference

22 August 2017

4

1 reference

22 August 2017

200-205

1 reference

https://scigraph.springernature.com/pub.10.1038/nchembio.1211

22 August 2017

0 references

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Functional imaging of legumain in cancer using a new quenched activity-based probe

23 August 2017

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DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses

23 August 2017

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Brain Penetrant LRRK2 Inhibitor

23 August 2017

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Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies

23 August 2017

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Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes

23 August 2017

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A nonpeptidic cathepsin S activity-based probe for noninvasive optical imaging of tumor-associated macrophages

23 August 2017

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The synthesis and in vivo evaluation of [18F]PF-9811: a novel PET ligand for imaging brain fatty acid amide hydrolase (FAAH).

23 August 2017

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Interrogating signaling nodes involved in cellular transformations using kinase activity probes

23 August 2017

1 reference

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Functional imaging of proteases: recent advances in the design and application of substrate-based and activity-based probes

23 August 2017

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Identification of direct target engagement biomarkers for kinase-targeted therapeutics

23 August 2017

1 reference

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Positron emission tomography molecular imaging for drug development

23 August 2017

1 reference

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In situ kinase profiling reveals functionally relevant properties of native kinases

23 August 2017

1 reference

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Lipidomics at the interface of structure and function in systems biology

23 August 2017

1 reference

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

23 August 2017

1 reference

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Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

23 August 2017

1 reference

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The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

23 August 2017

1 reference

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Small-animal positron emission tomography as a tool for neuropharmacology

23 August 2017

1 reference

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Chemical phylogenetics of histone deacetylases

23 August 2017

1 reference

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Sensitive multiplexed analysis of kinase activities and activity-based kinase identification

23 August 2017

1 reference

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Noninvasive optical imaging of apoptosis by caspase-targeted activity-based probes

23 August 2017

1 reference

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Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

23 August 2017

1 reference

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Target site occupancy: emerging generalizations from clinical and preclinical studies

23 August 2017

1 reference

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Targeting cancer with small molecule kinase inhibitors

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Peptidase substrates via global peptide profiling

23 August 2017

1 reference

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Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

The role of imaging in proof of concept for CNS drug discovery and development

23 August 2017

1 reference

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Accelerating drug development using biomarkers: a case study with sitagliptin, a novel DPP4 inhibitor for type 2 diabetes

23 August 2017

1 reference

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In vitro receptor binding assays: general methods and considerations.

23 August 2017

1 reference

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

23 August 2017

1 reference

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Recognizing and exploiting differences between RNAi and small-molecule inhibitors

23 August 2017

1 reference

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Strategic approach to fit-for-purpose biomarkers in drug development

23 August 2017

1 reference

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Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors

23 August 2017

1 reference

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High-throughput screening assays for the identification of chemical probes

23 August 2017

1 reference

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Scaffold composition and biological relevance of screening libraries.

23 August 2017

1 reference

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A clickable inhibitor reveals context-dependent autoactivation of p90 RSK

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Activity-based probes for proteomic profiling of histone deacetylase complexes

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

The development of proteasome inhibitors as anticancer drugs

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

A stepwise huisgen cycloaddition process: copper(I)-catalyzed regioselective "ligation" of azides and terminal alkynes

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Dopamine D2 and D3 receptor occupancy in normal humans treated with the antipsychotic drug aripiprazole (OPC 14597): a study using positron emission tomography and [11C]raclopride

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Cell surface engineering by a modified Staudinger reaction

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Using photolabile ligands in drug discovery and development.

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Activity-based protein profiling: the serine hydrolases

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Clinical perspectives for irreversible tyrosine kinase inhibitors in cancer

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

ABPP methodology: introduction and overview

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Photoaffinity labeling in activity-based protein profiling

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Using transcriptome sequencing to identify mechanisms of drug action and resistance

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

A HIF-regulated VHL-PTP1B-Src signaling axis identifies a therapeutic target in renal cell carcinoma

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

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

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Activity-based probes that target diverse cysteine protease families

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Activity-based probes for studying the activity of flavin-dependent oxidases and for the protein target profiling of monoamine oxidase inhibitors

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Evaluation of 11C-GSK189254 as a novel radioligand for the H3 receptor in humans using PET.

23 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously

1 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4004587

Drug candidates derailed in case of mistaken identity

1 September 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23508173

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Affinity labeling of neuronal acetylcholine receptor subunits with an alpha-neurotoxin that blocks receptor function

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23508173

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1038/NCHEMBIO.1211

1 reference

22 August 2017

1 reference

22 August 2017

1 reference

PMCID

4004587