Craig M. Crews

Publications

• Multiplex CRISPR/Cas Screen in Regenerating Haploid Limbs of Chimeric Axolotls
  ELife. Jan, 2020  |   Pubmed ID: 31989926
• Proteolysis-Targeting Chimeras As Therapeutics and Tools for Biological Discovery
  Cell. Jan, 2020  |   Pubmed ID: 31955850
• Design, Synthesis and Biological Evaluation of Proteolysis Targeting Chimeras (PROTACs) As a BTK Degraders with Improved Pharmacokinetic Properties
  Bioorganic & Medicinal Chemistry Letters. Feb, 2020  |   Pubmed ID: 31879210
• Targeted Protein Degradation: Expanding the Toolbox
  Nature Reviews. Drug Discovery. 12, 2019  |   Pubmed ID: 31666732
• Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs
  ACS Central Science. Oct, 2019  |   Pubmed ID: 31660436
• Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation
  Cancer Research. Sep, 2019  |   Pubmed ID: 31311809
• Targeted Protein Internalization and Degradation by ENDosome TArgeting Chimeras (ENDTACs)
  ACS Central Science. Jun, 2019  |   Pubmed ID: 31263767
• PROteolysis TArgeting Chimeras (PROTACs) - Past, Present and Future
  Drug Discovery Today. Technologies. Apr, 2019  |   Pubmed ID: 31200855
• Protein Folding State-dependent Sorting at the Golgi Apparatus
  Molecular Biology of the Cell. 08, 2019  |   Pubmed ID: 31166830
• RUNX1-targeted Therapy for AML Expressing Somatic or Germline Mutation in RUNX1
  Blood. 07, 2019  |   Pubmed ID: 31023702
• Targeted Protein Degradation: Elements of PROTAC Design
  Current Opinion in Chemical Biology. 06, 2019  |   Pubmed ID: 31004963
• BETP Degradation Simultaneously Targets Acute Myelogenous Leukemia Stem Cells and the Microenvironment
  The Journal of Clinical Investigation. 05, 2019  |   Pubmed ID: 30829648
• Evolving Rules for Protein Degradation? Insights from the Zinc Finger Degrome
  Biochemistry. 02, 2019  |   Pubmed ID: 30681837
• Differential PROTAC Substrate Specificity Dictated by Orientation of Recruited E3 Ligase
  Nature Communications. 01, 2019  |   Pubmed ID: 30631068
• Targeting Nuclear β-catenin As Therapy for Post-myeloproliferative Neoplasm Secondary AML
  Leukemia. 06, 2019  |   Pubmed ID: 30575820
• MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity Via Simultaneous Degradation of BRD4 and Stabilization of P53
  Cancer Research. 01, 2019  |   Pubmed ID: 30385614
• Addressing Kinase-Independent Functions of Fak Via PROTAC-Mediated Degradation
  Journal of the American Chemical Society. 12, 2018  |   Pubmed ID: 30444612
• Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
  Journal of the American Chemical Society. 12, 2018  |   Pubmed ID: 30427680
• Androgen Receptor Degradation by the Proteolysis-targeting Chimera ARCC-4 Outperforms Enzalutamide in Cellular Models of Prostate Cancer Drug Resistance
  Communications Biology. 2018  |   Pubmed ID: 30271980
• Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure-Degradation Relationships
  ChemMedChem. 08, 2018  |   Pubmed ID: 29870139
• Targeted Protein Unfolding Uncovers a Golgi-specific Transcriptional Stress Response
  Molecular Biology of the Cell. 06, 2018  |   Pubmed ID: 29851555
• Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation
  Biochemistry. 07, 2018  |   Pubmed ID: 29851337
• Protein Targeting Chimeric Molecules Specific for Bromodomain and Extra-terminal Motif Family Proteins Are Active Against Pre-clinical Models of Multiple Myeloma
  Leukemia. 10, 2018  |   Pubmed ID: 29581547
• Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
  Cell Chemical Biology. 01, 2018  |   Pubmed ID: 29129718
• The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
  Cell Chemical Biology. 01, 2018  |   Pubmed ID: 29129716
