Challenges of Academic Drug Discovery in Cancer
Tuesday April 27, 2021
4:00 pm
-
5:30 pm
Eastern Time (ET)
View session on the EB Virtual Platform (EB registration required)
BEH
DCP
DMDD
MP
TOX
Chair :
Markos Leggas
University of Kentucky
Michelle Arkin
University of California, San Francisco
This symposium will draw on the experiences of academic investigators to highlight their scientific efforts and challenges in academic drug discovery. Speakers will highlight individual paths and experiences including a new effort between academia and pharma to exploit artificial intelligence and machine learning to accelerate drug discovery. Presentations will feature diverse efforts to develop drugs with topics ranging from the development of new computational platforms for accelerating drug discovery, the identification and pharmacologic targeting of p97 as a novel cancer target, and the development of dual-kinase inhibitors as a polypharmacologic strategy for overcoming adaptive resistance to therapy in acute myeloid leukemia.
Speakers
Donna Huryn
- University of Pittsburgh
Discovery of P97 Modulators - An Emerging Cancer Target
P97, a AAA ATPase, plays an essential role in protein homeostasis, and is an emerging cancer target. This presentation will focus on the identification and optimization of allosteric inhibitors of p97 through a unique collaboration that brought together expertise in essential scientific disciplines.
Craig Thomas
- National Center for Advancing Translational Sciences (NCATS), NIH
Development of Dual RTK+IRAK Inhibitors as a Means to Overcome Adaptive Resistance in Multiple Cancer Settings
Kinase inhibitor therapy has transformed how we treat multiple cancers. Unfortunately, resistance to these drugs eventually emerges in the form of both adaptive and acquired resistance pathways. Here, we describe a dual FLT3/IRAK inhibitor with activity versus all known FLT3 mutations responsible for acquired resistance while also overcoming adaptive resistance manifested through amplified IRAK signaling.
Markos Leggas
- University of Kentucky
Drugging the ‘Undruggable’ – ETS Transcription Factor Inhibitors
Aberrant transcription factor fusions are the hallmark of Ewing sarcoma and are highly expressed in leukemia and prostate cancer. This presentation will focus on the discovery of novel mithramycin analogues that are highly potent and selective against Ewing sarcoma as well as the challenges of developing what might become the first therapeutic to target transcription factors directly.
Michelle Arkin
- University of California, San Francisco
Accelerating Discovery through AI – The ATOM Public/Private Consortium
Advances (and hype) in artificial intelligence and machine learning promise to accelerate discovery of new medicines. For academics, the ability to computationally optimize in vivo properties would have a dramatic impact on development of new chemical probes and experimental therapeutics. The ATOM consortium brings together state-of-the-art computing power with systems-level computational and experimental models with the goal of developing open-source data and methodologies to advance the science of AI in drug discovery.