We are pleased to announce the upcoming seminar titled "A critical evaluation of the approaches to targeted protein degradation for drug discovery and development: PROTAC versus Molecular glue degraders" presented by Serge Mignani, PhD, from CQM and the Centre d’Études et de Recherche sur le Médicament de Normandie & Argobio Studio, Paris (France). This seminar will take place on the 09th and 11th of June 2025 at the conference room 0.57, Campus of Penteada, University of Madeira, starting at 15:00 on both days.
Space is limited, so please be sure to complete your registration as soon as possible.
Abstract:
Protein degradation is the process by which proteins are broken down into smaller peptides or amino acids. Protein degraders are molecules that facilitate or enhance this process. Targeted protein degradation (TPD) was discovered twenty years ago through PROTAC technology and is now developing rapidly, thanks to the involvement of scientists from industry and academia. PROTAC chimeras are heterobifunctional molecules that can simultaneously link a protein to degradation and an E3 ubiquitin ligase. It has been demonstrated that PROTACs can degrade proteins that were previously considered "undruggable". Two PROTACs are currently undergoing clinical trials for the treatment of breast (ARV471) and prostate (ARV110) cancers. Proteasome-induced protein degradation is also induced by other types of molecules, such as molecular glues. A molecular glue is a proximity-inducible small molecule that can exert precise temporal control over various biological processes, including signal transduction, transcription, chromatin regulation, and the folding, localization, and degradation of proteins. As a chemical inducer of proximity, molecular glue can promote the dimerization or colocalization of two proteins through the formation of ternary complexes, leading to distinct biological and pharmacological functions.
Molecular glue degraders offer advantages in terms of drug-like properties and potential for central nervous system (CNS) indications, while PROTACs allow for rational design and broad targeting potential. Overcoming the challenges associated with each approach, such as the serendipitous discovery of molecular glue degraders and the drug-like properties of PROTACs, will be crucial for their successful clinical application.
As the field of TPD continues to evolve, we can expect to see the development of even more effective approaches.
Molecular glue and PROTAC strategies offer new avenues for drug development in the field of targeted protein degradation. Both molecular glue degraders and PROTACs show great promise as drugs.
In this presentation, we will analyze the characteristics, advantages, and limitations of each type of degrading molecule. We will also discuss the significant interest in identifying new drug targets that are difficult to access. Designing degraders, PROTAC is challenging because slight alterations to their structure can affect the formation of the ternary complex and subsequent degradation. We will also discuss this important aspect.
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Registration until 08th June 2025. |
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Registration form Limited seats available |