PROTAC

Targeted protein degradation services

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Eliminate disease-causing proteins: combine the benefits of small molecule drugs with gene-based knockdown technology.

  • to expedite your route to market with safer more effective PROTAC therapies
  • to provide valuable target validation for your protein of interest via targeted knock-down at the protein level

Proteolysis-targeting chimeras (PROTACs) are continuing to pave the way for precision targeted and better drugs for a range of diseases. The disruption of scaffolding function, potential to treat ‘undruggable’ proteins, as well as the catalytic mechanisms of action are just some of the many benefits of this new modality. 

The challenge

Working with PROTACs, however, does present some challenges, including:

  • Gaining access to the right expertise, technology and support needed to effectively characterize PROTAC efficacy and mechanism of action 
  • Being able to effectively assess critical parameters such as the order of binding to the target protein and E3 ubiquitin ligase, and identifying whether the target protein is ubiquitinated
  • Ensuring development programs remain compliant with the ever-shifting regulatory landscape, while also ensuring that technologies and approaches deployed work first-time

Bifunctional degraders of BRPF1 that retain the antiproliferative phenotype

Poster

The solution

Bring together state-of-the-art analytical technology and specialist expertise to overcome your PROTAC development challenges.

Concept Life Sciences is comprised of a diverse team of scientists and problem solvers who take an orthogonal approach to analytics and process development. 

Our medicinal, synthetic and computational chemists, ADME scientists and biologists offer a range of services designed to help you overcome challenges specific to your PROTAC development program – helping you accelerate your design-make-test cycle: 

  • Our customers are given direct access to a multidisciplinary team of application scientists with unequaled experience working within PROTAC development programs – meaning they can help you overcome the specific challenges you are facing and identify the right technology for your projects
  • Our chemists have significant experience of working with Cereblon, VHL and IAP-based PROTACs and have established a library of linkers available in-house, along with the knowledge and expertise on linker design and synthesis to accelerate your PROTAC program
  • We utilize state-of-the-art technologies that enable real-time characterization of both PROTAC efficacy and mechanism of action, addressing key questions to accelerate PROTAC development, profiling, and guidance on chemical structure−activity relationships. 

ADME profiling

Concept Life Sciences offers a range of in vitro ADMET and in vivo DMPK services, delivering high quality, accurate and reproducible data. In addition to our core service of validated robust assays, we can modify and/or customize your assay design, ensuring a science-led, flexible and quality-driven approach which is important for atypical molecules such as PROTACs. We will help you make technical choices or strategic decisions on test compound characterization, SAR generation and optimization of compound design, supporting you in de-risking your best route to clinic.

Computational modeling for PROTAC design

Computational modeling of your protein of interest, PROTAC and E3 ligase can facilitate the design of the best vectors and linker lengths. With state-of-the-art modeling software, we can provide structure based drug design (SBDD) support to prioritize and identify the best PROTAC design ideas.

Supporting your PROTAC research projects

We can prepare Fee-For-Service quotes for synthesis of discrete PROTACs upon request. Or to fully utilise our expertise, we are more than happy to discuss how our experts in Chemistry, Biology and ADME could bolster your PROTAC drug-discovery programs via an FTE approach. Our team of experienced scientists, with depth and breadth of knowledge and expertise, share your passion for delivering science.

How can we help you unlock a future of more targeted therapies?

To find out more about how our integrated team of experts can help you accelerate product development and speed up your route to market, contact us today.