BARCELONA, Spain I May 14, 2020 I La Merie Publishing announced the release of its newest report about Targeted Protein Degradation. The report “Targeted Protein Degradation by Novel PROTACs and Molecular Glues 2020: a landscape analysis of companies, technologies, targets, investors and partners from an industry perspective” provides a landscape description and analysis of Targeted Protein Degradation (TPD) technologies and of discovery and development of TPD drug candidates from an industry perspective.
The human proteome accounts for more than 30,000 proteins that have multiple biological functions in the human body. However, more than >80% of proteins are still out of reach and remain undruggable targets. Targeted protein degradation has recently emerged as a novel pharmacological modality that promises to overcome small molecule limitations whilst retainding their key advantages.
The PROTAC technology takes advantage of the ubiquitin–proteasome system to selectively degrade a protein of interest (POI). In brief, a PROTAC is a bifunctional heterodimer that binds simultaneously to a POI and to an ubiquitin E3 ligase, the two ends being linked together by a chemical tether. The close vicinity of the POI and the E3 ligase caused by the PROTAC triggers its ubiquitination. The tagged POI is then recognized and decomposed by the proteasome 26S, therefore freeing the PROTAC for further iterative cycles of degradation. Thus, only sub-stoichiometric amounts are needed for potent activity. In comparison with a small-molecule inhibitor that requires high systemic exposure to sustain a pharmacological effect, the catalytic nature of PROTACs gives them the advantage to act effectively with a low systemic exposure, which is translated into reduced off-target problems and toxic side effects.
This report evaluates the industry landscape of targeted protein degradation with novel PROTAC and molecular glue technologies and compounds. The report is based on the identification and description of 20 major biopharmaceutical and 24 technology-focused companies with targeted protein degradation technologies and research and development activities.
The report brings you up-to-date with information about and analysis of
- Approaches of Targeted Protein Degradation with heterobifunctional PROteolysis‐TArgeting Chimeras (PROTACs) and monovalent molecular glue compounds;
- Stakeholders in the field: technology and major pharmaceutical companies and investors;
- Technologies of Targeted Protein Degradation;
- Targets and therapeutic area selected for PROTAC and molecular glue drug discovery;
- PROTAC Optimization: target identification, novel E3 ligases, ligase binders, linkers; ternary complex analysis
- New Approaches: lysosomal degradation, bio-PROTACs
- Preclinical and clinical experience with selected PROTACs and molecular glues;
- Financing situation of technology companies and key investors in the field
- Partnering deals with financial terms;
- Major pharmaceutical companies: in-house technologies, R&D, collaborations and equity purchase.
The report Targeted Protein Degradation by Novel PROTACs and Molecular Glues 2020: a landscape analysis of companies, technologies, targets, investors and partners from an industry perspective can be acquired at La Merie Publishing’s online store www.lamerie.com: https://lamerie.com/report/targeted-protein-degradation-by-novel-protacs-and-molecular-glues-2020-a-landscape-analysis-of-companies-technologies-targets-investors-and-partners-from-an-industry-perspective/
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SOURCE: La Merie Publishing