Exploiting Cancer Vulnerabilities by Blocking of the DHODH and GPX4 Pathways: A Multifunctional Bodipy/PROTAC Nanoplatform for the Efficient Synergistic Ferroptosis Therapy.
Sign Up to like & getrecommendations! Published in 2023 at "Advanced healthcare materials"
DOI: 10.1002/adhm.202300871
Abstract: Ferroptosis is a form of programmed cell death and plays an important role in many diseases. Dihydroorotate dehydrogenase (DHODH) and glutathione peroxidase 4 (GPX4) play major roles in cell resistance to ferroptosis. Therefore, inactivation of… read more here.
Keywords: ferroptosis therapy; dhodh; protac; gpx4 ... See more keywords
An Oral PROTAC Targeting HPK1 Degradation Potentiates Anti-Solid Tumor Immunity.
Sign Up to like & getrecommendations! Published in 2024 at "Advanced materials"
DOI: 10.1002/adma.202411454
Abstract: Hematopoietic progenitor pinase1 (HPK1) knockout has been identified as an efficient route to enhance anti-tumor immune response. Here, this work develops an oral proteolysis targeting chimera (PROTAC) targeting HPK1 to efficiently and selectively degrade HPK1… read more here.
Keywords: protac; protac targeting; targeting hpk1; tumor ... See more keywords
PROTAC and Molecular Glue Degraders of the Oncogenic RNA Binding Protein Lin28
Sign Up to like & getrecommendations! Published in 2024 at "Macromolecular Bioscience"
DOI: 10.1002/mabi.202400427
Abstract: The interaction between proteins and RNA is crucial for regulating gene expression, with dysregulation often linked to diseases such as cancer. The RNA‐binding protein (RBP) Lin28 inhibits the tumor suppressor microRNA (miRNA) let‐7, making it… read more here.
Keywords: lin28; protac; molecular glue; binding protein ... See more keywords
Development of selective mono or dual PROTAC degrader probe of CDK isoforms.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111952
Abstract: Cyclin-dependent kinase (CDK) family members are promising molecular targets in discovering potent inhibitors in disease settings, they function differentially. CDK2, CDK4 and CDK6, directly regulate the cell cycle, while CDK9 primarily modulates the transcription regulation.… read more here.
Keywords: degrader; development selective; protac; selective mono ... See more keywords
Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112186
Abstract: Anti-apoptotic protein BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance, rendering it an attractive target for cancer treatment. However, BCL-XL inhibitors such as ABT-263 cannot be safely used in the clinic because… read more here.
Keywords: abt 263; protac; bcl degraders; target ... See more keywords
Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112800
Abstract: Histone deacetylases (HDACs) play important roles in inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD). Unravelling of and interfering with the functions of specific isoenzymes contributing to inflammation provides opportunities for drug development.… read more here.
Keywords: proteolysis targeting; protac; degradation; histone deacetylases ... See more keywords
The state of the art of PROTAC technologies for drug discovery.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114290
Abstract: Protein degradation technology has progressed dramatically since 2001 when proteolysis targeting chimera (PROTAC) was first reported. Various of distinctive degradation technologies based on PROTAC have been developed for the degradation of kinases, nuclear receptors, epigenetic… read more here.
Keywords: technologies drug; protac; protac technologies; degradation ... See more keywords
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemistry"
DOI: 10.1021/acs.biochem.8b00391
Abstract: Inhibition of Bruton's tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies, yet >80% of CLL patients develop… read more here.
Keywords: degradation; protac; btk; bruton tyrosine ... See more keywords
In Silico-Driven THIOMAB Approach for Stable PROTAC Conjugates by Docking Payloads in Antibody Cavities.
Sign Up to like & getrecommendations! Published in 2025 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.4c00588
Abstract: The heterobifunctional proteolysis targeting chimeras (PROTACs) are a class of emerging therapeutic modalities that enable selective degradation of target proteins in cells. As antibody payloads, they offer several advantages compared to conventional chemical toxins, such… read more here.
Keywords: protac; antibody; thiomab approach; silico driven ... See more keywords
PRosettaC: Rosetta Based Modeling of PROTAC Mediated Ternary Complexes
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.0c00589
Abstract: Proteolysis-targeting chimeras (PROTACs), which induce degradation by recruitment of an E3 ligase to a target protein, are gaining much interest as a new pharmacological modality. However, designing PROTACs is challenging. Formation of a ternary complex… read more here.
Keywords: protein; ternary complex; ternary complexes; protac ... See more keywords
Improved Accuracy for Modeling PROTAC-Mediated Ternary Complex Formation and Targeted Protein Degradation via New In Silico Methodologies.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.0c00897
Abstract: Extending upon our previous publication (Drummond, M., Williams, C., In Silico Modeling of PROTAC-mediated Ternary Complexes: Validation and Application, J. Chem. Inf. Model., 2019, 59, 1634-1644), in this work two additional computational methods are presented… read more here.
Keywords: ternary complex; protac mediated; protac; mediated ternary ... See more keywords