Proteolysis targeting chimera or PROTAC is a novel drug discovery strategy that has brought a paradigm shift and significant opportunity to transform the way medicinal chemistry and drug discovery programs are currently planned and executed. With sub-stoichiometric catalytic mode of action, PROTACs reduce the need for target occupancy as necessitated with traditional small molecule inhibitors. PROTACs hold great promise to target highly mutable kinases and signalling proteins, which promote cancer and drug resistance (e.g., KRAS, BRAF and EGFR).
This webinar will focus on our efforts with PROTACs in the areas of inflammation and cancer. Specifically, we will discuss challenges and opportunities for developing PROTACs in the areas of autoimmune and inflammatory diseases driven by IL-1R/TLR1 signaling and inflammasome activation and in potentially undruggable epigenetic pathways that involve bromodomain proteins, histone acetyltransferases and deacetylases.
Since targeted proteolysis relies on the cellular ubiquitination machinery, expanding the portfolio of E3 ligases will be crucial to broaden the capabilities of targeted protein degradation. This will be particularly impactful from the point of view of tissue specific expression of E3 ligases and those selectively expressed in diseased cells.
This webinar will also address some of the DMPK challenges of PROTACs. Properties of PROTACs fall mostly outside the “Lipinski rule of 5” of small molecule druggability and lead to complex DMPK optimization challenges. There is little IVIV correlation and unique strategies and optimizations are required for orally targeted protein degrader candidates. Panelists will share how the staff at GVK BIO have helped overcome some of these challenges to accelerate the development of PROTACs.
Amar Thyagarajan, Ph.D., Global Strategy Head and Head of North America BD (Biology Solutions), GVK Biosciences and Aragen Biosciences
Amar Thyagarajan heads the global strategy and North American business development for the Biology Solutions vertical at GVK BIO and Aragen Biosciences. He is a cell biologist and biochemist by training and holds a PhD in Neuroscience from the State University of New York and completed his post-doctoral fellowship at the Massachusetts Institute of Technology, Cambridge MA. Prior to joining GVK BIO/Aragen, Dr. Thyagarajan held leadership positions at Crown Biosciences and Taconic Biosciences.
Venkatesh Babu Jayaraman, Principal Scientific Manager, GVK Biosciences
Venkatesh Babu is a Principal Scientific Manager and leads in vitro biology assay development and screening for several PROTAC drug discovery projects at GVK BIO. He has been instrumental in establishing targeted protein degradation assays to support PROTAC research and his team has made significant contributions in screening PROTAC candidates using several assays in medium and high throughput formats. Babu has a Masters degree in Biochemistry from Madurai Kamaraj University and has 2 decades of experience in drug discovery. He has worked on various technology platforms including nanotechnology and high throughput automation.
Who Should Attend?
Director and Senior level professionals from biopharmaceutical companies, including:
- Research Scientist
- Principal Scientist
- Lead Scientist
- Associate Director
- Director-level Scientists Working on Targeted Protein Degrader 9TPD Programs or PROTAC programs.
- VP of Chemistry/Biology
- CSO leading TPD or PROTAC programs
- Academic Scientists Working on TPD/PROTAC
- Non-Profit Organization Scientists Working on TPD/PROTAC
What You Will Learn
In this webinar, participants will learn:
- PROTAC technology and challenges in the field
- Opportunities and strategies for developing PROTACs in cancer and inflammation
- Screening PROTACs: available tools and assays for mechanistic profiling
- DMPK optimization for oral bioavailability
GVK BIO is a global Contract Research and Development Organization (CRDO) providing research and development services to the biopharma and life sciences industry. We enable our customers to bring their products to market in a fast yet cost-efficient manner. GVK BIO employs a no-conflict model and ensures no internal programs that can potentially conflict with our customers projects. Our team of over 2500+ well qualified scientists, backed by rigorous processes, scalable practices, modern facilities and a strong customer-centric partnering approach, makes it India’s leading CRDO. Spread across 55 acres, GVK BIO has seven state-of-the-art research facilities: five in India and two in USA. All facilities conform to stringent regulatory standards. Our infrastructure has a built-up area of 1,200,000 sq. ft. housing chemistry labs, biology labs, analytical labs, formulation development labs, kilo labs, AAALAC accredited animal house, pilot plants and manufacturing facilities. GVK BIO has been assessed by all the leading regulatory agencies of the world including USFDA, WHO, PMDA, EDQM, MFDS and EMEA.
In 2014, GVK BIO acquired Aragen Bioscience, Inc., a US-based Biologics CRO. With Aragen, GVK BIO is uniquely positioned to support client programs in both small and large molecules.