| P2093 | author name string | Craig M Crews | |
| | Mariell Pettersson | |
| P2860 | cites work | 3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation | Q89289670 |
| | Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action | Q91103575 |
| | SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate | Q91322597 |
| | Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity | Q91342440 |
| | Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach | Q91364216 |
| | Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin-proteasome pathway | Q91663988 |
| | Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion | Q93070327 |
| | Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation | Q93171987 |
| | IAP antagonists induce autoubiquitination of c-IAPs, NF-kappaB activation, and TNFalpha-dependent apoptosis | Q24300707 |
| | Identification of a primary target of thalidomide teratogenicity | Q24302178 |
| | Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide | Q24614147 |
| | In vivo activation of the p53 pathway by small-molecule antagonists of MDM2 | Q27642888 |
| | Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α | Q27674529 |
| | Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface | Q27674729 |
| | Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction | Q27677509 |
| | Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide | Q27684738 |
| | Structural basis of lenalidomide-induced CK1α degradation by the CRL4(CRBN) ubiquitin ligase | Q27704179 |
| | Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib | Q27853011 |
| | Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings | Q27861111 |
| | Small molecules destabilize cIAP1 by activating auto-ubiquitylation | Q28266432 |
| | Lenalidomide causes selective degradation of IKZF1 and IKZF3 in multiple myeloma cells | Q28303091 |
| | Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition | Q28822022 |
| | DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation | Q28830958 |
| | The druggable genome | Q29547361 |
| | Cancer drug resistance: an evolving paradigm | Q29616694 |
| | Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). | Q30313275 |
| | Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation | Q34083015 |
| | Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. | Q34478968 |
| | Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. | Q34479551 |
| | A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. | Q47411648 |
| | The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study | Q47411655 |
| | Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders | Q47423838 |
| | HaloTag7: a genetically engineered tag that enhances bacterial expression of soluble proteins and improves protein purification | Q47739171 |
| | Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation. | Q48000406 |
| | Quantitative Analysis of Ligand Induced Heterodimerization of Two Distinct Receptors | Q48059363 |
| | Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. | Q48100900 |
| | Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. | Q48151643 |
| | Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders. | Q48195544 |
| | Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway | Q48510798 |
| | Specific Knockdown of Endogenous Tau Protein by Peptide-Directed Ubiquitin-Proteasome Degradation | Q48801026 |
| | Proteolysis targeting peptide (PROTAP) strategy for protein ubiquitination and degradation. | Q50885577 |
| | Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC). | Q50932257 |
| | Thioamide substitution to probe the hydroxyproline recognition of VHL ligands. | Q52323183 |
| | The dTAG system for immediate and target-specific protein degradation. | Q52340959 |
| | Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). | Q52600736 |
| | Kinase inhibitors: the road ahead. | Q52653219 |
| | Phthalimide conjugations for the degradation of oncogenic PI3K. | Q52721092 |
| | Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand. | Q52866950 |
| | Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase using PROTAC-mediated Degradation. | Q54977556 |
| | Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules. | Q55043775 |
| | Trial watch: phase II and phase III attrition rates 2011-2012. | Q55057294 |
| | Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC) | Q57066011 |
| | Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance | Q57135992 |
| | Homo-PROTACs for the Chemical Knockdown of Cereblon | Q57152575 |
| | New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm | Q57787515 |
| | MDM2-recruiting PROTAC Offers Superior, Synergistic Anti-proliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53 | Q58546852 |
| | SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate | Q64269515 |
| | Delineating the role of cooperativity in the design of potent PROTACs for BTK. | Q64940546 |
| | What is the right dose? The elusive optimal biologic dose in phase I clinical trials | Q80192978 |
| | Targeted degradation of the aryl hydrocarbon receptor by the PROTAC approach: a useful chemical genetic tool | Q81377065 |
| | Development of the first small molecule histone deacetylase 6 (HDAC6) degraders | Q88999848 |
| | PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies | Q89014299 |
| | Targeted protein degradation and the enzymology of degraders | Q89051103 |
| | Plasticity in binding confers selectivity in ligand-induced protein degradation | Q89070297 |
| | HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins | Q34480529 |
| | Catalytic in vivo protein knockdown by small-molecule PROTACs. | Q34480735 |
| | Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS. | Q34483086 |
| | Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics | Q34815558 |
| | Immunomodulatory agents lenalidomide and pomalidomide co-stimulate T cells by inducing degradation of T cell repressors Ikaros and Aiolos via modulation of the E3 ubiquitin ligase complex CRL4(CRBN.). | Q35064910 |
| | Twenty years on: the impact of fragments on drug discovery | Q36078186 |
| | New strategy for renal fibrosis: Targeting Smad3 proteins for ubiquitination and degradation | Q36090421 |
| | 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 degradation | Q36306106 |
| | Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs | Q36895558 |
| | Degradation of Akt using protein-catalyzed capture agents. | Q36943802 |
| | A comprehensive mathematical model for three-body binding equilibria | Q37029337 |
| | Predicting druggable binding sites at the protein-protein interface. | Q37337290 |
| | The 26 S proteasome: from basic mechanisms to drug targeting | Q37610623 |
| | Targeting IAP proteins for therapeutic intervention in cancer | Q37980321 |
| | Enzalutamide: a review of its use in metastatic, castration-resistant prostate cancer | Q38152744 |
| | Molecular mechanisms of antibiotic resistance. | Q38272908 |
| | New Modalities for Challenging Targets in Drug Discovery | Q38289100 |
| | The demographics of the ubiquitin system | Q38439051 |
| | How Beyond Rule of 5 Drugs and Clinical Candidates Bind to Their Targets. | Q38604743 |
| | A snapshot of biologic drug development: Challenges and opportunities | Q38651271 |
| | 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 Scaffolds | Q38673230 |
| | Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. | Q38710711 |
| | Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL. | Q38817737 |
| | Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins. | Q39718603 |
| | Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras. | Q40347061 |
| | Ubiquitin, proteasomes, and the regulation of intracellular protein degradation | Q40445002 |
| | Properties, variants, and applications of the immunoradiometric assay method | Q40512337 |
| | Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation | Q40558374 |
| | Chemical genetic control of protein levels: selective in vivo targeted degradation | Q40574972 |
| | Cooperative binding mitigates the high-dose hook effect. | Q41396728 |
| | Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection. | Q41934667 |
| | Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. | Q42217007 |
| | Medicinal chemistry in drug discovery in big pharma: past, present and future | Q42696948 |
| | Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand. | Q45858607 |
| | Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins. | Q45867253 |
| | Know your target, know your molecule | Q46728119 |
| | Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766). | Q47294366 |
| | Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)- | Q47324161 |
| | Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones? | Q47396409 |
| | Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead. | Q47411643 |
| P921 | main subject | proteolysis | Q33123 |
| P304 | page(s) | 15-27 | |
| P577 | publication date | 2019-02-13 | |
| P1433 | published in | Drug discovery today. Technologies | Q27723323 |
| P1476 | title | PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future | |
| P478 | volume | 31 | |