• Lineage Tracing of Genome-edited Alleles Reveals High Fidelity Axolotl Limb Regeneration
  ELife. 09, 2017  |   Pubmed ID: 28917058
• The Proteasome in Modern Drug Discovery: Second Life of a Highly Valuable Drug Target
  ACS Central Science. Aug, 2017  |   Pubmed ID: 28852696
• Small-Molecule Modulation of Protein Homeostasis
  Chemical Reviews. Sep, 2017  |   Pubmed ID: 28777566
• Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation
  ACS Chemical Biology. 10, 2017  |   Pubmed ID: 28767222
• Targeted Protein Degradation: from Chemical Biology to Drug Discovery
  Cell Chemical Biology. Sep, 2017  |   Pubmed ID: 28648379
• Targeted Protein Knockdown Using Small Molecule Degraders
  Current Opinion in Chemical Biology. Aug, 2017  |   Pubmed ID: 28605671
• Waste Disposal-An Attractive Strategy for Cancer Therapy
  Science (New York, N.Y.). 03, 2017  |   Pubmed ID: 28302825
• Proteolysis-Targeting Chimeras: Induced Protein Degradation As a Therapeutic Strategy
  ACS Chemical Biology. 04, 2017  |   Pubmed ID: 28263557
• Targeted Protein Degradation by PROTACs
  Pharmacology & Therapeutics. Jun, 2017  |   Pubmed ID: 28223226
• Novel BET Protein Proteolysis-targeting Chimera Exerts Superior Lethal Activity Than Bromodomain Inhibitor (BETi) Against Post-myeloproliferative Neoplasm Secondary (s) AML Cells
  Leukemia. 09, 2017  |   Pubmed ID: 28042144
• Induced Protein Degradation: an Emerging Drug Discovery Paradigm
  Nature Reviews. Drug Discovery. 02, 2017  |   Pubmed ID: 27885283
• Targeted Protein Degradation by Small Molecules
  Annual Review of Pharmacology and Toxicology. 01, 2017  |   Pubmed ID: 27732798
• Expeditious Synthesis of Isoquinolones and Isocoumarins with a Vinyl Borane As an Acetylene Equivalent
  European Journal of Organic Chemistry. Aug, 2016  |   Pubmed ID: 28781577
• PROTAC-induced BET Protein Degradation As a Therapy for Castration-resistant Prostate Cancer
  Proceedings of the National Academy of Sciences of the United States of America. 06, 2016  |   Pubmed ID: 27274052
• Inducing Protein Degradation As a Therapeutic Strategy
  Journal of Medicinal Chemistry. 06, 2016  |   Pubmed ID: 27199030
• Identification of MAC1: A Small Molecule That Rescues Spindle Bipolarity in Monastrol-Treated Cells
  ACS Chemical Biology. 06, 2016  |   Pubmed ID: 27121275
• Small-Molecule PROTACS: New Approaches to Protein Degradation
  Angewandte Chemie (International Ed. in English). Feb, 2016  |   Pubmed ID: 26756721
• Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
  Angewandte Chemie (International Ed. in English). Jan, 2016  |   Pubmed ID: 26593377
• Development of Small Molecules Targeting the Pseudokinase Her3
  Bioorganic & Medicinal Chemistry Letters. Aug, 2015  |   Pubmed ID: 26094118
• Small-Molecule-Mediated Degradation of the Androgen Receptor Through Hydrophobic Tagging
  Angewandte Chemie (International Ed. in English). Aug, 2015  |   Pubmed ID: 26083457
• Catalytic in Vivo Protein Knockdown by Small-molecule PROTACs
  Nature Chemical Biology. Aug, 2015  |   Pubmed ID: 26075522
• HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins
  ACS Chemical Biology. Aug, 2015  |   Pubmed ID: 26070106
• Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
  Chemistry & Biology. Jun, 2015  |   Pubmed ID: 26051217
• Generating and Identifying Axolotls with Targeted Mutations Using Cas9 RNA-guided Nuclease
  Methods in Molecular Biology (Clifton, N.J.). 2015  |   Pubmed ID: 25740494
• Pharmacological Targeting of the Pseudokinase Her3
  Nature Chemical Biology. Dec, 2014  |   Pubmed ID: 25326665
• Targeted Protein Destabilization Reveals an Estrogen-mediated ER Stress Response
  Nature Chemical Biology. Nov, 2014  |   Pubmed ID: 25242550
