PROTACs - Targeted Protein Degradation: Promises and Challenges Ahead
September 29, 2020 12:00 PM - 1:00 PM
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9/29/2020 12:00:00 PM
9/29/2020 1:00:00 PM
PROTACs - Targeted Protein Degradation: Promises and Challenges Ahead
Targeted protein degradation is an emerging therapeutic modality which has made tremendous progress and attracted massive investment in recent years. This modality is a class of bifunctional small molecules composed of an E3 ligase binder linked to a target protein binding moiety. It offers the possibility to degrade any intracellular target proteins regardless if there is a well-defined binding pocket in the target protein. Therefore, it opens numerous opportunities to drug many previously unreachable targets. However, the molecules tend to be bulky, floppy, greasy, and lack drug likeness properties. Nevertheless, increasing preclinical animal data has demonstrated the desired efficacy. Very recently, the early clinical safety and PK results are encouraging. In this forum our expert panel will share key learnings about this novel modality and discuss strategies to overcome potential challenges ahead.
Sponsored by MassBio's Drug Discovery forum working group.
MassBio makes every effort to accommodate our entire community at each of our events. Please let us know at least 3 days in advance of the event if you require special accommodations, such as captioning. Webinar, click "live-stream" button to view
Sponsored by MassBio's Drug Discovery forum working group.
MassBio makes every effort to accommodate our entire community at each of our events. Please let us know at least 3 days in advance of the event if you require special accommodations, such as captioning. Webinar, click "live-stream" button to view
- Paola Castaldi, PhD
- Director, Head of Chemical Biology and Proteomics at AstraZeneca
- Paola Castaldi is the Director and global Head of Chemical Biology & Proteomics at AstraZeneca. Her team is focused on supporting drug discovery programs across all therapeutics areas using state of the art technologies with specific emphasis on target identification, target engagement, MoA and off-target determination. Paola has played a critical role to establish a multi-omics and a therapeutic protein degradation platform at AstraZeneca providing both strategic and logistics directions. Before AstraZeneca, Paola was a key contributor of the Chemical Genetics group at Sanofi Oncology, Cambridge, MA with a focus on phenotypic drug discovery projects for the Wnt and KRAS oncogenic pathways. Prior to Sanofi Paola was at Makoto Life Sciences, where she was responsible for the chemistry strategies towards the identification of the PRPK/TPRKB complex as validated biological targets of immunomodulatory drugs that include lenalidomide (Revlimid), pomalidomide (Pomalyst) and thalidomide implicated in multiple myeloma. Paola Castaldi completed her undergraduate studies in pharmaceutical chemistry and received her Laurea (MSc) at University of Padova, Italy. She then went on to conduct graduate research studies at Imperial College London, UK and postdoctoral studies at UCSD and Boston University.
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- Adam M. Gilbert
- Senior Director - Discovery Sciences/Design and Synthesis Sciences, Pfizer
- Adam M. Gilbert received his B.A. in chemistry from Haverford College and his Ph.D. in organic chemistry from Columbia University working with Professor Thomas Katz. After a postdoctoral fellowship with Professor William Wulff at the University of Chicago, he joined Medical Research Division of American Cyanamid in Pearl River, NY which quickly became Wyeth Research. At Wyeth, Adam worked across multiple therapeutic areas: metabolic diseases, antibacterials, neuroscience, oncology and inflammation. He was also responsible for managing the Exploratory Chemistry Neuroscience Hit to Lead portfolio which ultimately produced several successful development programs. Adam joined Pfizer in Groton, CT in February 2010 as an Associate Research Fellow and a labhead in charge of the Experimental Design Chemistry – a group that focuses on key portfolio projects with challenging medicinal chemistry design issues including covalent inhibitors, allosteric GPCR modulators and chemoproteomics. His group helped successfully put multiple compounds into the clinic including PF-06651600, a selective JAK3 inhibitor currently in Ph III trials for Alopecia Areata. Adam Gilbert is currently a Senior Director at Pfizer where he leads Design and Synthesis Sciences – a medicinal chemistry group which focuses on new modalities and technologies in design, synthesis, computational chemistry, DEL chemistry, molecular properties and small molecule purification. His group is driving Pfizer’s effort on protein degradation.
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- Roy Pollock, PhD
- Senior Vice President, Biology at C4 Therapeutics
- Roy is Senior Vice President of Biology at C4 Therapeutics. Prior to joining C4 Therapeutics, Dr. Pollock was Vice President of Biology at Warp Drive Bio (acquired by Revolution Medicines) where he guided the discovery and characterization of inhibitors targeting the activated form of mutant KRAS using a novel tri-complex technology platform. Prior to joining Warp Drive, Dr. Pollock was at Epizyme where he led biology support for histone methyltransferase inhibitors targeting DOT1L (Pinometostat) and EZH2 (Tazverik™) from hit identification through to entry into Phase I clinical trials. Prior to Epizyme, Dr Pollock worked in oncology drug discovery at Merck Research Laboratories and ARIAD Pharmaceuticals. He holds a B.Sc. in biochemistry from St Andrews University in Scotland and a Ph.D. in Molecular Biology from Imperial College London.
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- Haojing Rong, PhD
- Vice President Of Preclinical Development, Kymera Therapeutics
- Haojing Rong is the Vice President of Preclinical Development at Kymera Therapeutics. She earned her Ph.D. at Faculty of Pharmaceutical Science of Ghent University in Belgium. Haojing started her career in the DMPK area at Amgen, Thousand Oaks, CA, followed by experiences at several large and small companies such as Merck, Amira Pharmaceuticals, and Pfizer Groton and Cambridge. She was a Director of Nonclinical Development at Shire prior to joining Kymera in 2018. Haojing’s interest and expertise include ADME and Tox knowledge integration for both small molecule and biotherapeutics, prediction of human pharmacokinetics, drug interactions using modeling and simulation, and applying integrated PK/PD modeling approach for both efficacy and safety for drug development.
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