Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs

article

Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs is …
instance of (P31):
scholarly articleQ13442814
review articleQ7318358

External links are
P356DOI10.1016/J.EBIOM.2018.09.005
P932PMC publication ID6197674
P698PubMed publication ID30224312

P2093author name stringLiwu Fu
Sainan An
P2860cites workFunctional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands.Q52673134
Multiplexed Proteome Dynamics Profiling Reveals Mechanisms Controlling Protein Homeostasis.Q52725933
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase using PROTAC-mediated Degradation.Q54977556
Small-molecule kinase inhibitors: an analysis of FDA-approved drugs.Q55052388
Greasy tags for protein removalQ59095262
Degradation of target protein in living cells by small-molecule proteolysis inducerQ75325862
Targeted degradation of the aryl hydrocarbon receptor by the PROTAC approach: a useful chemical genetic toolQ81377065
Protein targeting chimeric molecules specific for bromodomain and extra-terminal motif family proteins are active against pre-clinical models of multiple myelomaQ88182734
PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignanciesQ89014299
Identification of a primary target of thalidomide teratogenicityQ24302178
Molecular epidemiology of EGFR and KRAS mutations in 3,026 lung adenocarcinomas: higher susceptibility of women to smoking-related KRAS-mutant cancersQ24611043
Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomideQ24614147
The dynamic nature of the kinomeQ26852588
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
Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1αQ27674529
Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α InteractionQ27677509
Targeting of the MET receptor tyrosine kinase by small molecule inhibitors leads to MET accumulation by impairing the receptor downregulationQ28513426
DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradationQ28830958
Ubiquitination of hypoxia-inducible factor requires direct binding to the beta-domain of the von Hippel-Lindau proteinQ29615928
Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals).Q30313275
Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor.Q33942731
Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradationQ34083015
Small-molecule inhibitors of protein-protein interactions: progressing toward the realityQ34263719
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulatorsQ34294692
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.Q34478968
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.Q34479551
HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion ProteinsQ34480529
Catalytic in vivo protein knockdown by small-molecule PROTACs.Q34480735
Pharmacological targeting of the pseudokinase Her3Q34514043
Induced protein degradation: an emerging drug discovery paradigmQ34545841
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancerQ34610455
Cancer cell death induced by novel small molecules degrading the TACC3 protein via the ubiquitin-proteasome pathwayQ34662199
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomicsQ34815558
E3 ubiquitin ligases as cancer targets and biomarkersQ35082710
Nature Biotechnology's academic spinouts of 2013.Q35146529
Small-molecule modulation of Ras signalingQ35188280
Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic TaggingQ35666096
Small-Molecule PROTACS: New Approaches to Protein DegradationQ35891557
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
The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor StudiesQ36584337
EGFR exon 20 insertion mutations in lung adenocarcinomas: prevalence, molecular heterogeneity, and clinicopathologic characteristics.Q37021792
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancerQ37065079
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
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.Q38817737
Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells.Q39102535
Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.Q39406339
Use of PROTACS as molecular probes of angiogenesisQ39464707
Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein.Q39574650
Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins.Q39718603
Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancerQ39939428
Definition of functionally important mechanistic differences among selective estrogen receptor down-regulatorsQ40073529
Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras.Q40347061
Chemical genetic control of protein levels: selective in vivo targeted degradationQ40574972
Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cellsQ41190385
Acquired MET expression confers resistance to EGFR inhibition in a mouse model of glioblastoma multiforme.Q41816118
Inhibitor mediated protein degradation.Q42178606
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.Q42217007
Androgen receptor gene mutation, rearrangement, polymorphism.Q42738421
Results of the CONFIRM phase III trial comparing fulvestrant 250 mg with fulvestrant 500 mg in postmenopausal women with estrogen receptor-positive advanced breast cancer.Q42882393
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
Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands.Q45868652
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.Q47411643
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 StudyQ47411655
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
Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands.Q48265414
BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cellsQ50433449
Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC).Q50932257
The dTAG system for immediate and target-specific protein degradation.Q52340959
Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).Q52600736
P275copyright licenseCreative Commons Attribution-NonCommercial-NoDerivs 4.0 InternationalQ24082749
P407language of work or nameEnglishQ1860
P921main subjecttargeted therapyQ492646
biomedical investigative techniqueQ66648976
small molecule librariesQ50573438
P304page(s)553-562
P577publication date2018-10-01
P1433published inEBioMedicineQ24912341
P1476titleSmall-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
P478volume36

Reverse relations

cites work (P2860)
Q61809000Bivalent Ligands for Protein Degradation in Drug Discovery
Q92073027Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs
Q89810816Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells
Q89823393Degradation of proteins by PROTACs and other strategies
Q111442197Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins
Q92453516Dual targeting of SREBP2 and ERRα by carnosic acid suppresses RANKL-mediated osteoclastogenesis and prevents ovariectomy-induced bone loss
Q96128046Identification of a potent and selective covalent Pin1 inhibitor
Q92191065Neuroinflammation as a Factor of Neurodegenerative Disease: Thalidomide Analogs as Treatments
Q92647353Novel immunomodulatory drugs and neo-substrates
Q90186445PROTACs- a game-changing technology
Q92310282PROTACs: great opportunities for academia and industry
Q90461512Pharmacological Targeting of BET Bromodomain Proteins in Acute Myeloid Leukemia and Malignant Lymphomas: From Molecular Characterization to Clinical Applications
Q89462180Quantitating Endosomal Escape of a Library of Polymers for mRNA Delivery
Q92578345SMARCA2-deficiency confers sensitivity to targeted inhibition of SMARCA4 in esophageal squamous cell carcinoma cell lines
Q100407251Targeted Protein Degradation as a Promising Tool for Epigenetic Upregulation of Fetal Hemoglobin
Q89865609Targeting the SAGA and ATAC Transcriptional Coactivator Complexes in MYC-Driven Cancers

Search more.