• Highly Efficient Targeted Mutagenesis in Axolotl Using Cas9 RNA-guided Nuclease
  Development (Cambridge, England). May, 2014  |   Pubmed ID: 24764077
• Small-molecule Control of Intracellular Protein Levels Through Modulation of the Ubiquitin Proteasome System
  Angewandte Chemie (International Ed. in English). Feb, 2014  |   Pubmed ID: 24459094
• A Bidirectional System for the Dynamic Small Molecule Control of Intracellular Fusion Proteins
  ACS Chemical Biology. Oct, 2013  |   Pubmed ID: 23978068
• Posttranslational Protein Knockdown Coupled to Receptor Tyrosine Kinase Activation with PhosphoPROTACs
  Proceedings of the National Academy of Sciences of the United States of America. May, 2013  |   Pubmed ID: 23674677
• From Epoxomicin to Carfilzomib: Chemistry, Biology, and Medical Outcomes
  Natural Product Reports. May, 2013  |   Pubmed ID: 23575525
• Dissecting Fragment-based Lead Discovery at the Von Hippel-Lindau Protein:hypoxia Inducible Factor 1α Protein-protein Interface
  Chemistry & Biology. Oct, 2012  |   Pubmed ID: 23102223
• Small-molecule Inhibitors of the Interaction Between the E3 Ligase VHL and HIF1α
  Angewandte Chemie (International Ed. in English). Nov, 2012  |   Pubmed ID: 23065727
• Microarray Analysis of MicroRNA Expression During Axolotl Limb Regeneration
  PloS One. 2012  |   Pubmed ID: 23028429
• A HaloTag-based Small Molecule Microarray Screening Methodology with Increased Sensitivity and Multiplex Capabilities
  ACS Chemical Biology. Dec, 2012  |   Pubmed ID: 23013033
• Targeting the Von Hippel-Lindau E3 Ubiquitin Ligase Using Small Molecules to Disrupt the VHL/HIF-1α Interaction
  Journal of the American Chemical Society. Mar, 2012  |   Pubmed ID: 22369643
• Identification of Hydrophobic Tags for the Degradation of Stabilized Proteins
  Chembiochem : a European Journal of Chemical Biology. Mar, 2012  |   Pubmed ID: 22271667
• Disruption of Wnt Planar Cell Polarity Signaling by Aberrant Accumulation of the MetAP-2 Substrate Rab37
  Chemistry & Biology. Oct, 2011  |   Pubmed ID: 22035799
• Small-molecule Hydrophobic Tagging-induced Degradation of HaloTag Fusion Proteins
  Nature Chemical Biology. Aug, 2011  |   Pubmed ID: 21725302
• A Genetic Interaction Network of Five Genes for Human Polycystic Kidney and Liver Diseases Defines Polycystin-1 As the Central Determinant of Cyst Formation
  Nature Genetics. Jun, 2011  |   Pubmed ID: 21685914
• Triptolide Directly Inhibits DCTP Pyrophosphatase
  Chembiochem : a European Journal of Chemical Biology. Jul, 2011  |   Pubmed ID: 21671327
• Gene Expression Profile of the Regeneration Epithelium During Axolotl Limb Regeneration
  Developmental Dynamics : an Official Publication of the American Association of Anatomists. Jul, 2011  |   Pubmed ID: 21648017
• Natural Product Inhibitors of the Ubiquitin-proteasome Pathway
  Current Drug Targets. Oct, 2011  |   Pubmed ID: 21561423
• Unexpected Stereochemical Tolerance for the Biological Activity of Tyroscherin
  Bioorganic & Medicinal Chemistry. Mar, 2011  |   Pubmed ID: 21315614
• HIV Protease-mediated Activation of Sterically Capped Proteasome Inhibitors and Substrates
  Journal of the American Chemical Society. Feb, 2011  |   Pubmed ID: 21186803
• Total Synthesis and Biological Evaluation of Tyroscherin
  Organic Letters. Oct, 2010  |   Pubmed ID: 20831175
• Targeting the Undruggable Proteome: the Small Molecules of My Dreams
  Chemistry & Biology. Jun, 2010  |   Pubmed ID: 20609404
• Reversal of TNP-470-induced Endothelial Cell Growth Arrest by Guanine and Guanine Nucleosides
  The Journal of Pharmacology and Experimental Therapeutics. Sep, 2010  |   Pubmed ID: 20571059
