Search engine for discovering works of Art, research articles, and books related to Art and Culture
Javascript must be enabled to continue!
Proteolysis targeting chimeras (PROTACs) in cancer therapy
View through CrossRef
AbstractExploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs). PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ligase. The bridging between the protein of interest and the E3 ligase mediated by the PROTAC facilitates ubiquitination of the protein and its proteasomal degradation. In this review we discuss the molecular medicine behind PROTAC mechanism of action, with special emphasis on recent developments and their potential translation to the clinical setting.
Springer Science and Business Media LLC
Title: Proteolysis targeting chimeras (PROTACs) in cancer therapy
Description:
AbstractExploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs).
PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ligase.
The bridging between the protein of interest and the E3 ligase mediated by the PROTAC facilitates ubiquitination of the protein and its proteasomal degradation.
In this review we discuss the molecular medicine behind PROTAC mechanism of action, with special emphasis on recent developments and their potential translation to the clinical setting.
Related Results
New Frontiers in the Discovery and Development of PROTACs
New Frontiers in the Discovery and Development of PROTACs
Abstract:
Proteolysis targeting chimeras (PROTACs) are an emerging class of targeted protein degraders that coopt the intracellular degradation machinery to selectively deplete the...
Abstract 403: Versican proteolysis in endometrial cancer
Abstract 403: Versican proteolysis in endometrial cancer
Abstract
Background: Endometrial cancer exhibits differential immunogenicity across molecular subtypes. Specifically, mismatch repair (MMR) deficiency in a subset of...
Edoxaban and Cancer-Associated Venous Thromboembolism: A Meta-analysis of Clinical Trials
Edoxaban and Cancer-Associated Venous Thromboembolism: A Meta-analysis of Clinical Trials
Abstract
Introduction
Cancer patients face a venous thromboembolism (VTE) risk that is up to 50 times higher compared to individuals without cancer. In 2010, direct oral anticoagul...
International Breast Cancer Study Group (IBCSG)
International Breast Cancer Study Group (IBCSG)
This section provides current contact details and a summary of recent or ongoing clinical trials being coordinated by International Breast Cancer Study Group (IBCSG). Clinical tria...
Variation in T and B Cell Deficiency in Different Mouse Allogeneic Radiation Chimeras
Variation in T and B Cell Deficiency in Different Mouse Allogeneic Radiation Chimeras
Abstract
The immunologic deficiency of allogeneic radiation chimeras was examined in vitro by culturing spleen cells of the chimera with allogeneic or syngeneic (to ...
Diagnostic Rate of the Cancer by BDORT Utilizing the Cancer Slide
Diagnostic Rate of the Cancer by BDORT Utilizing the Cancer Slide
Purpose:
To make a diagnosis of cancer with BDORT (resonance test), we can choose two methods. One is to use a chemical agent like Integrin α5β1 or Oncogene C-f...
Breast Carcinoma within Fibroadenoma: A Systematic Review
Breast Carcinoma within Fibroadenoma: A Systematic Review
Abstract
Introduction
Fibroadenoma is the most common benign breast lesion; however, it carries a potential risk of malignant transformation. This systematic review provides an ove...
Developing Pharmacokinetic/Pharmacodynamic Relationships With PROTACs
Developing Pharmacokinetic/Pharmacodynamic Relationships With PROTACs
Many examples of PROTACs possessing in vivo efficacy in pre-clinical studies have now been disclosed. While building pharmacokinetic (PK)/pharmacodynamic (PD) relationships is reco...