标题
Proteolysis targeting chimeras (PROTACs) in cancer therapy
作者
关键词
-
出版物
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
Volume 39, Issue 1, Pages -
出版商
Springer Science and Business Media LLC
发表日期
2020-09-15
DOI
10.1186/s13046-020-01672-1
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Transcription Factor Inhibition: Lessons Learned and Emerging Targets
- (2020) Andrew Chen et al. TRENDS IN MOLECULAR MEDICINE
- Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
- (2019) Blake E. Smith et al. Nature Communications
- Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions
- (2019) Johannes Popow et al. JOURNAL OF MEDICINAL CHEMISTRY
- The 26S Proteasome Utilizes a Kinetic Gateway to Prioritize Substrate Degradation
- (2019) Jared A.M. Bard et al. CELL
- PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding
- (2019) Christopher P. Tinworth et al. ACS Chemical Biology
- Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader
- (2019) Hannah Tovell et al. ACS Chemical Biology
- From Inhibition to Degradation: Targeting the Anti-apoptotic Protein Myeloid Cell Leukemia 1 (MCL1)
- (2019) James William Papatzimas et al. JOURNAL OF MEDICINAL CHEMISTRY
- Acquired Resistance to BET-PROTACs(Proteolysis Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 ligase Complexes
- (2019) Lu Zhang et al. MOLECULAR CANCER THERAPEUTICS
- Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models
- (2019) M Catarina Silva et al. eLife
- Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation
- (2019) Hong Chen et al. BIOORGANIC CHEMISTRY
- Small Molecule Targets TMED9 and Promotes Lysosomal Degradation to Reverse Proteinopathy
- (2019) Moran Dvela-Levitt et al. CELL
- BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
- (2019) William Farnaby et al. Nature Chemical Biology
- Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16
- (2019) Xiaoyu Zhang et al. Nature Chemical Biology
- Targeting IRAK4 for Degradation with PROTACs
- (2019) Joao Nunes et al. ACS Medicinal Chemistry Letters
- Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader
- (2019) Hannah Tovell et al. ACS Chemical Biology
- Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer
- (2019) María del Mar Noblejas-López et al. JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
- Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders
- (2019) Shang Su et al. JOURNAL OF MEDICINAL CHEMISTRY
- Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK)
- (2019) Xiaotian Kong et al. JOURNAL OF MEDICINAL CHEMISTRY
- Plasticity of the Cullin-RING Ligase Repertoire Shapes Sensitivity to Ligand-Induced Protein Degradation
- (2019) Cristina Mayor-Ruiz et al. MOLECULAR CELL
- A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo
- (2019) Longchuan Bai et al. CANCER CELL
- Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity
- (2019) Thomas H. Pillow et al. ChemMedChem
- Antibody-Drug Conjugates: A Comprehensive Review
- (2019) Puregmaa Khongorzul et al. MOLECULAR CANCER RESEARCH
- Targeted protein degradation: expanding the toolbox
- (2019) Matthieu Schapira et al. NATURE REVIEWS DRUG DISCOVERY
- Lysosomes as dynamic regulators of cell and organismal homeostasis
- (2019) Andrea Ballabio et al. NATURE REVIEWS MOLECULAR CELL BIOLOGY
- Cellular quality control by the ubiquitin-proteasome system and autophagy
- (2019) Christian Pohl et al. SCIENCE
- PROTAC induced-BET protein degradation exhibits potent anti-osteosarcoma activity by triggering apoptosis
- (2019) Chengcheng Shi et al. Cell Death & Disease
- Design, Synthesis, and Biological Evaluation of MEK PROTACs
- (2019) Stefan Vollmer et al. JOURNAL OF MEDICINAL CHEMISTRY
- A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
- (2019) Sajid Khan et al. NATURE MEDICINE
- TRIB3 supports breast cancer stemness by suppressing FOXO1 degradation and enhancing SOX2 transcription
- (2019) Jin-mei Yu et al. Nature Communications
- Trastuzumab-Targeted Biodegradable Nanoparticles for Enhanced Delivery of Dasatinib in HER2+ Metastasic Breast Cancer
- (2019) Enrique Niza et al. Nanomaterials
- Structure and Function of the 26S Proteasome
- (2018) Jared A.M. Bard et al. Annual Review of Biochemistry
- Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression
- (2018) Chong Qin et al. JOURNAL OF MEDICINAL CHEMISTRY
- 3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation
- (2018) Andrea Testa et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)