• Activation of the Planar Cell Polarity Formin DAAM1 Leads to Inhibition of Endothelial Cell Proliferation, Migration, and Angiogenesis
  Proceedings of the National Academy of Sciences of the United States of America. Apr, 2010  |   Pubmed ID: 20351293
• Chemical Inducers of Targeted Protein Degradation
  The Journal of Biological Chemistry. Apr, 2010  |   Pubmed ID: 20147751
• Triptolide Reduces Cyst Formation in a Neonatal to Adult Transition Pkd1 Model of ADPKD
  Nephrology, Dialysis, Transplantation : Official Publication of the European Dialysis and Transplant Association - European Renal Association. Jul, 2010  |   Pubmed ID: 20139063
• Identification and Characterization of a Peptidic Ligand for Ras
  Chembiochem : a European Journal of Chemical Biology. Mar, 2010  |   Pubmed ID: 20082398
• Total Synthesis and Structure-activity Investigation of the Marine Natural Product Neopeltolide
  Journal of the American Chemical Society. Sep, 2009  |   Pubmed ID: 19663512
• Design and Applications of Bifunctional Small Molecules: Why Two Heads Are Better Than One
  ACS Chemical Biology. Nov, 2008  |   Pubmed ID: 19112665
• A Role for Planar Cell Polarity Signaling in Angiogenesis
  Angiogenesis. 2008  |   Pubmed ID: 18798004
• Targeted Intracellular Protein Degradation Induced by a Small Molecule: En Route to Chemical Proteomics
  Bioorganic & Medicinal Chemistry Letters. Nov, 2008  |   Pubmed ID: 18752944
• Triptolide Reduces Cystogenesis in a Model of ADPKD
  Journal of the American Society of Nephrology : JASN. Sep, 2008  |   Pubmed ID: 18650476
• Triptolide-induced Transcriptional Arrest is Associated with Changes in Nuclear Substructure
  Cancer Research. Jul, 2008  |   Pubmed ID: 18593926
• Proteasome Inhibition by Fellutamide B Induces Nerve Growth Factor Synthesis
  Chemistry & Biology. May, 2008  |   Pubmed ID: 18482702
• Chemical Genetics: Exploring the Role of the Proteasome in Cell Biology Using Natural Products and Other Small Molecule Proteasome Inhibitors
  Journal of Medicinal Chemistry. May, 2008  |   Pubmed ID: 18393403
• Molecular Understanding and Modern Application of Traditional Medicines: Triumphs and Trials
  Cell. Sep, 2007  |   Pubmed ID: 17803898
• Synthesis of the C3-C18 Fragment of Amphidinolides G and H
  Organic Letters. Aug, 2007  |   Pubmed ID: 17616200
• Triptolide is a Traditional Chinese Medicine-derived Inhibitor of Polycystic Kidney Disease
  Proceedings of the National Academy of Sciences of the United States of America. Mar, 2007  |   Pubmed ID: 17360534
• A Chemical and Genetic Approach to the Mode of Action of Fumagillin
  Chemistry & Biology. Sep, 2006  |   Pubmed ID: 16984890
• Myriaporone 3/4 Structure--activity Relationship Studies Define a Pharmacophore Targeting Eukaryotic Protein Synthesis
  Molecular BioSystems. Aug, 2006  |   Pubmed ID: 16880957
• Targeted Gene Disruption of Methionine Aminopeptidase 2 Results in an Embryonic Gastrulation Defect and Endothelial Cell Growth Arrest
  Proceedings of the National Academy of Sciences of the United States of America. Jul, 2006  |   Pubmed ID: 16790550
• Neurotrophic Peptide Aldehydes: Solid Phase Synthesis of Fellutamide B and a Simplified Analog
  Bioorganic & Medicinal Chemistry Letters. Jul, 2006  |   Pubmed ID: 16697191
• Synthetic Studies on Amphidinolide B1
  Organic Letters. Feb, 2006  |   Pubmed ID: 16435851
• Studies on Calcium Dependence Reveal Multiple Modes of Action for Triptolide
  Chemistry & Biology. Dec, 2005  |   Pubmed ID: 16356843
• Development and Characterization of Proteasome Inhibitors
  Methods in Enzymology. 2005  |   Pubmed ID: 16338383
• Stereoselective Assembly of a 1,3-diene Via Coupling Between an Allenic Acetate and a (B)-alkylborane: Synthetic Studies on Amphidinolide B1
