Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).

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Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766). is …
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scholarly articleQ13442814

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P356DOI10.1021/ACS.JMEDCHEM.7B01406
P932PMC publication ID5815658
P698PubMed publication ID29240418

P50authorPaul WorkmanQ7154482
Nicola E A ChessumQ89635496
Elisa PasquaQ89635498
Mark StubbsQ89635502
Paul A ClarkeQ38546651
Keith JonesQ42289984
Matthew D CheesemanQ42289987
Birgit WildingQ59559269
Bugra OzerQ86928483
Rosemary BurkeQ87855031
Ian CollinsQ89426612
P2093author name stringJohn J Caldwell
Swee Y Sharp
Martin Rowlands
Meirion Richards
P Craig McAndrew
Giampiero Colombano
P2860cites workPirin is an iron-dependent redox regulator of NF-κBQ24294125
Molecular architecture and assembly of the DDB1-CUL4A ubiquitin ligase machineryQ24302241
Target engagement in lead generationQ26827296
Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar AffinitiesQ27640584
Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomideQ27684738
Structural basis of lenalidomide-induced CK1α degradation by the CRL4(CRBN) ubiquitin ligaseQ27704179
Global quantification of mammalian gene expression controlQ28238103
How does multiple testing correction work?Q28267689
Ubiquitin-independent proteasomal degradationQ28290917
DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradationQ28830958
Cupins: the most functionally diverse protein superfamily?Q30164325
Monitoring protein interactions in living cells with fluorescence lifetime imaging microscopyQ30411241
Fluorescence polarization competition assay: the range of resolvable inhibitor potency is limited by the affinity of the fluorescent ligandQ30729180
Rapid palladium-catalyzed synthesis of esters from aryl halides utilizing Mo(CO)(6) as a solid carbon monoxide sourceQ31149344
Evaluation of dynamic polar molecular surface area as predictor of drug absorption: comparison with other computational and experimental predictorsQ31941605
A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitorsQ34067085
Proteasome inhibitors: from research tools to drug candidatesQ34341985
Biochemical mechanisms of drug action: what does it take for success?Q34344862
Tracking cancer drugs in living cells by thermal profiling of the proteomeQ34441561
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.Q34478968
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.Q34479551
Catalytic in vivo protein knockdown by small-molecule PROTACs.Q34480735
Target engagement and drug residence time can be observed in living cells with BRET.Q34503961
Induced protein degradation: an emerging drug discovery paradigmQ34545841
DCAFs, the missing link of the CUL4-DDB1 ubiquitin ligaseQ34641190
Chiral inversion and hydrolysis of thalidomide: mechanisms and catalysis by bases and serum albumin, and chiral stability of teratogenic metabolitesQ34663680
In vitro trans-monolayer permeability calculations: often forgotten assumptionsQ35595393
Thermal proteome profiling for unbiased identification of direct and indirect drug targets using multiplexed quantitative mass spectrometry.Q35778631
Small-Molecule PROTACS: New Approaches to Protein DegradationQ35891557
Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development.Q36149268
Features of selective kinase inhibitorsQ36173396
Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling.Q36238589
Nonclassical Size Dependence of Permeation Defines Bounds for Passive Adsorption of Large Drug Molecules.Q36242161
In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs).Q36268420
Structural basis of PROTAC cooperative recognition for selective protein degradationQ36306106
Chemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathwayQ36309724
Thalidomide metabolism and hydrolysis: mechanisms and implicationsQ36569878
A comprehensive mathematical model for three-body binding equilibriaQ37029337
Activity-based protein profiling: from enzyme chemistry to proteomic chemistryQ37119021
Measuring and interpreting the selectivity of protein kinase inhibitorsQ37537075
Colloidal drug formulations can explain "bell-shaped" concentration-response curvesQ37701412
Determining target engagement in living systemsQ37732146
Applications of Fluorine in Medicinal ChemistryQ38552042
Protein Knockdown Technology: Application of Ubiquitin Ligase to Cancer TherapyQ38631145
Thermal proteome profiling: unbiased assessment of protein state through heat-induced stability changesQ38666368
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor ScaffoldsQ38673230
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.Q38710711
Small-Molecule Target Engagement in CellsQ38799360
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.Q38817737
Isosteric analogs of lenalidomide and pomalidomide: synthesis and biological activityQ39241734
Impact of linker length on the activity of PROTACsQ39648105
Angiotensin II pseudopeptides containing 1,3,5-trisubstituted benzene scaffolds with high AT2 receptor affinityQ40362761
Prediction of intracellular exposure bridges the gap between target- and cell-based drug discoveryQ41256404
Pirin regulates epithelial to mesenchymal transition independently of Bcl3-Slug signaling.Q41438372
Multiple hypothesis testing in proteomics: a strategy for experimental work.Q42173706
Quantitating drug-target engagement in single cells in vitro and in vivoQ42275555
Physicochemical determinants of passive membrane permeability: role of solute hydrogen-bonding potential and volume.Q43770038
Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand.Q45858607
ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signalingQ46707032
Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation.Q48000406
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic ScreenQ48125728
Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1.Q48151643
How Big Is Too Big for Cell Permeability?Q48197834
Targeting secondary protein complexes in drug discovery: studying the druggability and chemical biology of the HSP70/BAG1 complexQ48237303
Beyond Overton's rule: quantitative modeling of passive permeation through tight cell monolayers.Q48563848
Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC).Q50932257
An exact correction to the "Cheng-Prusoff" correction.Q52576210
A Perspective on the Kinetics of Covalent and Irreversible InhibitionQ60962649
Finding the sweet spot: the role of nature and nurture in medicinal chemistryQ84032484
P433issue3
P407language of work or nameEnglishQ1860
P304page(s)918-933
P577publication date2018-01-05
P1433published inJournal of Medicinal ChemistryQ900316
P1476titleDemonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)
P478volume61

Reverse relations

cites work (P2860)
Q92758130A critical evaluation of the approaches to targeted protein degradation for drug discovery
Q92042152Assessing the Cell Permeability of Bivalent Chemical Degraders Using the Chloroalkane Penetration Assay
Q90719868Critical Assessment of Targeted Protein Degradation as a Research Tool and Pharmacological Modality
Q92189593Developing degraders: principles and perspectives on design and chemical space
Q58417674Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure-Degradation Relationships
Q89996627Inducing the Degradation of Disease-Related Proteins Using Heterobifunctional Molecules
Q90186445PROTACs- a game-changing technology
Q92310282PROTACs: great opportunities for academia and industry
Q92758119PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future
Q89518885Principle and design of pseudo-natural products
Q64885983Privileged Structures and Polypharmacology within and between Protein Families.
Q92512732Protein-slaying drugs could be the next blockbuster therapies
Q95923717RAC1 as a Therapeutic Target in Malignant Melanoma
Q96431675Targeted protein degradation as a powerful research tool in basic biology and drug target discovery
Q59287278The size matters? A computational tool to design bivalent ligands

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