- (2018) Chung Hyo Kang et al. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
- Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity
- (2018) Jinlei Bian et al. BIOORGANIC CHEMISTRY
- Refining Early Antitumoral Drug Development
- (2018) Alberto Ocaña et al. TRENDS IN PHARMACOLOGICAL SCIENCES
- Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
- (2018) Sainan An et al. EBioMedicine
- Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6
- (2018) William McCoull et al. ACS Chemical Biology
- UbiHub: a data hub for the explorers of ubiquitination pathways
- (2018) Lihua Liu et al. BIOINFORMATICS
- Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
- (2018) Vittoria Zoppi et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression
- (2018) Yangbing Li et al. JOURNAL OF MEDICINAL CHEMISTRY
- Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
- (2018) George M. Burslem et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation
- (2018) Philipp M. Cromm et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders
- (2017) Scott J. Hughes et al. Essays in Biochemistry
- 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)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)
- (2017) Pedro Soares et al. JOURNAL OF MEDICINAL CHEMISTRY
- 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
- (2017) Kwok-Ho Chan et al. JOURNAL OF MEDICINAL CHEMISTRY
- Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells
- (2017) D T Saenz et al. LEUKEMIA
- Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation
- (2017) Calla M Olson et al. Nature Chemical Biology
- Strategies and challenges for the next generation of antibody–drug conjugates
- (2017) Alain Beck et al. NATURE REVIEWS DRUG DISCOVERY
- BET inhibitors as novel therapeutic agents in breast cancer
- (2017) Alberto Ocaña et al. Oncotarget
- PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
- (2016) Kanak Raina et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
- (2015) Michael Zengerle et al. ACS Chemical Biology
- Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
- (2015) Ashton C. Lai et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
- (2015) Jing Lu et al. CHEMISTRY & BIOLOGY
- Oncogene addiction: pathways of therapeutic response, resistance, and road maps toward a cure
- (2015) R. Pagliarini et al. EMBO REPORTS
- Catalytic in vivo protein knockdown by small-molecule PROTACs
- (2015) Daniel P Bondeson et al. Nature Chemical Biology
- Phthalimide conjugation as a strategy for in vivo target protein degradation
- (2015) G. E. Winter et al. SCIENCE
- Paradigms of protein degradation by the proteasome
- (2014) Tomonao Inobe et al. CURRENT OPINION IN STRUCTURAL BIOLOGY
- 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 Affinities
- (2014) Carles Galdeano et al. JOURNAL OF MEDICINAL CHEMISTRY
- Targeting bromodomains: epigenetic readers of lysine acetylation
- (2014) Panagis Filippakopoulos et al. NATURE REVIEWS DRUG DISCOVERY
- Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib
- (2014) Jennifer A. Woyach et al. NEW ENGLAND JOURNAL OF MEDICINE
- Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface
- (2012) Inge Van Molle et al. CHEMISTRY & BIOLOGY
- HECT and RING finger families of E3 ubiquitin ligases at a glance
- (2012) M. B. Metzger et al. JOURNAL OF CELL SCIENCE
- Hallmarks of Cancer: The Next Generation
- (2011) Douglas Hanahan et al. CELL
- Selective inhibition of BET bromodomains
- (2010) Panagis Filippakopoulos et al. NATURE
- The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy
- (2010) L. A. Honigberg et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Control of cell growth by the SCF and APC/C ubiquitin ligases
- (2009) Jeffrey R Skaar et al. CURRENT OPINION IN CELL BIOLOGY
- Ubiquitin-like protein activation by E1 enzymes: the apex for downstream signalling pathways
- (2009) Brenda A. Schulman et al. NATURE REVIEWS MOLECULAR CELL BIOLOGY
- Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics
- (2008) Ashley R. Schneekloth et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Diversity of degradation signals in the ubiquitin–proteasome system
- (2008) Tommer Ravid et al. NATURE REVIEWS MOLECULAR CELL BIOLOGY
Find Funding. Review Successful Grants.
Explore over 25,000 new funding opportunities and over 6,000,000 successful grants.
ExploreFind the ideal target journal for your manuscript
Explore over 38,000 international journals covering a vast array of academic fields.
Search