  Organic Letters. Aug, 2005  |   Pubmed ID: 16092840
• Developing Microcolin A Analogs As Biological Probes
  Bioorganic & Medicinal Chemistry Letters. Sep, 2005  |   Pubmed ID: 15993592
• Chemical Approaches to Controlling Intracellular Protein Degradation
  Chembiochem : a European Journal of Chemical Biology. Jan, 2005  |   Pubmed ID: 15532104
• Total Synthesis of TMC-95A and -B Via a New Reaction Leading to Z-enamides. Some Preliminary Findings As to SAR
  Journal of the American Chemical Society. May, 2004  |   Pubmed ID: 15149232
• Chemical Genetic Control of Protein Levels: Selective in Vivo Targeted Degradation
  Journal of the American Chemical Society. Mar, 2004  |   Pubmed ID: 15038727
• A Single Amino Acid Residue Defines the Difference in Ovalicin Sensitivity Between Type I and II Methionine Aminopeptidases
  The Journal of Biological Chemistry. Mar, 2004  |   Pubmed ID: 14676204
• Small-molecule Inhibitors of the Cell Cycle: an Overview
  Progress in Cell Cycle Research. 2003  |   Pubmed ID: 14593706
• Feeding the Machine: Mechanisms of Proteasome-catalyzed Degradation of Ubiquitinated Proteins
  Current Opinion in Chemical Biology. Oct, 2003  |   Pubmed ID: 14580555
• Chemical Genetics: Adding to the Developmental Biology Toolbox
  Developmental Cell. Jul, 2003  |   Pubmed ID: 12852848
• Simplified Synthetic TMC-95A/B Analogues Retain the Potency of Proteasome Inhibitory Activity
  Chembiochem : a European Journal of Chemical Biology. Jun, 2003  |   Pubmed ID: 12794861
• Chemical Genetics: a Small Molecule Approach to Neurobiology
  Neuron. Nov, 2002  |   Pubmed ID: 12441047
• Inhibitors of NF-kappaB Signaling: Design and Synthesis of a Biotinylated Isopanepoxydone Affinity Reagent
  Bioorganic & Medicinal Chemistry Letters. Dec, 2002  |   Pubmed ID: 12419384
• Total Synthesis of Luminacin D
  Organic Letters. Sep, 2002  |   Pubmed ID: 12201723
• Characterization of a Novel Mammalian Phosphatase Having Sequence Similarity to Schizosaccharomyces Pombe PHO2 and Saccharomyces Cerevisiae PHO13
  Biochemistry. Jun, 2002  |   Pubmed ID: 12056916
• Protacs: Chimeric Molecules That Target Proteins to the Skp1-Cullin-F Box Complex for Ubiquitination and Degradation
  Proceedings of the National Academy of Sciences of the United States of America. Jul, 2001  |   Pubmed ID: 11438690
• The Ubiquitin-proteasome Pathway and Proteasome Inhibitors
  Medicinal Research Reviews. Jul, 2001  |   Pubmed ID: 11410931
• Cells Adapted to the Proteasome Inhibitor 4-hydroxy- 5-iodo-3-nitrophenylacetyl-Leu-Leu-leucinal-vinyl Sulfone Require Enzymatically Active Proteasomes for Continued Survival
  Proceedings of the National Academy of Sciences of the United States of America. Jan, 2001  |   Pubmed ID: 11149939
• The Antiangiogenic Agent TNP-470 Requires P53 and P21CIP/WAF for Endothelial Cell Growth Arrest
  Proceedings of the National Academy of Sciences of the United States of America. Nov, 2000  |   Pubmed ID: 11070090
• The Selective Proteasome Inhibitors Lactacystin and Epoxomicin Can Be Used to Either Up- or Down-regulate Antigen Presentation at Nontoxic Doses
  Journal of Immunology (Baltimore, Md. : 1950). Jun, 2000  |   Pubmed ID: 10843664
• Epoxomicin, a Potent and Selective Proteasome Inhibitor, Exhibits in Vivo Antiinflammatory Activity
  Proceedings of the National Academy of Sciences of the United States of America. Aug, 1999  |   Pubmed ID: 10468620
• The Anti-angiogenic Agent Fumagillin Covalently Binds and Inhibits the Methionine Aminopeptidase, MetAP-2
  Proceedings of the National Academy of Sciences of the United States of America. Jun, 1997  |   Pubmed ID: 9177176