Ubiquitin‐independent, Proteasome‐mediated targeted degradation of KRAS in pancreatic adenocarcinoma cells using an engineered ornithine decarboxylase/antizyme system
Sign Up to like & getrecommendations! Published in 2019 at "Iubmb Life"
DOI: 10.1002/iub.1945
Abstract: The oncogene KRAS not only promotes the tumorigenesis of pancreatic cancers but also is required for the malignant progression and metastasis of these cancers. Many methods have been explored to influence the malignant biological behavior… read more here.
Keywords: degradation; ornithine decarboxylase; decarboxylase antizyme; targeted degradation ... See more keywords
Advances in targeted degradation of endogenous proteins
Sign Up to like & getrecommendations! Published in 2019 at "Cellular and Molecular Life Sciences"
DOI: 10.1007/s00018-019-03112-6
Abstract: Protein silencing is often employed as a means to aid investigations in protein function and is increasingly desired as a therapeutic approach. Several types of protein silencing methodologies have been developed, including targeting the encoding… read more here.
Keywords: protein; degradation endogenous; degradation; advances targeted ... See more keywords
Gluing Proteins for Targeted Degradation.
Sign Up to like & getrecommendations! Published in 2021 at "Cancer cell"
DOI: 10.1016/j.ccell.2020.12.020
Abstract: Targeted protein degradation is an emerging technology for drug development. An article published in Nature reported a novel mechanism of targeted protein degradation triggered by small-molecule-induced polymerization of the oncogenic transcription factor BCL6. read more here.
Keywords: degradation; proteins targeted; targeted degradation; gluing proteins ... See more keywords
Nucleic-Acid-Based Targeted Degradation in Drug Discovery.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00875
Abstract: Targeted protein degradation (TPD), represented by proteolysis-targeting chimera (PROTAC), has emerged as a novel therapeutic modality in drug discovery. However, the application of conventional PROTACs is limited to protein targets containing cytosolic domains with ligandable… read more here.
Keywords: degradation; targeted degradation; drug discovery; nucleic acid ... See more keywords
Targeted Degradation of MDM2 as a New Approach to Improve the Efficacy of MDM2-p53 Inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01945
Abstract: MDM2 is a key oncogenic protein that serves as a negative regulator of the tumor suppressor p53. While a number of inhibitors of the MDM2-p53 interaction have progressed to clinical testing as treatments for a… read more here.
Keywords: improve efficacy; mdm2 p53; targeted degradation;
Targeted Degradation of mRNA Decapping Enzyme DcpS by a VHL-Recruiting PROTAC.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical biology"
DOI: 10.1021/acschembio.2c00145
Abstract: The RNA decapping scavenger protein, DcpS, has recently been identified as a dependency in acute myeloid leukemia (AML). The potent DcpS inhibitor RG3039 attenuates AML cell viability, and shRNA knockdown of DcpS is also antiproliferative.… read more here.
Keywords: targeted degradation; dcps; aml cell; protac ... See more keywords
Targeted Degradation of KRASG12D as Potential Therapy in Cancer.
Sign Up to like & getrecommendations! Published in 2023 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.3c00111
Abstract: Selective proteolysis represents a cutting-edge therapeutic approach that is garnering global interest due to its capacity to eradicate pathogenic biomolecules within cellular environments. For instance, the PROTAC technology brings the ubiquitin proteasome system degradation machinery… read more here.
Keywords: potential therapy; therapy cancer; krasg12d potential; targeted degradation ... See more keywords
TF-PROTACs Enable Targeted Degradation of Transcription Factors.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.1c03852
Abstract: Transcription factors (TFs) represent a major class of therapeutic targets for the treatment of human diseases including cancer. Although the biological functions and even crystal structures of many TFs have been clearly elucidated, there is… read more here.
Keywords: degradation; protacs enable; targeted degradation; enable targeted ... See more keywords
Targeted Degradation of 53BP1 Using Ubiquitin Variant Induced Proximity
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12040479
Abstract: In recent years, researchers have leveraged the ubiquitin-proteasome system (UPS) to induce selective degradation of proteins by E3 ubiquitin ligases, which has great potential as novel therapeutics for human diseases, including cancer and neurodegenerative disorders.… read more here.
Keywords: ubiquitin variant; targeted degradation; proximity; variant induced ... See more keywords
Protein-Targeted Degradation Agents Based on Natural Products
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph16010046
Abstract: Natural products are an important source of drug lead compounds, and natural products with significant biological activity are constantly being discovered and used in clinical practice. At present, natural products play an important role in… read more here.
Keywords: natural products; targeted degradation; degradation agents; protacs molecular ... See more keywords